Trial Outcomes & Findings for A Study to Evaluate Pirtobrutinib (LOXO-305) in Healthy Adult Participants (NCT NCT06181006)
NCT ID: NCT06181006
Last Updated: 2025-01-14
Results Overview
TEAE is defined as an adverse event (AE) which starts on or after the first administration of study drug. A serious adverse event is defined as any AE occurring at any dose that results in any of the following outcomes: death; a life-threatening adverse drug experience; inpatient hospitalization or prolongation of existing hospitalization; a persistent or significant disability/incapacity; a congenital anomaly/birth defect; an important medical event that may require medical or surgical intervention to prevent any of the above outcomes.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
24 participants
Primary outcome timeframe
Baseline up to 46 days
Results posted on
2025-01-14
Participant Flow
Participant milestones
| Measure |
Cohort 1: 300 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 300 milligram (mg) administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
Overall Study
STARTED
|
6
|
6
|
6
|
6
|
|
Overall Study
Received at Least 1 Dose of Study Drug
|
6
|
6
|
6
|
6
|
|
Overall Study
COMPLETED
|
6
|
6
|
6
|
6
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Study to Evaluate Pirtobrutinib (LOXO-305) in Healthy Adult Participants
Baseline characteristics by cohort
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
Total
n=24 Participants
Total of all reporting groups
|
|---|---|---|---|---|---|
|
Age, Continuous
|
41.8 years
STANDARD_DEVIATION 11.79 • n=5 Participants
|
36.2 years
STANDARD_DEVIATION 9.15 • n=7 Participants
|
33.2 years
STANDARD_DEVIATION 10.85 • n=5 Participants
|
35.3 years
STANDARD_DEVIATION 5.47 • n=4 Participants
|
36.6 years
STANDARD_DEVIATION 9.55 • n=21 Participants
|
|
Sex: Female, Male
Female
|
4 Participants
n=5 Participants
|
2 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
2 Participants
n=4 Participants
|
8 Participants
n=21 Participants
|
|
Sex: Female, Male
Male
|
2 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
6 Participants
n=5 Participants
|
4 Participants
n=4 Participants
|
16 Participants
n=21 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
4 Participants
n=5 Participants
|
6 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
3 Participants
n=4 Participants
|
15 Participants
n=21 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
2 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
4 Participants
n=5 Participants
|
3 Participants
n=4 Participants
|
9 Participants
n=21 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 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
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Race (NIH/OMB)
Black or African American
|
2 Participants
n=5 Participants
|
1 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
2 Participants
n=4 Participants
|
7 Participants
n=21 Participants
|
|
Race (NIH/OMB)
White
|
4 Participants
n=5 Participants
|
5 Participants
n=7 Participants
|
3 Participants
n=5 Participants
|
3 Participants
n=4 Participants
|
15 Participants
n=21 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
1 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
1 Participants
n=21 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
1 Participants
n=4 Participants
|
1 Participants
n=21 Participants
|
|
Region of Enrollment
United States
|
6 participants
n=5 Participants
|
6 participants
n=7 Participants
|
6 participants
n=5 Participants
|
6 participants
n=4 Participants
|
24 participants
n=21 Participants
|
PRIMARY outcome
Timeframe: Baseline up to 46 daysPopulation: All enrolled participants who received at least one dose of study drug.
TEAE is defined as an adverse event (AE) which starts on or after the first administration of study drug. A serious adverse event is defined as any AE occurring at any dose that results in any of the following outcomes: death; a life-threatening adverse drug experience; inpatient hospitalization or prolongation of existing hospitalization; a persistent or significant disability/incapacity; a congenital anomaly/birth defect; an important medical event that may require medical or surgical intervention to prevent any of the above outcomes.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
Number of Participants With One or More Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Event(s) (SAEs)
SAEs
|
0 Participants
|
0 Participants
|
0 Participants
|
0 Participants
|
|
Number of Participants With One or More Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Event(s) (SAEs)
TEAEs
|
1 Participants
|
0 Participants
|
0 Participants
|
3 Participants
|
SECONDARY outcome
Timeframe: Day 1 (predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: AUC0-24 of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to 24 Hours Post-dose (AUC0-24) of Pirtobrutinib
|
84100 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 27.2
|
135000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 81.8
|
200000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 22.6
|
225000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 22.3
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: AUC0-t of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Area Under the Concentration Versus Time Curve From Hour Zero to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib
|
143000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 29.8
|
259000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 101
|
379000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 16.9
|
490000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 26.8
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: AUC0-inf of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of Pirtobrutinib
|
144000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 30.1
|
260000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 100
|
382000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 16.9
|
492000 hour*nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 26.9
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: %AUCextrap of pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Pirtobrutinib
|
0.869 percentage of AUCextrap
Geometric Coefficient of Variation 39.9
|
0.504 percentage of AUCextrap
Geometric Coefficient of Variation 61.2
|
0.474 percentage of AUCextrap
Geometric Coefficient of Variation 113
|
0.458 percentage of AUCextrap
Geometric Coefficient of Variation 48.1
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: Cmax of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Maximum Observed Plasma Concentration (Cmax) of Pirtobrutinib
|
6600 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 28.7
|
9050 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 65.9
|
13700 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 32.8
|
13000 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 27.1
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: Tmax of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib
|
3.25 hours
Interval 1.5 to 7.0
|
2.75 hours
Interval 2.0 to 4.0
|
3.00 hours
Interval 2.5 to 7.0
|
4.01 hours
Interval 2.5 to 9.0
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: λZ of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 1)
Subject 1
|
0.0367 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 1)
Subject 2
|
0.0423 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 1)
Subject 3
|
0.0242 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 1)
Subject 4
|
0.0477 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 1)
Subject 5
|
0.0285 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 1)
Subject 6
|
0.0469 1/hour (1/h)
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: λZ of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 2)
Subject 1
|
0.0322 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 2)
Subject 2
|
0.0317 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 2)
Subject 3
|
0.0381 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 2)
Subject 4
|
0.0327 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 2)
Subject 5
|
0.0353 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 2)
Subject 6
|
0.0368 1/hour (1/h)
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: λZ of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 3)
Subject 1
|
0.0279 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 3)
Subject 2
|
0.0263 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 3)
Subject 3
|
0.0339 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 3)
Subject 4
|
0.0339 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 3)
Subject 5
|
0.0295 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 3)
Subject 6
|
0.0410 1/hour (1/h)
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: λZ of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 4)
Subject 1
|
0.0291 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 4)
Subject 2
|
0.0367 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 4)
Subject 3
|
0.0330 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 4)
Subject 4
|
0.0313 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 4)
Subject 5
|
0.0320 1/hour (1/h)
|
—
|
—
|
—
|
|
PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib (Cohort 4)
Subject 6
|
0.0396 1/hour (1/h)
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: CL/F of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib
|
2.08 liter per hour (L/h)
Geometric Coefficient of Variation 30.1
|
2.31 liter per hour (L/h)
Geometric Coefficient of Variation 100
|
2.10 liter per hour (L/h)
Geometric Coefficient of Variation 16.9
|
1.83 liter per hour (L/h)
Geometric Coefficient of Variation 26.9
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: Vz/F of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Apparent Volume of Distribution at Terminal Phase (Vz/F) of Pirtobrutinib
|
57.0 Liter (L)
Geometric Coefficient of Variation 23.5
|
67.1 Liter (L)
Geometric Coefficient of Variation 96.2
|
66.1 Liter (L)
Geometric Coefficient of Variation 26.4
|
54.7 Liter (L)
Geometric Coefficient of Variation 23.2
|
SECONDARY outcome
Timeframe: Day 1 (Predose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 7, 9, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose)Population: All participants who received a dose of Pirtobrutinib, had at least 1 quantifiable PK concentration of Pirtobrutinib and had at least 1 PK parameter computed.
PK: t1/2 of Pirtobrutinib.
Outcome measures
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 Participants
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
PK: Apparent Plasma Terminal Elimination Half-life (t1/2) of Pirtobrutinib
|
19.0 hours
Geometric Coefficient of Variation 28.4
|
20.2 hours
Geometric Coefficient of Variation 7.71
|
21.9 hours
Geometric Coefficient of Variation 16.3
|
20.7 hours
Geometric Coefficient of Variation 11.2
|
Adverse Events
Cohort 1: 300 mg Pirtobrutinib
Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths
Cohort 2: 600 mg Pirtobrutinib
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
Cohort 3: 800 mg Pirtobrutinib
Serious events: 0 serious events
Other events: 0 other events
Deaths: 0 deaths
Cohort 4: 900 mg Pirtobrutinib
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Cohort 1: 300 mg Pirtobrutinib
n=6 participants at risk
Participants received a single dose of Pirtobrutinib 300 mg administered orally on Day 1.
|
Cohort 2: 600 mg Pirtobrutinib
n=6 participants at risk
Participants received a single dose of Pirtobrutinib 600 mg administered orally on Day 1.
|
Cohort 3: 800 mg Pirtobrutinib
n=6 participants at risk
Participants received a single dose of Pirtobrutinib 800 mg administered orally on Day 1.
|
Cohort 4: 900 mg Pirtobrutinib
n=6 participants at risk
Participants received a single dose of Pirtobrutinib 900 mg administered orally on Day 1.
|
|---|---|---|---|---|
|
Nervous system disorders
Headache
|
16.7%
1/6 • Number of events 1 • Upto 46 days
All enrolled participants who received at least one dose of study drug.
|
0.00%
0/6 • Upto 46 days
All enrolled participants who received at least one dose of study drug.
|
0.00%
0/6 • Upto 46 days
All enrolled participants who received at least one dose of study drug.
|
33.3%
2/6 • Number of events 2 • Upto 46 days
All enrolled participants who received at least one dose of study drug.
|
|
Skin and subcutaneous tissue disorders
Petechiae
|
0.00%
0/6 • Upto 46 days
All enrolled participants who received at least one dose of study drug.
|
0.00%
0/6 • Upto 46 days
All enrolled participants who received at least one dose of study drug.
|
0.00%
0/6 • Upto 46 days
All enrolled participants who received at least one dose of study drug.
|
16.7%
1/6 • Number of events 1 • Upto 46 days
All enrolled participants who received at least one dose of study drug.
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60