A Study of Two Different Formulations of Pirtobrutinib (LOXO-305) In Healthy Participants

NCT06258174 | Completed Phase 1 Results FDA Drug

• 2 other identifiers: LOXO-BTK-21050J2N-OX-JZNV
• Study Type: interventional
• Target: 28
• Locations: 1 country
• Sites: 1

Brief Summary

The main purpose of this study is to compare two different formulations (mixtures) of pirtobrutinib (LOXO-305) in healthy participants. This study will compare how much of each formulation gets into the blood stream and how long it takes the body to remove it. Information about any side effects that may occur will be collected. The study will last up to 65 days.

Conditions

Healthy

Outcome Measures

Primary Outcomes (10)

• Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time 0 to 24 Hours Post-dose (AUC0-24) of Pirtobrutinib

  PK: AUC0-24 of Pirtobrutinib

  Predose, 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 postdose

• PK: Area Under the Concentration Versus Time Curve From Time Zero to the Last Measurable Concentration (AUC0-t) of Pirtobrutinib

  PK: AUC0-t of Pirtobrutinib

  Predose, 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 postdose

• PK: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of Pirtobrutinib

  PK: AUC0-inf of Pirtobrutinib

  Predose, 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 postdose

• PK: Percentage Extrapolation for AUC0-inf (%AUCextrap) of Pirtobrutinib

  PK: %AUCextrap of Pirtobrutinib

  Predose, 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 postdose

• PK: Apparent Systemic Clearance (CL/F) of Pirtobrutinib

  PK: CL/F of Pirtobrutinib

  Predose, 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 postdose

• PK: Apparent Plasma Terminal Elimination Half-life (t1/2) of Pirtobrutinib

  PK: t1/2 of Pirtobrutinib

  Predose, 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 postdose

• PK: Maximum Observed Plasma Concentration (Cmax) of Pirtobrutinib

  PK: Cmax of Pirtobrutinib

  Predose, 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 postdose

• PK: Time to Maximum Observed Plasma Concentration (Tmax) of Pirtobrutinib

  PK: Tmax of Pirtobrutinib

  Predose, 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 postdose

• PK: Apparent Terminal Elimination Rate Constant (λZ) of Pirtobrutinib

  PK: λZ of Pirtobrutinib

  Predose, 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 postdose

• PK: Apparent Volume of Distribution During the Terminal Phase (Vz/F) of Pirtobrutinib

  PK: Vz/F of Pirtobrutinib

  Predose, 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 postdose

Study Arms (2)

200 mg Pirtobrutinib (Sequence R/T)

EXPERIMENTAL

Period 1: Participants received a reference formulation (R) of oral pirtobrutinib 200 milligrams (mg) on day 1. Period 2: Participants received a test formulation (T) of oral pirtobrutinib 200 mg on day 8. There was a washout period of 7 days between the doses of pirtobrutinib.

Drug: Pirtobrutinib

200 mg Pirtobrutinib (Sequence T/R)

EXPERIMENTAL

Period 1: Participants received a test formulation (T) of oral pirtobrutinib 200 mg on day 1. Period 2: Participants received a reference formulation (R) of oral pirtobrutinib 200 mg on day 8. There was a washout period of 7 days between the doses of pirtobrutinib.

Drug: Pirtobrutinib

Interventions

Pirtobrutinib DRUG

Administered orally.

Also known as: LOXO-305, LY3527727

200 mg Pirtobrutinib (Sequence R/T); 200 mg Pirtobrutinib (Sequence T/R)

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Males and females of non-childbearing potential.
• Within body mass index (BMI) range 18.0 to 32.0 kilograms per square meter (kg/m²).
• Participants will be in good general health, based on medical history, physical examination findings, vital signs, 12 lead electrocardiogram (ECG), or clinical laboratory tests, as determined by the Investigator (or designee).

You may not qualify if:

• History or presence of any of the following, deemed clinically significant by the Investigator (or designee), and/or Sponsor:
• liver disease
• pancreatitis
• peptic ulcer disease
• intestinal malabsorption
• cholecystectomy
• gastric reduction surgery
• history or presence of clinically significant cardiovascular disease.
• Participants with out-of-range, at-rest vital signs.
• Abnormal laboratory values determined to be clinically significant by the Investigator (or designee).
• Clinically significant abnormality, as determined by the Investigator (or designee), from physical examination.
• Participation in any other investigational study drug trial involving administration of any investigational drug in the past 30 days or 5 half-lives, whichever was longer, prior to Day 1.
• Use or intention to use any prescription or over-the-counter medications within 14 days prior to Day 1 and through end of trial.
• History or presence, upon clinical evaluation, of any illness that, in the opinion of the Investigator, would interfere with the ability to provide informed consent or comply with study instructions, or that might confound the interpretation of the study results, or put the participant at undue risk.
• Donation of blood from 56 days prior to Screening, plasma or platelets from 4 weeks prior to Screening.

Sponsors & Collaborators

• Eli Lilly and Company: lead
• Loxo Oncology, Inc.: collaborator

Study Sites (1)

Labcorp Drug Development

Dallas, Texas, 75247, United States

Location

MeSH Terms

Interventions

pirtobrutinib

Results Point of Contact

• Title: Chief Medical Officer
• Organization: Eli Lilly and Company

ClinicalTrials.gov@lilly.com

800- 545-5979

Study Officials

• Renee Ward, MD, PhD

  Loxo Oncology, Inc.

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: GT60
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 6, 2024
• First Posted: February 14, 2024
• Study Start: September 28, 2021
• Primary Completion: December 22, 2021
• Study Completion: December 22, 2021
• Last Updated: January 13, 2025
• Results First Posted: January 13, 2025

Record last verified: 2024-11

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)