Trial Outcomes & Findings for A Study of Carbon-14-Labelled [14C] LOXO-305 (Pirtobrutinib) in Healthy Male Participants (NCT NCT06180954)
NCT ID: NCT06180954
Last Updated: 2025-01-13
Results Overview
AUC0-inf of LOXO-305 in plasma.
COMPLETED
PHASE1
9 participants
Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dose
2025-01-13
Participant Flow
Participant milestones
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
Participants received a single dose of 200 milligram (mg) LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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Part 2: LOXO-305 Oral Tablet + [14C]-LOXO-305 IV Solution
Participants received:
* a single dose of 200 mg LOXO-305 administered as 2×100 mg oral tablets
* followed 2 hours later by a single dose of less than 100 microgram (μg) of \[14C\]-LOXO-305 (approximately 1 microcurie radioactivity) administered as an intravenous (IV) push over approximately 2 minutes.
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|---|---|---|
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Overall Study
STARTED
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4
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5
|
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Overall Study
Received at Least One Dose of Study Drug.
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4
|
5
|
|
Overall Study
COMPLETED
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4
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5
|
|
Overall Study
NOT COMPLETED
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0
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0
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Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Study of Carbon-14-Labelled [14C] LOXO-305 (Pirtobrutinib) in Healthy Male Participants
Baseline characteristics by cohort
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
Part 2: LOXO-305 Oral Tablet + [14C]-LOXO-305 IV Solution
n=5 Participants
Participants received:
* a single dose of 200 mg LOXO-305 administered as 2×100 mg oral tablets
* followed 2 hours later by a single dose of less than 100 μg of \[14C\]-LOXO-305 (approximately 1 microcurie radioactivity) administered as an IV push over approximately 2 minutes.
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Total
n=9 Participants
Total of all reporting groups
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|---|---|---|---|
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Age, Continuous
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39.5 years
STANDARD_DEVIATION 3.42 • n=5 Participants
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24 years
STANDARD_DEVIATION 5.15 • n=7 Participants
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30.9 years
STANDARD_DEVIATION 9.18 • n=5 Participants
|
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Sex: Female, Male
Female
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0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
4 Participants
n=5 Participants
|
5 Participants
n=7 Participants
|
9 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
0 Participants
n=5 Participants
|
1 Participants
n=7 Participants
|
1 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
4 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
8 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
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0 Participants
n=5 Participants
|
1 Participants
n=7 Participants
|
1 Participants
n=5 Participants
|
|
Race (NIH/OMB)
White
|
3 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
7 Participants
n=5 Participants
|
|
Race (NIH/OMB)
More than one race
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1 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
1 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
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4 Participants
n=5 Participants
|
5 Participants
n=7 Participants
|
9 Participants
n=5 Participants
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-inf of LOXO-305 in plasma.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: Pharmacokinetics (PK): Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
|
75300 hours*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 14.8
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-inf of total radioactivity in plasma and whole blood.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Plasma
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111000 hours*nanogram equivalent per gram
Geometric Coefficient of Variation 15.8
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Part 1: PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Whole Blood
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71200 hours*nanogram equivalent per gram
Geometric Coefficient of Variation 12.6
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-t of LOXO-305 in plasma.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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Part 1: PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
|
74500 hours*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 14.9
|
PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-t of total radioactivity in plasma and whole blood.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Plasma
|
109000 hours*nanogram equivalent per gram
Geometric Coefficient of Variation 16.1
|
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Part 1: PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Whole Blood
|
68900 hours*nanogram equivalent per gram
Geometric Coefficient of Variation 13
|
PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Cmax of LOXO-305 in plasma.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Maximum Observed Plasma Concentration (Cmax) of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
|
3530 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 8.8
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Cmax of total radioactivity in plasma and whole blood.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Maximum Observed Plasma Concentration (Cmax) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Plasma
|
4280 nanogram equivalent per gram
Geometric Coefficient of Variation 7.7
|
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Part 1: PK: Maximum Observed Plasma Concentration (Cmax) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Whole Blood
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3020 nanogram equivalent per gram
Geometric Coefficient of Variation 7.7
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Tmax of LOXO-305 in plasma.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Time to Maximum Observed Concentration (Tmax) of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
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1.80 hours
Interval 1.5 to 3.0
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Tmax of total radioactivity in plasma and whole blood.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Time to Maximum Observed Concentration (Tmax) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Plasma
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1.80 hours
Interval 1.5 to 4.0
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Part 1: PK: Time to Maximum Observed Concentration (Tmax) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Whole Blood
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1.80 hours
Interval 1.5 to 3.0
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
t1/2 of LOXO-305 in plasma.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Apparent Terminal Elimination Half-life (t1/2) of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
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17.8 hours
Standard Deviation 2.26
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
t1/2 of total radioactivity in plasma and whole blood.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Apparent Terminal Elimination Half-life (t1/2) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Plasma
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25.3 hours
Standard Deviation 4.76
|
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Part 1: PK: Apparent Terminal Elimination Half-life (t1/2) of Total Radioactivity in Plasma and Whole Blood Following a Single Oral Dose of [14C]-LOXO-305
Whole Blood
|
21.7 hours
Standard Deviation 3.08
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PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
CL/F of LOXO-305 in plasma.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Apparent Systemic Clearance (CL/F) of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
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2.69 liter per hour (L/h)
Geometric Coefficient of Variation 15.8
|
PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Vz/F of LOXO-305 in plasma.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Apparent Volume of Distribution (Vz/F) of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
|
68.8 liter (L)
Geometric Coefficient of Variation 21
|
PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-inf of plasma LOXO-305 relative to AUC0-inf of plasma total radioactivity, expressed in ratio.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Ratio of AUC0-inf of Plasma LOXO-305 to AUC0-inf of Plasma Total Radioactivity
|
0.680 ratio
Geometric Coefficient of Variation 1.2
|
PRIMARY outcome
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-inf of whole blood total radioactivity relative to AUC0-inf of plasma total radioactivity, expressed in ratio.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
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Part 1: PK: Ratio of AUC0-inf of Whole Blood Total Radioactivity to AUC0-inf of Plasma Total Radioactivity
|
0.642 ratio
Geometric Coefficient of Variation 3.4
|
PRIMARY outcome
Timeframe: Pre-dose, 0 (time of dose), 6, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The urine sampling time points from pre-dose through 360 hours post-dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Cumulative Amount of Total Radioactivity Excreted in Urine
|
116 milligram equivalent (mg eq)
Standard Deviation 4.05
|
PRIMARY outcome
Timeframe: 0 (time of dose), 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The feces sampling time points from the 0 hour (i.e. time of dose) through 360 hours post-dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
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|---|---|
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Part 1: PK: Cumulative Amount of Total Radioactivity Excreted in Feces
|
75.5 milligram equivalent (mg eq)
Standard Deviation 5.29
|
PRIMARY outcome
Timeframe: 0 (time of dose), 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The feces sampling time points from the 0 hour (i.e. time of dose) through 360 hours post-dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
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Part 1: PK: Mean Cumulative Percentage of Total Radioactivity Excreted in Feces
|
37.3 percentage of total radioactivity
Standard Deviation 2.31
|
PRIMARY outcome
Timeframe: Pre-dose, 0 (time of dose), 6, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The urine sampling time points from pre-dose through 360 hours post-dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 1: PK: Mean Cumulative Percentage of Total Radioactivity Excreted in Urine
|
57 percentage of total radioactivity
Standard Deviation 2.16
|
PRIMARY outcome
Timeframe: 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264 h post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The metabolic profile of LOXO-305 following a single oral dose of \[14C\]-LOXO-305 was done to assess the presence of LOXO-305 and various metabolites (M1 to M4, M11, M12, M15 to M22) in plasma using high-performance liquid chromatography with radiochemical detection. Metabolites are identified by comparison with known standards (when available) and/or by liquid chromatography/tandem mass spectrometry analysis. The presence of any metabolite in a given matrix is indicated as '1' and absence from that matrix is indicated as '0'.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
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Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M3
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M4
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M11
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M15
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M16
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M17
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M18
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M19
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M22
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
Loxo-305
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M1
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M2
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M12
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M20
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Plasma Following a Single Oral Dose of [14C]-LOXO-305
M21
|
0 sample positive
|
PRIMARY outcome
Timeframe: Pre-dose, 0 (time of dose), 6, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The metabolic profile of LOXO-305 following a single oral dose of \[14C\]-LOXO-305 was done to assess the presence of LOXO-305 and various metabolites (M1 to M4, M11, M12, M15 to M22) in urine using high-performance liquid chromatography with radiochemical detection. Metabolites are identified by comparison with known standards (when available) and/or by liquid chromatography/tandem mass spectrometry analysis. The presence of any metabolite in a given matrix is indicated as '1' and absence from that matrix is indicated as '0'.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M2
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M15
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M22
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
Loxo-305
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M1
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M3
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M4
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M11
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M12
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M16
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M17
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M18
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M19
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M20
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Urine Following a Single Oral Dose of [14C]-LOXO-305
M21
|
0 sample positive
|
PRIMARY outcome
Timeframe: 0 (time of dose), 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360 hours post-dosePopulation: All part 1 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The metabolic profile of LOXO-305 following a single oral dose of \[14C\]-LOXO-305 was done to assess the presence of LOXO-305 and various metabolites (M1 to M4, M11, M12, M15 to M22) in feces using high-performance liquid chromatography with radiochemical detection. Metabolites are identified by comparison with known standards (when available) and/or by liquid chromatography/tandem mass spectrometry analysis. The presence of any metabolite in a given matrix is indicated as '1' and absence from that matrix is indicated as '0'.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M1
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M4
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
Loxo-305
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M2
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M3
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M11
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M12
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M15
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M16
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M17
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M18
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M19
|
0 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M20
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M21
|
1 sample positive
|
|
Part 1: PK: Metabolic Profile of LOXO-305 in Feces Following a Single Oral Dose of [14C]-LOXO-305
M22
|
1 sample positive
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0.5, 1, 2 hours post oral dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-inf of LOXO-305 in plasma. The sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of LOXO-305 in Plasma
|
105000 hours*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 28.1
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-inf of \[14C\]-LOXO-305 in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of [14C]-LOXO-305 in Plasma
|
13700 hours*picogram per milliliter
Geometric Coefficient of Variation 29
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-inf of total radioactivity in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Total Radioactivity in Plasma
|
18300 hours*picogram equivalent per milliliter
Geometric Coefficient of Variation 25.2
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0.5, 1, 2 hours post oral dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-t of LOXO-305 in plasma. The sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) of LOXO-305 in Plasma
|
104000 hours*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 28.7
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-t of \[14C\]-LOXO-305 in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) of [14C]-LOXO-305 in Plasma
|
13700 hours*picogram per milliliter
Geometric Coefficient of Variation 29.2
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
AUC0-t of Total Radioactivity in Plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Area Under the Concentration-time Curve From Hour 0 to the Last Measurable Concentration (AUC0-t) of Total Radioactivity in Plasma
|
18000 hours*picogram equivalent per milliliter
Geometric Coefficient of Variation 25.8
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0.5, 1, 2 hours post oral dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Cmax of LOXO-305 in plasma. The sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Maximum Observed Plasma Concentration (Cmax) of LOXO-305 in Plasma
|
4490 nanograms per milliliter (ng/mL)
Geometric Coefficient of Variation 19.2
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Cmax of \[14C\]-LOXO-305 in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Maximum Observed Plasma Concentration (Cmax) of [14C]-LOXO-305 in Plasma
|
994 picogram per milliliter (pg/mL)
Geometric Coefficient of Variation 31.6
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Cmax of Total Radioactivity in Plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Maximum Observed Plasma Concentration (Cmax) of Total Radioactivity in Plasma
|
1110 picogram equivalent per milliliter
Geometric Coefficient of Variation 53.1
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0.5, 1, 2 hours post oral dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Tmax of LOXO-305 in plasma. The sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Time to Maximum Observed Concentration (Tmax) of LOXO-305 in Plasma
|
5.00 hours
Interval 2.03 to 5.0
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Tmax of \[14C\]-LOXO-305 in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Time to Maximum Observed Concentration (Tmax) of [14C]-LOXO-305 in Plasma
|
0.167 hours
Interval 0.0333 to 12.0
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Tmax of Total Radioactivity in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Time to Maximum Observed Concentration (Tmax) of Total Radioactivity in Plasma
|
0.167 hours
Interval 0.0333 to 0.167
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0.5, 1, 2 hours post oral dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
t1/2 of LOXO-305 in plasma. The sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Apparent Terminal Elimination Half-life (t1/2) of LOXO-305 in Plasma
|
18.7 hours
Standard Deviation 1.68
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
t1/2 of \[14C\]-LOXO-305 in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Apparent Terminal Elimination Half-life (t1/2) of [14C]-LOXO-305 in Plasma
|
17.6 hours
Standard Deviation 1.24
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
t1/2 of Total Radioactivity in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Apparent Terminal Elimination Half-life (t1/2) of Total Radioactivity in Plasma
|
37.4 hours
Standard Deviation 9.72
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0.5, 1, 2 hours post oral dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
CL/F of LOXO-305 in plasma. The sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Apparent Systemic Clearance (CL/F) of LOXO-305 in Plasma
|
1.90 liter per hour (L/h)
Geometric Coefficient of Variation 28.1
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0.5, 1, 2 hours post oral dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Vz/F of LOXO-305 in plasma. The sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Apparent Volume of Distribution During the Terminal Phase (Vz/F) of LOXO-305 in Plasma
|
51.0 liter (L)
Geometric Coefficient of Variation 23.6
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0.5, 1, 2 hours post oral dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The absolute bioavailability expressed in ratio was calculated using the formula= AUC0-inf (oral) x Dose (IV) divided by AUC0-inf (IV) x Dose (oral) . The sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Absolute Bioavailability of LOXO-305 in Plasma
|
0.855 ratio
Geometric Coefficient of Variation 7.2
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
CL of \[14C\]-LOXO-305 in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Total Clearance (CL) of [14C]-LOXO-305 in Plasma
|
1.63 liter per hour (L/h)
Geometric Coefficient of Variation 29.7
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dose.Population: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Vz of \[14C\]-LOXO-305 in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Volume of Distribution (Vz) of [14C]-LOXO-305 in Plasma
|
41.2 liter (L)
Geometric Coefficient of Variation 29
|
PRIMARY outcome
Timeframe: Pre-IV dose, 0.03, 0.17, 0.33, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
Vss of \[14C\]-LOXO-305 in plasma. The sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Volume of Distribution at Steady State (Vss) of [14C]-LOXO-305 in Plasma
|
36.3 liter (L)
Geometric Coefficient of Variation 24.2
|
PRIMARY outcome
Timeframe: Pre-IV dose, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
CLR of \[14C\]-LOXO-305 in urine collection. The urine sampling time points from pre-IV dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Renal Clearance (CLR) of [14C]-LOXO-305
|
0.116 liter per hour (L/h)
Geometric Coefficient of Variation 36.8
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0 (time of oral dose), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The urine sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Cumulative Amount of [14C]-LOXO-305 Excreted in Urine
|
1.59 microgram (μg)
Geometric Coefficient of Variation 28.3
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0 (time of oral dose), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The urine sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Cumulative Amount of Total Radioactivity Excreted in Urine
|
14.1 microgram equivalent (μg eq)
Geometric Coefficient of Variation 11.4
|
PRIMARY outcome
Timeframe: 0 (time of oral dose), 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The Feces sampling time points from the 0 hour (i.e. time of oral dose) through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Cumulative Amount of [14C]-LOXO-305 Excreted in Feces
|
3.02 microgram (μg)
Geometric Coefficient of Variation 40.5
|
PRIMARY outcome
Timeframe: 0 (time of oral dose), 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The Feces sampling time points from the 0 hour (i.e. time of oral dose) through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Cumulative Amount of Total Radioactivity Excreted in Feces
|
4.97 microgram equivalent (μg eq)
Geometric Coefficient of Variation 38.4
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0 (time of oral dose), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The urine sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Mean Cumulative Percentage of [14C]-LOXO-305 Excreted in Urine
|
7.12 percentage of [14C]-LOXO-305
Geometric Coefficient of Variation 28.9
|
PRIMARY outcome
Timeframe: Pre-oral dose, 0 (time of oral dose), 4, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The urine sampling time points from pre-oral dose through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Mean Cumulative Percentage of Total Radioactivity Excreted in Urine
|
63.1 percentage of total radioactivity
Geometric Coefficient of Variation 11.2
|
PRIMARY outcome
Timeframe: 0 (time of oral dose), 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The Feces sampling time points from the 0 hour (i.e. time of oral dose) through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Mean Cumulative Percentage of [14C]-LOXO-305 Excreted in Feces
|
13.5 percentage of [14C]-LOXO-305
Geometric Coefficient of Variation 40.5
|
PRIMARY outcome
Timeframe: 0 (time of oral dose), 12, 24, 48, 72, 96, 120, 144, 168, 192 hours post IV dosePopulation: All part 2 participants who received \[14C\]-LOXO-305 and had at least 1 quantifiable PK concentration, and for whom at least 1 PK parameter was computed. Participants were excluded from the analysis if they had an AE of vomiting that occurred at or before 2 times the median time to maximum observed plasma concentration (Tmax).
The Feces sampling time points from the 0 hour (i.e. time of oral dose) through 192 hours post-IV dose were used to assess this outcome.
Outcome measures
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=5 Participants
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
|---|---|
|
Part 2: PK: Mean Cumulative Percentage of Total Radioactivity Excreted in Feces
|
22.3 percentage of total radioactivity
Geometric Coefficient of Variation 38.8
|
Adverse Events
Part 1: [14C]-LOXO-305 Oral Solution
Part 2: LOXO-305 Oral Tablet + [14C]-LOXO-305 IV Solution
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Part 1: [14C]-LOXO-305 Oral Solution
n=4 participants at risk
Participants received a single dose of 200 mg LOXO-305 radiolabelled with carbon-14, i.e., \[14C\]-LOXO-305 (approximately 200 microcurie radioactivity) administered as an oral solution.
|
Part 2: LOXO-305 Oral Tablet + [14C]-LOXO-305 IV Solution
n=5 participants at risk
Participants received:
a single dose of 200 mg LOXO-305 administered as 2×100 mg oral tablets followed 2 hours later by a single dose of less than 100 μg of \[14C\]-LOXO-305 (approximately 1 microcurie radioactivity) administered as an IV push over approximately 2 minutes.
|
|---|---|---|
|
Gastrointestinal disorders
Diarrhoea
|
25.0%
1/4 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
20.0%
1/5 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
|
Injury, poisoning and procedural complications
Post procedural contusion
|
0.00%
0/4 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
60.0%
3/5 • Number of events 3 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
|
Injury, poisoning and procedural complications
Procedural pain
|
0.00%
0/4 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
40.0%
2/5 • Number of events 2 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
|
Injury, poisoning and procedural complications
Skin abrasion
|
25.0%
1/4 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
0.00%
0/5 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
|
Injury, poisoning and procedural complications
Skin laceration
|
0.00%
0/4 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
20.0%
1/5 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
|
Investigations
Heart rate increased
|
0.00%
0/4 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
20.0%
1/5 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
|
Nervous system disorders
Headache
|
25.0%
1/4 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
0.00%
0/5 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
|
Respiratory, thoracic and mediastinal disorders
Epistaxis
|
25.0%
1/4 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
0.00%
0/5 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
|
Skin and subcutaneous tissue disorders
Papule
|
25.0%
1/4 • Number of events 1 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
0.00%
0/5 • Part 1: Baseline up to Day 29; Part 2: Baseline up to Day 16
All participants who received at least one dose of study drug. As per the planned safety analyses, AE data was reported per treatment regimen.
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60