Healthy
Conditions
Brief summary
The main purpose of this study is to conduct blood tests to measure how much pirtobrutinib (LOXO-305) is in the bloodstream and how the body handles and eliminates pirtobrutinib (LOXO-305) after meals and on an empty stomach. The study will also evaluate the safety and tolerability of pirtobrutinib (LOXO-305). Participants will stay in this study for up to 53 days (screening through follow-up call).
Interventions
DRUGPirtobrutinib
Administered orally.
Sponsors
Loxo Oncology, Inc.
Eli Lilly and Company
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Must have Body mass index (BMI) within the range of 18.0 to 32.0 kilograms per square meter (kg/m²), inclusive at Screening * Male and female participants in good health, determined by no clinically significant findings from medical history, 12-lead Electrocardiogram (ECG), vital sign measurements, or clinical laboratory evaluations as assessed by the investigator * Female participants of non-childbearing potential and male participants who follow standard contraceptive methods * Must have comply with all study procedures, including the 15-night stay at the Clinical Research Unit (CRU) and follow-up phone call
Exclusion criteria
* History or presence of any diseases or conditions of clinical significance by the Investigator (or designee) and/or Sponsor * Positive serologic test for hepatitis B surface antigen (HBsAg), hepatitis B virus immunoglobulin M (HBV IgM) core antibody, hepatitis C virus (HCV) antibody, or human immunodeficiency virus (HIV) antibody at Screening. * Positive polymerase chain reaction (PCR) test for COVID-19 at Screening * Known ongoing alcohol and/or drug abuse within 2 years prior to Screening * History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance, unless approved by the Investigator (or designee) * Have previously received pirtobrutinib (LOXO-305) in any other study investigating pirtobrutinib (LOXO-305), within 30 days prior to Day 1
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to 24 Hours Post-dose (AUC0-24) of Pirtobrutinib | 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 | PK: AUC0-24 of pirtobrutinib was reported. |
| PK: Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib | 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 8 | PK: AUC0-t of pirtobrutinib was reported. |
| PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Pirtobrutinib | 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 8 | PK: AUC0-inf of pirtobrutinib was reported. |
| PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Pirtobrutinib | 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 8 | PK: %AUCextrap of pirtobrutinib was reported. |
| PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib | 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 8 | PK: CL/F of pirtobrutinib was reported. |
| PK: Apparent Plasma Terminal Elimination Half-life (t½) of Pirtobrutinib | 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 8 | PK: t½ of pirtobrutinib was reported. |
| PK: Maximum Observed Concentration (Cmax) of Pirtobrutinib | 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 8 | PK: Cmax of pirtobrutinib was reported. |
| PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib | 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 8 | PK: Tmax of pirtobrutinib was reported. |
| PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | 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 8 | PK: Lambda Z of pirtobrutinib was reported. |
| PK: Apparent Volume of Distribution at the Terminal Phase (Vz/F) of Pirtobrutinib | 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 8 | PK: Vz/F of pirtobrutinib was reported |
Countries
United States
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| 200 mg Pirtobrutinib: Treatment AB 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. | 10 |
| 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. | 10 |
| Total | 20 |
Baseline characteristics
| Characteristic | 200 mg Pirtobrutinib: Treatment AB | Total | 200 mg Pirtobrutinib: Treatment BA |
|---|---|---|---|
| Age, Continuous | 35.9 years STANDARD_DEVIATION 10.1 | 35.9 years STANDARD_DEVIATION 10.33 | 35.9 years STANDARD_DEVIATION 11.1 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 6 Participants | 13 Participants | 7 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 4 Participants | 7 Participants | 3 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Asian | 1 Participants | 1 Participants | 0 Participants |
| Race (NIH/OMB) Black or African American | 3 Participants | 5 Participants | 2 Participants |
| Race (NIH/OMB) More than one race | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) White | 6 Participants | 14 Participants | 8 Participants |
| Region of Enrollment United States | 10 Participants | 20 Participants | 10 Participants |
| Sex: Female, Male Female | 2 Participants | 4 Participants | 2 Participants |
| Sex: Female, Male Male | 8 Participants | 16 Participants | 8 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk |
|---|---|---|
| deaths Total, all-cause mortality | 0 / 20 | 0 / 20 |
| other Total, other adverse events | 2 / 20 | 2 / 20 |
| serious Total, serious adverse events | 0 / 20 | 0 / 20 |
Outcome results
Primary
Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to 24 Hours Post-dose (AUC0-24) of Pirtobrutinib
PK: AUC0-24 of pirtobrutinib was reported.
Time frame: 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
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | 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 |
| 200 mg Pirtobrutinib (Fed) | Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to 24 Hours Post-dose (AUC0-24) of Pirtobrutinib | 45500 hour nanogram per milliliter (h*ng/mL) | Geometric Coefficient of Variation 42 |
Primary
PK: Apparent Plasma Terminal Elimination Half-life (t½) of Pirtobrutinib
PK: t½ of pirtobrutinib was reported.
Time frame: 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 8
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Plasma Terminal Elimination Half-life (t½) of Pirtobrutinib | 18.4 hour | Geometric Coefficient of Variation 22.2 |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Plasma Terminal Elimination Half-life (t½) of Pirtobrutinib | 19.2 hour | Geometric Coefficient of Variation 25.4 |
Primary
PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib
PK: CL/F of pirtobrutinib was reported.
Time frame: 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 8
Population: 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..
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib | 2.35 liter per hour (L/h) | Geometric Coefficient of Variation 25 |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib | 2.53 liter per hour (L/h) | Geometric Coefficient of Variation 48.3 |
Primary
PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib
PK: Lambda Z of pirtobrutinib was reported.
Time frame: 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 8
Population: 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.
| Arm | Measure | Group | Value (NUMBER) |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 19 | 0.0408 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 1 | 0.0199 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 2 | 0.0355 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 3 | 0.0308 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 4 | 0.0457 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 5 | 0.0473 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 6 | 0.0333 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 7 | 0.0394 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 8 | 0.0427 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 9 | 0.0404 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 10 | 0.0315 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 11 | 0.0554 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 12 | 0.0302 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 13 | 0.0331 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 14 | 0.0362 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 15 | 0.0382 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 16 | 0.0466 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 17 | 0.0392 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 18 | 0.0432 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 20 | 0.0408 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 17 | 0.0440 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 19 | 0.0397 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 10 | 0.0365 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 1 | 0.0155 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 15 | 0.0396 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 2 | 0.0363 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 11 | 0.0513 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 3 | 0.0303 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 20 | 0.0360 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 4 | 0.0436 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 12 | 0.0344 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 5 | 0.0352 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 16 | 0.0381 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 6 | 0.0307 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 13 | 0.0265 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 7 | 0.0381 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 18 | 0.0418 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 8 | 0.0459 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 14 | 0.0383 1/hour (1/h) |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Pirtobrutinib | Subject 9 | 0.0395 1/hour (1/h) |
Primary
PK: Apparent Volume of Distribution at the Terminal Phase (Vz/F) of Pirtobrutinib
PK: Vz/F of pirtobrutinib was reported
Time frame: 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 8
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | PK: Apparent Volume of Distribution at the Terminal Phase (Vz/F) of Pirtobrutinib | 62.5 liter | Geometric Coefficient of Variation 21.2 |
| 200 mg Pirtobrutinib (Fed) | PK: Apparent Volume of Distribution at the Terminal Phase (Vz/F) of Pirtobrutinib | 70.1 liter | Geometric Coefficient of Variation 43.4 |
Primary
PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Pirtobrutinib
PK: AUC0-inf of pirtobrutinib was reported.
Time frame: 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 8
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | 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 |
| 200 mg Pirtobrutinib (Fed) | PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Pirtobrutinib | 79000 h*ng/mL | Geometric Coefficient of Variation 48.3 |
Primary
PK: Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib
PK: AUC0-t of pirtobrutinib was reported.
Time frame: 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 8
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | 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 |
| 200 mg Pirtobrutinib (Fed) | PK: Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib | 77800 h*ng/mL | Geometric Coefficient of Variation 48.9 |
Primary
PK: Maximum Observed Concentration (Cmax) of Pirtobrutinib
PK: Cmax of pirtobrutinib was reported.
Time frame: 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 8
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | PK: Maximum Observed Concentration (Cmax) of Pirtobrutinib | 4200 nanogram per milliliter (ng/mL) | Geometric Coefficient of Variation 18.6 |
| 200 mg Pirtobrutinib (Fed) | PK: Maximum Observed Concentration (Cmax) of Pirtobrutinib | 3250 nanogram per milliliter (ng/mL) | Geometric Coefficient of Variation 35.9 |
Primary
PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Pirtobrutinib
PK: %AUCextrap of pirtobrutinib was reported.
Time frame: 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 8
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Pirtobrutinib | 1.21 percentage of AUCextrap | Geometric Coefficient of Variation 43.7 |
| 200 mg Pirtobrutinib (Fed) | PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Pirtobrutinib | 1.25 percentage of AUCextrap | Geometric Coefficient of Variation 65.1 |
Primary
PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib
PK: Tmax of pirtobrutinib was reported.
Time frame: 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 8
Population: 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.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| 200 mg Pirtobrutinib (Fasted) | PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib | 3.00 hour |
| 200 mg Pirtobrutinib (Fed) | PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib | 4.00 hour |