Trial Outcomes & Findings for A Study to Assess Absolute Bioavailability (ABA) of Mobocertinib (TAK-788) and to Characterize Mass Balance, Pharmacokinetics (PK), Metabolism, and Excretion of Carbon-14 ([14C])-Mobocertinib in Male Healthy Participants (NCT NCT03811834)

Results Overview

Absolute bioavailability (F), defined as the fraction or percentage of the unchanged, orally administered dose that is systemically available, relative to the total dose administered intravenously. Percent Absolute Oral Bioavailability (%F) was calculated as dose of \[14C\]-mobocertinib intravenous in mg\*AUC∞ of mobocertinib (oral)/dose of mobocertinib (oral)\* AUC∞ of \[14C\]-mobocertinib (intravenous)\*100.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

7 participants

Primary outcome timeframe

Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Results posted on

2024-02-12

Participant Flow

Participants took part in the study at 1 investigative site in the United States from 22 January 2019 to 11 March 2019.

Healthy male participants were enrolled in this 2-period study to receive mobocertinib 160 milligram (mg), capsules followed by carbon-14 \[14C\]-mobocertinib 50 microgram (mcg), infusion in Period 1 (Absolute Bioavailability \[ABA\]) and \[14C\]-mobocertinib 160 mg, solution in Period 2 (Absorption, Distribution, Metabolism, and Elimination \[ADME\]).

Participant milestones

Participant milestones
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg + [14C]-Mobocertinib 160 mg Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 microcurie \[mcCi\]), infusion, intravenously, once on Day 1 of Period 1, further followed by a washout period of 9 days, followed by \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1 ( 7 Days) STARTED	7
Period 1 ( 7 Days) COMPLETED	6
Period 1 ( 7 Days) NOT COMPLETED	1
Washout Period (9 Days) STARTED	6
Washout Period (9 Days) COMPLETED	6
Washout Period (9 Days) NOT COMPLETED	0
Period 2 (10 Days) STARTED	6
Period 2 (10 Days) COMPLETED	6
Period 2 (10 Days) NOT COMPLETED	0

Reasons for withdrawal

Reasons for withdrawal
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg + [14C]-Mobocertinib 160 mg Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 microcurie \[mcCi\]), infusion, intravenously, once on Day 1 of Period 1, further followed by a washout period of 9 days, followed by \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1 ( 7 Days) Adverse Event	1

Baseline Characteristics

A Study to Assess Absolute Bioavailability (ABA) of Mobocertinib (TAK-788) and to Characterize Mass Balance, Pharmacokinetics (PK), Metabolism, and Excretion of Carbon-14 ([14C])-Mobocertinib in Male Healthy Participants

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg +[14C]-Mobocertinib 160 mg n=7 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1, further followed by a washout period of 9 days, followed by \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Age, Continuous	38.6 years STANDARD_DEVIATION 12.75 • n=5 Participants
Sex: Female, Male Female	0 Participants n=5 Participants
Sex: Female, Male Male	7 Participants n=5 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	2 Participants n=5 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	5 Participants n=5 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=5 Participants
Race (NIH/OMB) Asian	0 Participants n=5 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	1 Participants n=5 Participants
Race (NIH/OMB) Black or African American	1 Participants n=5 Participants
Race (NIH/OMB) White	5 Participants n=5 Participants
Race (NIH/OMB) More than one race	0 Participants n=5 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants
Region of Enrollment United States	7 Participants n=5 Participants
Weight	83.74 kilogram (Kg) STANDARD_DEVIATION 6.141 • n=5 Participants
Height	175.9 centimeter (cm) STANDARD_DEVIATION 4.14 • n=5 Participants
Body mass index (BMI)	27.079 kilogram per square meter (kg/m^2) STANDARD_DEVIATION 1.6520 • n=5 Participants

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The pharmacokinetic (PK) set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This outcome measure (OM) was planned to be assessed only in Period 1.

Absolute bioavailability (F), defined as the fraction or percentage of the unchanged, orally administered dose that is systemically available, relative to the total dose administered intravenously. Percent Absolute Oral Bioavailability (%F) was calculated as dose of \[14C\]-mobocertinib intravenous in mg\*AUC∞ of mobocertinib (oral)/dose of mobocertinib (oral)\* AUC∞ of \[14C\]-mobocertinib (intravenous)\*100.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1: Percent Absolute Oral Bioavailability (%F) for Mobocertinib	36.7 percentage bioavailability Interval 22.4 to 60.2	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Urine Relative to the Administered Radioactive Dose	3.57 percentage of radioactive dose Geometric Coefficient of Variation 12.6	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Feces Relative to the Administered Radioactive Dose	76.0 percentage of radioactive dose Geometric Coefficient of Variation 6.5	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2: Amount of Total Radioactivity Excreted in Urine (Ae[UR])	5.777 milligram equivalent (mg eq) Geometric Coefficient of Variation 12.6	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2: Amount of Total Radioactivity Excreted in Feces (Ae[Fe])	123.1 mg eq Geometric Coefficient of Variation 6.1	—

PRIMARY outcome

Timeframe: Day 1: Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed "n" are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib Pre-dose	0.00 percentage of radioactive dose Standard Deviation 0.00	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 0-12 hours	1.061 percentage of radioactive dose Standard Deviation 0.22924	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 12-24 hours	0.7462 percentage of radioactive dose Standard Deviation 0.15716	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 24-48 hours	0.7364 percentage of radioactive dose Standard Deviation 0.12118	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 48-72 hours	0.3443 percentage of radioactive dose Standard Deviation 0.051037	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 72-96 hours	0.2173 percentage of radioactive dose Standard Deviation 0.040842	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 96-120 hours	0.1425 percentage of radioactive dose Standard Deviation 0.027883	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 120-144 hours	0.1050 percentage of radioactive dose Standard Deviation 0.021753	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 144-168 hours	0.07582 percentage of radioactive dose Standard Deviation 0.041180	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 168-192 hours	0.07517 percentage of radioactive dose Standard Deviation 0.012835	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 192-216 hours	0.05243 percentage of radioactive dose Standard Deviation 0.029772	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib 216-240 hours	0.05137 percentage of radioactive dose Standard Deviation 0.029359	—

PRIMARY outcome

Timeframe: Day 1: at Pre-dose, 0-24 hours (hrs), 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs; 240-264 hrs, 264-288 hrs, 288-312 hrs, 213-408 hrs and 408-432 hrs

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed "n" are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib Pre-dose	0.00 percentage of radioactive dose Standard Deviation 0.00	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 0-24 hours	16.13 percentage of radioactive dose Standard Deviation 16.772	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 24-48 hours	27.78 percentage of radioactive dose Standard Deviation 19.584	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 48-72 hours	16.10 percentage of radioactive dose Standard Deviation 21.089	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 72-96 hours	4.214 percentage of radioactive dose Standard Deviation 5.3488	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 96-120 hours	3.066 percentage of radioactive dose Standard Deviation 2.8311	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 120-144 hours	1.638 percentage of radioactive dose Standard Deviation 1.8080	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 144-168 hours	2.756 percentage of radioactive dose Standard Deviation 3.3943	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 168-192 hours	0.9919 percentage of radioactive dose Standard Deviation 0.83406	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 192-216 hours	2.069 percentage of radioactive dose Standard Deviation 1.0034	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 216-240 hours	1.695 percentage of radioactive dose Standard Deviation 1.1513	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 240-264 hours	0.1056 percentage of radioactive dose Standard Deviation 0.14927	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 264-288 hours	0.2216 percentage of radioactive dose Standard Deviation 0.31341	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 288-312 hours	0.7632 percentage of radioactive dose Standard Deviation NA Standard deviation could not be calculated because single participant was analyzed.	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 312-408 hours	0.3107 percentage of radioactive dose Standard Deviation NA Standard deviation could not be calculated because single participant was analyzed.	—
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib 408-432 hours	0.1143 percentage of radioactive dose Standard Deviation NA Standard deviation could not be calculated because single participant was analyzed.	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: Mobocertinib	51.0 ng/mL Geometric Coefficient of Variation 34.9	—
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32960	22.7 ng/mL Geometric Coefficient of Variation 19.8	—
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32914	4.28 ng/mL Geometric Coefficient of Variation 34.7	—
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: Mobocertinib	40.5 ng/mL Geometric Coefficient of Variation 29.1	—
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32960	26.7 ng/mL Geometric Coefficient of Variation 10.6	—
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32914	3.05 ng/mL Geometric Coefficient of Variation 28.6	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: Mobocertinib	6.00 hours Interval 3.0 to 6.0	—
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32960	4.00 hours Interval 3.0 to 5.0	—
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32914	6.00 hours Interval 3.0 to 6.0	—
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: Mobocertinib	5.01 hours Interval 2.01 to 6.01	—
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32960	5.01 hours Interval 3.02 to 5.01	—
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32914	5.01 hours Interval 4.01 to 6.01	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood Plasma: Mobocertinib	22.8 hours Geometric Coefficient of Variation 26.6	—
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood Plasma: AP32960	30.5 hours Geometric Coefficient of Variation 21.1	—
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood Plasma: AP32914	14.0 hours Geometric Coefficient of Variation 30.6	—
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood Whole Blood: Mobocertinib	20.5 hours Geometric Coefficient of Variation 25.4	—
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood Whole Blood: AP32960	30.9 hours Geometric Coefficient of Variation 12.1	—
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood Whole Blood: AP32914	12.8 hours Geometric Coefficient of Variation 23.1	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: Mobocertinib	956 nanogramhour per milliliter (nghr/mL) Geometric Coefficient of Variation 38.6	—
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32960	486 nanogramhour per milliliter (nghr/mL) Geometric Coefficient of Variation 26.7	—
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32914	73.4 nanogramhour per milliliter (nghr/mL) Geometric Coefficient of Variation 39.9	—
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: Mobocertinib	729 nanogramhour per milliliter (nghr/mL) Geometric Coefficient of Variation 32.8	—
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32960	556 nanogramhour per milliliter (nghr/mL) Geometric Coefficient of Variation 20.2	—
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32914	52.4 nanogramhour per milliliter (nghr/mL) Geometric Coefficient of Variation 37.3	—

PRIMARY outcome

Timeframe: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: Mobocertinib	945 ng*hr/mL Geometric Coefficient of Variation 39.2	—
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32960	471 ng*hr/mL Geometric Coefficient of Variation 27.5	—
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32914	63.6 ng*hr/mL Geometric Coefficient of Variation 45.7	—
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: Mobocertinib	718 ng*hr/mL Geometric Coefficient of Variation 33.2	—
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32960	543 ng*hr/mL Geometric Coefficient of Variation 20.5	—
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32914	45.7 ng*hr/mL Geometric Coefficient of Variation 40.4	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: Mobocertinib	944.9 ng*hr/mL Geometric Coefficient of Variation 39.2	—
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32960	471.1 ng*hr/mL Geometric Coefficient of Variation 27.5	—
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) Plasma: AP32914	63.61 ng*hr/mL Geometric Coefficient of Variation 45.7	—
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: Mobocertinib	717.7 ng*hr/mL Geometric Coefficient of Variation 33.2	—
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32960	542.8 ng*hr/mL Geometric Coefficient of Variation 20.5	—
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) Whole Blood: AP32914	45.74 ng*hr/mL Geometric Coefficient of Variation 40.4	—

PRIMARY outcome

Timeframe: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, Cmax: Maximum Observed Plasma Radioactivity Concentration Equivalents for [14C]-Mobocertinib	1250 nanogram equivalent/milliliter(ng eq/mL) Geometric Coefficient of Variation 13.4	—

PRIMARY outcome

Timeframe: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, Cmax: Maximum Observed Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib	725 nanogram equivalent/ gram (ng eq/g) Geometric Coefficient of Variation 14.6	—

PRIMARY outcome

Timeframe: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) Equivalents for [14C]-Mobocertinib Plasma	24.0 hours Interval 8.02 to 36.0	—
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) Equivalents for [14C]-Mobocertinib Whole Blood	24.0 hours Interval 8.01 to 36.0	—

PRIMARY outcome

Timeframe: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, t(1/2z): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib Plasma	281 hours Geometric Coefficient of Variation 29.1	—
Period 2, t(1/2z): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib Whole Blood	301 hours Geometric Coefficient of Variation 28.1	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUC∞: Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib	556000 nanogram equivalent*hour per milliliter Geometric Coefficient of Variation 14.9	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUC∞: Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib	325000 nanogram equivalent*hour per gram Geometric Coefficient of Variation 21.2	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUClast: Area Under the Plasma Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib	230300 nanogram equivalent*hour per milliliter Geometric Coefficient of Variation 15.5	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUClast: Area Under the Whole Blood Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]- Mobocertinib	131000 nanogram equivalent*hour per gram Geometric Coefficient of Variation 18.5	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUCt : Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib	145400 nanogram equivalent*hour per milliliter Geometric Coefficient of Variation 35.3	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, AUCt : Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib	70190 nanogram equivalent*hour per gram Geometric Coefficient of Variation 32.4	—

PRIMARY outcome

Timeframe: Day 1: at Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs and 216-240 hrs post dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed "n" are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 120 to 144 hours	0.005860 mg Standard Deviation 0.0055472	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: Pre-dose	0.001072 mg Standard Deviation 0.0010474	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 0 to 12 hours	0.1917 mg Standard Deviation 0.10878	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 12 to 24 hours	0.2047 mg Standard Deviation 0.084347	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 24 to 48 hours	0.1628 mg Standard Deviation 0.050589	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 48 to 72 hours	0.05069 mg Standard Deviation 0.029114	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 72 to 96 hours	0.02087 mg Standard Deviation 0.013052	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 96 to 120 hours	0.01028 mg Standard Deviation 0.0052244	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 144 to 168 hours	0.002438 mg Standard Deviation 0.0014131	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 168 to 192 hours	0.0009682 mg Standard Deviation 0.0011637	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 192 to 216 hours	0.0009890 mg Standard Deviation 0.00090295	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib: 216 to 240 hours	0.0002824 mg Standard Deviation 0.00063158	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: Pre-dose	0.005308 mg Standard Deviation 0.0045461	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 0-12 hours	0.2948 mg Standard Deviation 0.078117	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 12-24 hours	0.2199 mg Standard Deviation 0.056834	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 24-48 hours	0.2166 mg Standard Deviation 0.049030	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 48-72 hours	0.09444 mg Standard Deviation 0.020647	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 72-96 hours	0.05401 mg Standard Deviation 0.014311	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 96-120 hours	0.03017 mg Standard Deviation 0.0070669	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 120-144 hours	0.01764 mg Standard Deviation 0.0068670	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 144-168 hours	0.01082 mg Standard Deviation 0.0028229	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 168-192 hours	0.007272 mg Standard Deviation 0.0023649	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 192-216 hours	0.005427 mg Standard Deviation 0.0021935	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960: 216-240 hours	0.004235 mg Standard Deviation 0.0016891	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: Pre-dose	0.00 mg Standard Deviation 0.00	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 0-12 hours	0.08336 mg Standard Deviation 0.022896	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 12-24 hours	0.06029 mg Standard Deviation 0.015305	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 24-48 hours	0.04953 mg Standard Deviation 0.021338	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 48-72 hours	0.01543 mg Standard Deviation 0.0068257	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 72-96 hours	0.005859 mg Standard Deviation 0.0040117	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 96-120 hours	0.002477 mg Standard Deviation 0.0016606	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 120-144 hours	0.0008353 mg Standard Deviation 0.0010134	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 144-168 hours	0.0001780 mg Standard Deviation 0.00043613	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 168-192 hours	0.00 mg Standard Deviation 0.00	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 192-216 hours	0.00 mg Standard Deviation 0.00	—
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914: 216-240 hours	0.00 mg Standard Deviation 0.00	—

PRIMARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914) Mobocertinib	0.657 liter per hour ( L/h) Geometric Coefficient of Variation 44.3	—
Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32960	1.95 liter per hour ( L/h) Geometric Coefficient of Variation 22.5	—
Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914) AP32914	2.85 liter per hour ( L/h) Geometric Coefficient of Variation 27.9	—

PRIMARY outcome

Timeframe: At 0.5 hours (hrs), 1 hr, 2 hrs, 3 hrs, 4 hrs, 5 hrs, 6 hrs, 8 hrs, 12 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs, 144 hrs, 168 hrs, 192 hrs, 216 hrs and 240 hrs post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed "n" are the participants who were evaluable for the outcome measure at given timepoints. Here, '0' in the number analyzed field signifies that no participants were evaluable at specified time points. This OM was planned to be assessed only in Period 2.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 5 hours	0.8545 ratio Geometric Coefficient of Variation 17.2	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 0.5 hour	1.022 ratio Geometric Coefficient of Variation 21.9	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 1 hour	0.9851 ratio Geometric Coefficient of Variation 36.0	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 2 hours	0.9055 ratio Geometric Coefficient of Variation 25.3	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 3 hours	0.8403 ratio Geometric Coefficient of Variation 22.4	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 4 hours	0.8221 ratio Geometric Coefficient of Variation 23.3	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 6 hours	0.7647 ratio Geometric Coefficient of Variation 18.6	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 8 hours	0.7634 ratio Geometric Coefficient of Variation 20.7	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 12 hours	0.7573 ratio Geometric Coefficient of Variation 17.6	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 24 hours	0.8139 ratio Geometric Coefficient of Variation 23.0	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 36 hours	0.7028 ratio Geometric Coefficient of Variation 13.2	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 48 hours	0.7113 ratio Geometric Coefficient of Variation 14.7	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 72 hours	0.6453 ratio Geometric Coefficient of Variation 18.8	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 96 hours	0.6164 ratio Geometric Coefficient of Variation 18.0	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 120 hours	0.6260 ratio Geometric Coefficient of Variation 13.2	—
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) At 144 hours	0.5946 ratio Geometric Coefficient of Variation NA Geometric coefficient of variation could not be calculated because single participant was analyzed.	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) [14C]-Mobocertinib	146.3 picograms per milliliter (pg /mL) Geometric Coefficient of Variation 46.4	—
Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) [14C]- AP32960	1.842 picograms per milliliter (pg /mL) Geometric Coefficient of Variation 20.5	—
Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) [14C]- AP32914	2.432 picograms per milliliter (pg /mL) Geometric Coefficient of Variation 9.3	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration Mobocertinib	56.7 ng/mL Geometric Coefficient of Variation 52.2	—
Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration AP32960	23.29 ng/mL Geometric Coefficient of Variation 21.2	—
Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration AP32914	4.086 ng/mL Geometric Coefficient of Variation 36.0	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-mobocertinib	148 pg/mL Geometric Coefficient of Variation 44.0	—
Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-AP32960	6.631 pg/mL Geometric Coefficient of Variation 76.4	—
Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-AP32914	3.772 pg/mL Geometric Coefficient of Variation 33.8	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.

Data for mobocertinib and its metabolites (AP32960 and AP32914) is reported following the oral administration, and data for \[14C\]-mobocertinib and its metabolites (\[14C\]-AP32960 and \[14C\]-AP32914) is reported following intravenous administration.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration Mobocertinib	5.00 hours Interval 4.0 to 6.0	—
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration AP32960	4.502 hours Interval 4.0 to 6.0	—
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration AP32914	5.000 hours Interval 4.0 to 6.0	—
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-mobocertinib	0.26 hours Interval 0.26 to 1.25	—
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]- AP32960	3.257 hours Interval 2.25 to 8.26	—
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]- AP32914	2.26 hours Interval 2.26 to 2.26	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration Mobocertinib	1050 ng*hr/mL Geometric Coefficient of Variation 64.9	—
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration AP32960	478.2 ng*hr/mL Geometric Coefficient of Variation 30.6	—
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration AP32914	73.02 ng*hr/mL Geometric Coefficient of Variation 53.2	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed "n" are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 1.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-Mobocertinib	680 picogramhour/ milliliter (pghr/mL) Geometric Coefficient of Variation 30.4	—
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]- AP32960	187.8 picogramhour/ milliliter (pghr/mL) Geometric Coefficient of Variation 60.2	—
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]- AP32914	89.71 picogramhour/ milliliter (pghr/mL) Geometric Coefficient of Variation NA Geometric coefficient of variation could not be calculated because single participant was analyzed.	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration Mobocertinib	1032 ng*hr/mL Geometric Coefficient of Variation 65.6	—
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration AP32960	461.2 ng*hr/mL Geometric Coefficient of Variation 30.1	—
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration AP32914	66.92 ng*hr/mL Geometric Coefficient of Variation 53.6	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed "n" are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 1.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-Mobocertinib	617.9 pg*hr/mL Geometric Coefficient of Variation 34.0	—
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-AP32960	133.1 pg*hr/mL Geometric Coefficient of Variation 63.1	—
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-AP32914	31.52 pg*hr/mL Geometric Coefficient of Variation 113.7	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed "n" are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 1.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]- AP32914	31.52 picogramhour per milliliter (pghr/mL) Geometric Coefficient of Variation 113.7	—
Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]-Mobocertinib	617.9 picogramhour per milliliter (pghr/mL) Geometric Coefficient of Variation 34.0	—
Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration [14C]- AP32960	133.1 picogramhour per milliliter (pghr/mL) Geometric Coefficient of Variation 63.1	—

SECONDARY outcome

Timeframe: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose

Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed "n" are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 1.

Data for mobocertinib and its metabolites (AP32960 and AP32914) is reported following the oral administration, and data for \[14C\]-mobocertinib and its metabolites (\[14C\]-AP32960 and \[14C\]-AP32914) is reported following intravenous administration.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=6 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration Mobocertinib	22.9 hours Geometric Coefficient of Variation 17.9	—
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration AP32960	29.077 hours Geometric Coefficient of Variation 18.2	—
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration AP32914	12.545 hours Geometric Coefficient of Variation 37.5	—
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration [14C]-Mobocertinib	22.2 hours Geometric Coefficient of Variation 41.3	—
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration [14C]- AP32960	20.317 hours Geometric Coefficient of Variation 39.1	—
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration [14C]- AP32914	11.900 hours Geometric Coefficient of Variation NA Geometric coefficient of variation could not be calculated because single participant was analyzed.	—

SECONDARY outcome

Timeframe: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)

Population: The safety set included all participants who received at least one dose of study drug.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=7 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg n=6 Participants \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)	6 Participants	4 Participants

SECONDARY outcome

Timeframe: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)

Population: The safety set included all participants who received at least one dose of study drug.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=7 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg n=6 Participants \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings	0 Participants	0 Participants

SECONDARY outcome

Timeframe: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)

Population: The safety set included all participants who received at least one dose of study drug.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=7 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg n=6 Participants \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Number of Participants With Clinically Significant Change From Baseline in Vital Signs	0 Participants	0 Participants

SECONDARY outcome

Timeframe: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)

Population: The safety set included all participants who received at least one dose of study drug.

Outcome measures

Outcome measures
Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=7 Participants Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg n=6 Participants \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Number of Participants With Clinically Significant Change From Baseline in Laboratory Values	0 Participants	0 Participants

Adverse Events

Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg

Serious events: 0 serious events

Other events: 6 other events

Deaths: 0 deaths

[14C]-Mobocertinib 160 mg

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Additional Information

Medical Director

Takeda

Phone: +1-877-825-3327

Email: [email protected]

Results disclosure agreements

Principal investigator is a sponsor employee Research Organization shall not publish any articles or papers nor make any presentations, nor assist any other person in publishing any articles or papers or in making any presentations relating or referring to the Study or any results, data or insights from or any data, information or materials obtained or generated in the performance of its obligations without the prior written consent of Takeda, which consent may be granted or withheld in Takeda's sole discretion.
Publication restrictions are in place

Restriction type: OTHER

Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n=7 participants at risk Mobocertinib160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1.	[14C]-Mobocertinib 160 mg n=6 participants at risk \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.
Gastrointestinal disorders Constipation	14.3% 1/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Gastrointestinal disorders Diarrhoea	14.3% 1/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Gastrointestinal disorders Eructation	14.3% 1/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	0.00% 0/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Gastrointestinal disorders Faeces discoloured	0.00% 0/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Gastrointestinal disorders Haematochezia	0.00% 0/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Gastrointestinal disorders Nausea	28.6% 2/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	0.00% 0/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Gastrointestinal disorders Salivary hypersecretion	14.3% 1/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	0.00% 0/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Gastrointestinal disorders Vomiting	14.3% 1/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	0.00% 0/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
General disorders Chest discomfort	0.00% 0/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Injury, poisoning and procedural complications Contusion	14.3% 1/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	0.00% 0/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Metabolism and nutrition disorders Cow's milk intolerance	0.00% 0/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Musculoskeletal and connective tissue disorders Back pain	14.3% 1/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	0.00% 0/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Nervous system disorders Headache	0.00% 0/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Psychiatric disorders Insomnia	0.00% 0/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Respiratory, thoracic and mediastinal disorders Nasal congestion	0.00% 0/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	16.7% 1/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.
Respiratory, thoracic and mediastinal disorders Rhinorrhoea	14.3% 1/7 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.	0.00% 0/6 • Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41) At each visit the investigator had to document any occurrence of adverse events and abnormal laboratory findings. Any event spontaneously reported by the participant or observed by the investigator was recorded, irrespective of the relation to study treatment.