Phase 1
Completed N=16
A Study of the Effects of Pirtobrutinib (LOXO-305) on Repaglinide (CYP2C8 Substrate) in Healthy Participants
Healthy
Source: ClinicalTrials.gov NCT06165146 ↗
Enrolled (actual)
16
Serious AEs
0.0%
Results posted
Mar 2025
Primary outcomePrimary: Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Repaglinide — 9.59; 22.2 hour*nanogram per milliliter (h*ng/mL)
Summary
The main purpose of this study is to evaluate the effect of pirtobrutinib (LOXO-305) on single oral dose of repaglinide (CYP2C8 substrate) when administered as multiple doses by conducting the blood tests to measure how much pirtobrutinib (LOXO-305) is in the bloodstream and how the body handles and eliminates pirtobrutinib (LOXO-305) in adult healthy participants. The study will also evaluate the safety and tolerability of pirtobrutinib (LOXO-305). The study is conducted in two periods. Participants will stay in this study for up to 54 days.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Pharmacokinetics (PK): Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Repaglinide |
9.59; 22.2 | — |
| PRIMARY PK: Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity (AUC0-inf) of Repaglinide |
9.79; 22.5 | — |
| PRIMARY PK: Percentage of AUC0-inf Extrapolated (AUC%Extrap) of Repaglinide |
1.94; 1.10 | — |
| PRIMARY PK: Maximum Observed Concentration (Cmax) of Repaglinide |
6.88; 13.6 | — |
| PRIMARY PK: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Repaglinide |
0.625; 0.750 | — |
| PRIMARY PK: Apparent Terminal Elimination Rate Constant (Lambda Z) of Repaglinide |
0.128; 0.152; 0.130; 0.150; 0.228; 0.151 | — |
| PRIMARY PK: Apparent Systemic Clearance (CL/F) of Repaglinide |
51.1; 22.2 | — |
| PRIMARY PK: Apparent Plasma Terminal Elimination Half-life (t½) of Repaglinide |
4.86; 4.11 | — |
| PRIMARY PK: Apparent Volume of Distribution (Vz/F) of Repaglinide |
358; 131 | — |
| PRIMARY PK: Area Under the Concentration-time Curve, From Time 0 to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib |
184000 | — |
| PRIMARY PK: Area Under the Concentration-time Curve During a Dosing Interval (AUCtau) of Pirtobrutinib |
105000 | — |
| PRIMARY PK: Maximum Observed Concentration (Cmax) of Pirtobrutinib |
7220 | — |
| PRIMARY PK: Concentration Observed at the End of the Dosing Interval (Ctrough) of Pirtobrutinib |
3050 | — |
| PRIMARY PK: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib |
1.00 | — |
| PRIMARY PK: Apparent Systemic Clearance (CL/F) at Steady State of Pirtobrutinib |
1.91 | — |
Eligibility Criteria
Inclusion Criteria
- Must have Body mass index (BMI) within the range of 18.0 to 32.0 kilograms per square meter (kg/m²), inclusive
- 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 16-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
- 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)
Data sourced from ClinicalTrials.gov (NCT06165146). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.