Effect of Probenecid on Pexidartinib Pharmacokinetics

Overview

The primary objective of this trial is to assess the effect of probenecid on the pharmacokinetics (PK) of single-dose pexidartinib in healthy subjects. Secondary objectives are to assess the safety and tolerability of pexidartinib alone and in combination with probenecid. Participants will be confined to the clinic for approximately 32 days. Blood samples will be collected for PK analysis of pexidartinib and metabolites at predose and up to 312 hours (h) post dose.

Full Title of Study: “An Open-label, Randomized, 2-treatment, 2-period, Crossover Study to Evaluate the Effect of Probenecid on the Pharmacokinetics of Pexidartinib in Healthy Subjects”

Study Type

• Study Type: Interventional
• Study Design
  • Allocation: Randomized
  • Intervention Model: Crossover Assignment
  • Primary Purpose: Basic Science
  • Masking: None (Open Label)
• Study Primary Completion Date: March 30, 2017

Interventions

• Drug: Pexidartinib
  • Orally, on Day 2
• Drug: Probenecid
  • Orally, on Day 2

Arms, Groups and Cohorts

• Experimental: Pexidartinib then Probenecid
  • Participants receive Sequence AB: Treatment A (pexidartinib) first, then Treatment B (probenecid), with a washout period between them
• Experimental: Probenecid then Pexidartinib
  • Participants receive Sequence BA: Treatment B (probenecid) first, then Treatment A (pexidartinib), with a washout period between them

Clinical Trial Outcome Measures

Primary Measures

• Maximum Plasma Concentration (Cmax)
  • Time Frame: predose to 312 hours post dose
  • Maximum concentration of the drug and its metabolite in plasma
• Time to Maximum Concentration (Tmax)
  • Time Frame: within 312 hours post dose
  • Time at which the maximum concentration is reached
• Area under the curve to the last quantifiable measurement (AUClast)
  • Time Frame: within 312 hours post dose
  • Area under the drug concentration time curve from the first measurement to the last

Secondary Measures

• Number of participants experiencing an adverse event
  • Time Frame: within 312 hours post dose
  • Total number of participants experiencing any adverse event

Participating in This Clinical Trial

Inclusion Criteria

• Is a healthy, nonsmoking person with a body mass index of 18 kg/m2 to 30 kg/m2 (inclusive) at Screening – Is willing to be confined at the clinic for approximately 32 days – Is surgically sterile or a naturally postmenopausal female and not lactating, or a male who agrees to use double barrier methods of contraception and avoid donating sperm from Check-in until 90 d after the final dose of pexidartinib Exclusion Criteria:

• Has any history or condition, per protocol or in the opinion of the investigator, that might compromise the participant's safety, their ability to complete the trial, and or analysis of results

Gender Eligibility: All

Minimum Age: 18 Years

Maximum Age: 60 Years

Are Healthy Volunteers Accepted: Accepts Healthy Volunteers

Investigator Details

• Lead Sponsor
  • Daiichi Sankyo, Inc.
• Provider of Information About this Clinical Study
  • Sponsor
• Overall Official(s)
  • Clinical Study Leader, Study Director, Daiichi Sankyo, Inc.