MedPath

Effect of Probenecid on Pexidartinib Pharmacokinetics

Phase 1
Completed
Conditions
Pharmacokinetics in Healthy Volunteers
Interventions
Registration Number
NCT03138759
Lead Sponsor
Daiichi Sankyo
Brief Summary

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.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
16
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

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Pexidartinib then ProbenecidProbenecidParticipants receive Sequence AB: Treatment A (pexidartinib) first, then Treatment B (probenecid), with a washout period between them
Probenecid then PexidartinibPexidartinibParticipants receive Sequence BA: Treatment B (probenecid) first, then Treatment A (pexidartinib), with a washout period between them
Probenecid then PexidartinibProbenecidParticipants receive Sequence BA: Treatment B (probenecid) first, then Treatment A (pexidartinib), with a washout period between them
Pexidartinib then ProbenecidPexidartinibParticipants receive Sequence AB: Treatment A (pexidartinib) first, then Treatment B (probenecid), with a washout period between them
Primary Outcome Measures
NameTimeMethod
Maximum Plasma Concentration (Cmax)predose to 312 hours post dose

Maximum concentration of the drug and its metabolite in plasma

Time to Maximum Concentration (Tmax)within 312 hours post dose

Time at which the maximum concentration is reached

Area under the curve to the last quantifiable measurement (AUClast)within 312 hours post dose

Area under the drug concentration time curve from the first measurement to the last

Secondary Outcome Measures
NameTimeMethod
Number of participants experiencing an adverse eventwithin 312 hours post dose

Total number of participants experiencing any adverse event

Trial Locations

Locations (1)

Worldwide Clinical Trials Early Phase Services

🇺🇸

San Antonio, Texas, United States

© Copyright 2025. All Rights Reserved by MedPath