Trial Outcomes & Findings for A Study of the Effect of Food on Pirtobrutinib (LOXO-305) in Healthy Participants (NCT NCT06180980)
NCT ID: NCT06180980
Last Updated: 2025-03-07
Results Overview
PK: AUC0-24 of pirtobrutinib was reported.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
20 participants
Primary outcome timeframe
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours post-dose on Days 1 and 8
Results posted on
2025-03-07
Participant Flow
Participant milestones
| Measure |
200 mg Pirtobrutinib: Treatment AB
Participants received a single oral dose of 200 milligrams (mg) of pirtobrutinib administered in the morning on Day 1, under fasted conditions (Treatment A) followed by 200 mg pirtobrutinib administered orally in the morning on Day 8, under fed condition (Treatment B).
A washout period of 7 days was maintained between Treatments A and B.
|
200 mg Pirtobrutinib: Treatment BA
Participants received a single oral dose of 200 mg pirtobrutinib administered in the morning on Day 1, under fed conditions (Treatment B) followed by 200 mg of pirtobrutinib administered orally in the morning on Day 8, under fasted conditions (Treatment A).
A washout period of 7 days was maintained between Treatments A and B.
|
|---|---|---|
|
Overall Study
STARTED
|
10
|
10
|
|
Overall Study
Received at Least 1 Dose of Study Drug
|
10
|
10
|
|
Overall Study
COMPLETED
|
10
|
10
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Study of the Effect of Food on Pirtobrutinib (LOXO-305) in Healthy Participants
Baseline characteristics by cohort
| Measure |
200 mg Pirtobrutinib: Treatment AB
n=10 Participants
Participants received a single oral dose of 200 mg of pirtobrutinib administered in the morning on Day 1, under fasted conditions (Treatment A) followed by 200 mg pirtobrutinib administered orally in the morning on Day 8, under fed condition (Treatment B).
A washout period of 7 days was maintained between Treatments A and B.
|
200 mg Pirtobrutinib: Treatment BA
n=10 Participants
Participants received a single oral dose of 200 mg pirtobrutinib administered in the morning on Day 1, under fed conditions (Treatment B) followed by 200 mg of pirtobrutinib administered orally in the morning on Day 8, under fasted conditions (Treatment A).
A washout period of 7 days was maintained between Treatments A and B.
|
Total
n=20 Participants
Total of all reporting groups
|
|---|---|---|---|
|
Age, Continuous
|
35.9 years
STANDARD_DEVIATION 10.10 • n=99 Participants
|
35.9 years
STANDARD_DEVIATION 11.10 • n=107 Participants
|
35.9 years
STANDARD_DEVIATION 10.33 • n=206 Participants
|
|
Sex: Female, Male
Female
|
2 Participants
n=99 Participants
|
2 Participants
n=107 Participants
|
4 Participants
n=206 Participants
|
|
Sex: Female, Male
Male
|
8 Participants
n=99 Participants
|
8 Participants
n=107 Participants
|
16 Participants
n=206 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
6 Participants
n=99 Participants
|
7 Participants
n=107 Participants
|
13 Participants
n=206 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
4 Participants
n=99 Participants
|
3 Participants
n=107 Participants
|
7 Participants
n=206 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
0 Participants
n=206 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
0 Participants
n=206 Participants
|
|
Race (NIH/OMB)
Asian
|
1 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
1 Participants
n=206 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
0 Participants
n=206 Participants
|
|
Race (NIH/OMB)
Black or African American
|
3 Participants
n=99 Participants
|
2 Participants
n=107 Participants
|
5 Participants
n=206 Participants
|
|
Race (NIH/OMB)
White
|
6 Participants
n=99 Participants
|
8 Participants
n=107 Participants
|
14 Participants
n=206 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
0 Participants
n=206 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
0 Participants
n=206 Participants
|
|
Region of Enrollment
United States
|
10 Participants
n=99 Participants
|
10 Participants
n=107 Participants
|
20 Participants
n=206 Participants
|
PRIMARY outcome
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: AUC0-24 of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to 24 Hours Post-dose (AUC0-24) of Pirtobrutinib
|
51700 hour nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 18.7
|
45500 hour nanogram per milliliter (h*ng/mL)
Geometric Coefficient of Variation 42.0
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: AUC0-t of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib
|
83900 h*ng/mL
Geometric Coefficient of Variation 25.1
|
77800 h*ng/mL
Geometric Coefficient of Variation 48.9
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: AUC0-inf of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Pirtobrutinib
|
85100 h*ng/mL
Geometric Coefficient of Variation 25.0
|
79000 h*ng/mL
Geometric Coefficient of Variation 48.3
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: %AUCextrap of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Pirtobrutinib
|
1.21 percentage of AUCextrap
Geometric Coefficient of Variation 43.7
|
1.25 percentage of AUCextrap
Geometric Coefficient of Variation 65.1
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed..
PK: CL/F of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib
|
2.35 liter per hour (L/h)
Geometric Coefficient of Variation 25.0
|
2.53 liter per hour (L/h)
Geometric Coefficient of Variation 48.3
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: t½ of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Apparent Plasma Terminal Elimination Half-life (t½) of Pirtobrutinib
|
18.4 hour
Geometric Coefficient of Variation 22.2
|
19.2 hour
Geometric Coefficient of Variation 25.4
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: Cmax of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Maximum Observed Concentration (Cmax) of Pirtobrutinib
|
4200 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 18.6
|
3250 nanogram per milliliter (ng/mL)
Geometric Coefficient of Variation 35.9
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: Tmax of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib
|
3.00 hour
Interval 1.5 to 4.05
|
4.00 hour
Interval 2.5 to 8.0
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: Lambda Z of pirtobrutinib was reported.
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 1
|
0.0199 1/hour (1/h)
|
0.0155 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 2
|
0.0355 1/hour (1/h)
|
0.0363 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 3
|
0.0308 1/hour (1/h)
|
0.0303 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 4
|
0.0457 1/hour (1/h)
|
0.0436 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 5
|
0.0473 1/hour (1/h)
|
0.0352 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 6
|
0.0333 1/hour (1/h)
|
0.0307 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 7
|
0.0394 1/hour (1/h)
|
0.0381 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 8
|
0.0427 1/hour (1/h)
|
0.0459 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 9
|
0.0404 1/hour (1/h)
|
0.0395 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 10
|
0.0315 1/hour (1/h)
|
0.0365 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 11
|
0.0554 1/hour (1/h)
|
0.0513 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 12
|
0.0302 1/hour (1/h)
|
0.0344 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 13
|
0.0331 1/hour (1/h)
|
0.0265 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 14
|
0.0362 1/hour (1/h)
|
0.0383 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 15
|
0.0382 1/hour (1/h)
|
0.0396 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 16
|
0.0466 1/hour (1/h)
|
0.0381 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 17
|
0.0392 1/hour (1/h)
|
0.0440 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 18
|
0.0432 1/hour (1/h)
|
0.0418 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 19
|
0.0408 1/hour (1/h)
|
0.0397 1/hour (1/h)
|
|
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
Subject 20
|
0.0408 1/hour (1/h)
|
0.0360 1/hour (1/h)
|
PRIMARY outcome
Timeframe: Pre-dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, and 168 hours post-dose on Days 1 and 8Population: The PK Population was consisted of all participants who had received 1 dose of pirtobrutinib, had at least 1 quantifiable plasma concentration, and for whom at least 1 PK parameter was computed.
PK: Vz/F of pirtobrutinib was reported
Outcome measures
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 Participants
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
PK: Apparent Volume of Distribution at the Terminal Phase (Vz/F) of Pirtobrutinib
|
62.5 liter
Geometric Coefficient of Variation 21.2
|
70.1 liter
Geometric Coefficient of Variation 43.4
|
Adverse Events
200 mg Pirtobrutinib (Fasted)
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
200 mg Pirtobrutinib (Fed)
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
200 mg Pirtobrutinib (Fasted)
n=20 participants at risk
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fasted conditions in Treatment A and B.
|
200 mg Pirtobrutinib (Fed)
n=20 participants at risk
Participants received a single oral dose of 200 mg pirtobrutinib was administered in the morning on Day 1 or Day 8, under fed conditions in Treatment A and B.
|
|---|---|---|
|
Nervous system disorders
Dizziness
|
5.0%
1/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
0.00%
0/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
|
Nervous system disorders
Dysgeusia
|
5.0%
1/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
0.00%
0/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
|
Nervous system disorders
Headache
|
0.00%
0/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
5.0%
1/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
|
Gastrointestinal disorders
Diarrhoea
|
0.00%
0/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
5.0%
1/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
|
Gastrointestinal disorders
Dry mouth
|
0.00%
0/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
5.0%
1/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
|
Skin and subcutaneous tissue disorders
Petechiae
|
5.0%
1/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
0.00%
0/20 • Baseline to end of follow-up (up to 24 days)
All participants who received at least 1 dose of Pirtobrutinib.
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: GT60