Trial Outcomes & Findings for A Study of Absorption, Metabolism, Excretion, and Absolute Bioavailability of Carbon-14-Labelled [14C] Selpercatinib (LY3527723) in Healthy Male Participants (NCT NCT05630287)

NCT ID: NCT05630287

Last Updated: 2025-04-23

Results Overview

PK: AUClast of Selpercatinib in plasma

• Recruitment status: COMPLETED
• Study phase: PHASE1
• Target enrollment: 12 participants
• Primary outcome timeframe: PK: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose
• Results posted on: 2025-04-23

Participant Flow

Participants in Part 1 did not participate in Part 2, nor did participants in Part 2 participate in Part 1. Parts 1 and 2 were independent of each other and did not need to be conducted in sequential order.

Participant milestones

Measure	Carbon-14-labelled [14C]-Selpercatinib - Part 1 Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).	Selpercatinib and [14C]-Selpercatinib - Part 2 Participants received a single oral dose of 160 mg Selpercatinib followed by a single dose of \<100 µg of \[14C\]-Selpercatinib (containing approximately 1 µCi) administered intravenously (IV).
Overall Study STARTED	6	6
Overall Study Received at Least 1 Dose of Study Drug	6	6
Overall Study COMPLETED	6	6
Overall Study NOT COMPLETED	0	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

A Study of Absorption, Metabolism, Excretion, and Absolute Bioavailability of Carbon-14-Labelled [14C] Selpercatinib (LY3527723) in Healthy Male Participants

Baseline characteristics by cohort

Measure	Carbon-14-labelled [14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).	Selpercatinib and [14C]-Selpercatinib - Part 2 n=6 Participants Participants received a single oral dose of 160 mg Selpercatinib followed by a single dose of \<100 µg of \[14C\]-Selpercatinib (containing approximately 1 µCi) administered intravenously (IV).	Total n=12 Participants Total of all reporting groups
Age, Continuous	35 years STANDARD_DEVIATION 12.5 • n=5 Participants	32 years STANDARD_DEVIATION 6.2 • n=7 Participants	34 years STANDARD_DEVIATION 9.6 • n=5 Participants
Sex: Female, Male Female	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants
Sex: Female, Male Male	6 Participants n=5 Participants	6 Participants n=7 Participants	12 Participants n=5 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	1 Participants n=5 Participants	1 Participants n=7 Participants	2 Participants n=5 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	5 Participants n=5 Participants	5 Participants n=7 Participants	10 Participants n=5 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants
Race (NIH/OMB) Asian	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants
Race (NIH/OMB) Black or African American	2 Participants n=5 Participants	2 Participants n=7 Participants	4 Participants n=5 Participants
Race (NIH/OMB) White	4 Participants n=5 Participants	4 Participants n=7 Participants	8 Participants n=5 Participants
Race (NIH/OMB) More than one race	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants
Region of Enrollment United States	6 participants n=5 Participants	6 participants n=7 Participants	12 participants n=5 Participants

PRIMARY outcome

Timeframe: PK: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUClast of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) of Selpercatinib in Plasma (Part 1)	24100 hour*nanogram per milliliter (h*ng/mL) Geometric Coefficient of Variation 20.2

PRIMARY outcome

Timeframe: PK: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUClast of [14C] Selpercatinib in plasma and whole blood

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: AUClast of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Plasma	21400 h*ng equivalents per gram (h*ng Eq/g) Geometric Coefficient of Variation 21.9
PK: AUClast of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Whole Blood	11400 h*ng equivalents per gram (h*ng Eq/g) Geometric Coefficient of Variation 38.2

PRIMARY outcome

Timeframe: PK: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUC0-inf of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Area Under the Concentration-time Curve, From Time 0 Extrapolated to Infinity (AUC0-inf) of Selpercatinib in Plasma (Part 1)	24200 hours*nanogram per milliliter (h*ng/mL) Geometric Coefficient of Variation 20.2

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUC0-inf of [14C] Selpercatinib in plasma and whole blood

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: AUC0-inf of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Plasma	26900 h*ng Eq/g Geometric Coefficient of Variation 25.8
PK: AUC0-inf of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Whole Blood	16700 h*ng Eq/g Geometric Coefficient of Variation 32.8

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUC0-24 of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Area Under the Concentration-time Curve, From Time 0 to Hour 24 (AUC0-24) of Selpercatinib in Plasma (Part 1)	17100 h*ng/mL Geometric Coefficient of Variation 17.7

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUC0-24 of [14C] Selpercatinib in plasma and whole blood

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: (AUC0-24) of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Plasma	21400 h*ng Eq/g Geometric Coefficient of Variation 21.9
PK: (AUC0-24) of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Whole Blood	12600 h*ng Eq/g Geometric Coefficient of Variation 23.4

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Cmax of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Maximum Observed Concentration (Cmax) of Selpercatinib in Plasma (Part 1)	1890 ng/mL Geometric Coefficient of Variation 22.7

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Cmax of [14C] Selpercatinib in plasma and whole blood

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Cmax of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Plasma	2240 nanogram equivalents per gram (ng Eq/g) Geometric Coefficient of Variation 24.6
PK: Cmax of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Whole Blood	1260 nanogram equivalents per gram (ng Eq/g) Geometric Coefficient of Variation 25.8

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Tmax of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Time to Reach Cmax (Tmax) of Selpercatinib in Plasma (Part 1)	1.25 hour (h) Interval 1.0 to 1.5

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Tmax of [14C] Selpercatinib in plasma and whole blood

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Tmax of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Plasma	1.50 h Interval 1.0 to 1.5
PK: Tmax of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Whole Blood	1.50 h Interval 1.0 to 2.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: t½ of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Apparent First-order Terminal Elimination Half-life (t½) of Selpercatinib in Plasma (Part 1)	36.5 h Standard Deviation 18.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: t½ of [14C] Selpercatinib in plasma and whole blood

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: t½ of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Plasma	12.2 h Standard Deviation 2.36
PK: t½ of [14C] Selpercatinib in Plasma and Whole Blood (Part 1) for Total Radioactivity Whole Blood	10.5 h Standard Deviation 2.79

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: CL/F of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Apparent Systemic Clearance (CL/F) of Selpercatinibin Plasma (Part 1)	6.83 Liter per hour (L/h) Geometric Coefficient of Variation 20.2

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Vz/F of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Apparent Volume of Distribution During the Terminal Phase (Vz/F) of Selpercatinib in Plasma (Part 1)	323 Liter (L) Geometric Coefficient of Variation 45.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUC0-24 of Selpercatinib in plasma/AUC0-24 of total radioactivity in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Plasma Selpercatinib/Total Radioactivity AUC0-24 Ratio (Part 1)	0.799 Ratio Geometric Coefficient of Variation 4.4

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUC0-24 of total radioactivity in whole blood/AUC0-24 of total radioactivity in whole blood

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Blood/Plasma Total Radioactivity AUC0-24 Ratio (Part 1)	0.590 Ratio Geometric Coefficient of Variation 9.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUClast of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: AUClast of Selpercatinib in Plasma (Part 2)	20200 hour*picogram per mL (h*pg/mL) Geometric Coefficient of Variation 26.6

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUClast of [14C] Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: AUClast of [14C] Selpercatinib in Plasma (Part 2)	1680 h*pg/mL Geometric Coefficient of Variation 30.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUC0-inf of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=5 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: AUC0-inf of Selpercatinib in Plasma (Part 2)	20300 h*pg/mL Geometric Coefficient of Variation 26.6

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: AUC0-inf of [14C] Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=5 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: AUC0-inf of [14C] Selpercatinib in Plasma (Part 2)	1720 h*pg/mL Geometric Coefficient of Variation 33.5

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Cmax of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Cmax of Selpercatinib in Plasma (Part 2)	1550 ng/mL Geometric Coefficient of Variation 28.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Cmax of [14C] Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Cmax of [14C] Selpercatinib in Plasma (Part 2)	201 ng/mL Geometric Coefficient of Variation 30.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Tmax of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Tmax of Selpercatinib in Plasma (Part 2)	1.92 h Interval 1.0 to 1.92

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Tmax of [14C] Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Tmax of [14C] Selpercatinib in Plasma (Part 2)	0.167 h Interval 0.167 to 2.1

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: t½ of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: t½ of Selpercatinib in Plasma (Part 2)	31.5 h Standard Deviation 20.7

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: t½ of [14C] Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=5 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: t½ of [14C] Selpercatinib in Plasma (Part 2)	16.9 h Standard Deviation 7.97

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: CL/F of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: CL/F of Selpercatinib in Plasma (Part 2)	7.89 L/h Geometric Coefficient of Variation 26.6

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: CL of [14C] Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=5 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Systemic Clearance (CL) of [14C] Selpercatinib in Plasma (Part 2)	5.70 L/h Geometric Coefficient of Variation 33.4

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Vz/F of Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=6 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Vz/F of Selpercatinib in Plasma (Part 2)	307 L Geometric Coefficient of Variation 66.3

PRIMARY outcome

Timeframe: Pre-dose up to 168 hour post-dose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Vz of [14C] Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=5 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Volume of Distribution During the Terminal Phase (Vz) of [14C] Selpercatinib in Plasma (Part 2)	127 L Geometric Coefficient of Variation 56.8

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

PK: Vss of [14C] Selpercatinib in plasma

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=5 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Volume of Distribution at Steady State (Vss) of [14C] Selpercatinib in Plasma (Part 2)	85.0 L Geometric Coefficient of Variation 21.0

PRIMARY outcome

Timeframe: Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, and 168 hours postdose

Population: All participants who received at least 1 dose of study drug and had evaluable PK data.

Absolute bioavailability was determined by comparing the plasma exposure of LOXO-292 following oral dosing with the plasma exposure of [14C]-LOXO-292 following IV dosing.

Outcome measures

Measure	[14C]-Selpercatinib - Part 1 n=5 Participants Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).
PK: Absolute Bioavailability (F) of Selpercatinib in Plasma (Part 2)	0.732 Ratio Geometric Coefficient of Variation 13.9

Adverse Events

Carbon-14-labelled [14C]-Selpercatinib

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

Selpercatinib and [14C]-Selpercatinib

Serious events: 0 serious events

Other events: 1 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Measure	Carbon-14-labelled [14C]-Selpercatinib n=6 participants at risk Participants received a single oral dose of 165 milligram (mg) of \[14C\]-Selpercatinib (containing approximately 40 µCi).	Selpercatinib and [14C]-Selpercatinib n=6 participants at risk Participants received a single oral dose of 160 mg Selpercatinib followed by single dose of \<100 µg of \[14C\]-Selpercatinib (containing approximately 1 µCi) administered intravenously (IV).
Gastrointestinal disorders Abdominal pain	16.7% 1/6 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.	0.00% 0/6 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.
Gastrointestinal disorders Diarrhoea	50.0% 3/6 • Number of events 3 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.	0.00% 0/6 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.
Gastrointestinal disorders Dry mouth	0.00% 0/6 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.	16.7% 1/6 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.
Gastrointestinal disorders Nausea	33.3% 2/6 • Number of events 2 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.	0.00% 0/6 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.
Gastrointestinal disorders Vomiting	16.7% 1/6 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.	0.00% 0/6 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.
Nervous system disorders Headache	16.7% 1/6 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.	0.00% 0/6 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.
Vascular disorders Hot flush	16.7% 1/6 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.	0.00% 0/6 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16 Parts 1 and 2 will consist of all subjects who received at least 1 dose of study drug and have at least 1 post-dose safety assessment.

Additional Information

Chief Medical Officer

Eli Lilly and Company

Phone: 8005955979

Email: ClinicalTrials.gov@lilly.com

Results disclosure agreements

• Principal investigator is a sponsor employee
• Publication restrictions are in place

Restriction type: GT60