Effect of Probenecid on Pexidartinib Pharmacokinetics

Daiichi Sankyo

Status and phase: Completed; Phase 1

Conditions: Pharmacokinetics in Healthy Volunteers

Treatments: Drug: Pexidartinib; Drug: Probenecid

Study type: Interventional

Funder types: Industry

Identifiers

NCT03138759

PL3397-A-U122

Details and patient eligibility

About

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.

Enrollment: 16 patients

Sex: All

Ages: 18 to 60 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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16 participants in 2 patient groups

Pexidartinib then Probenecid

Experimental group

Description:

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

Treatment:

Drug: Probenecid

Drug: Pexidartinib

Probenecid then Pexidartinib

Experimental group

Description:

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

Treatment:

Drug: Probenecid

Drug: Pexidartinib