Effect of Low-Fat Food on Pexidartinib Pharmacokinetics in Healthy Volunteers

Daiichi Sankyo

Status and phase: Completed; Phase 1

Conditions: Healthy Volunteers

Treatments: Drug: Treatment A - 400 mg Fasting; Drug: Treatment B - 400 mg Fed; Drug: Treatment C - 200 mg Fed

Study type: Interventional

Funder types: Industry

Identifiers

NCT03901313

PL3397-A-U128

Details and patient eligibility

About

All participants in this study are healthy volunteers.

Throughout the study, healthy volunteers will have physical exams, electrocardiograms and clinical laboratory tests. The study staff will keep track of symptoms, diet, and what medications they are taking.

Each participant will get all three treatments (A, B and C). Only the order in which they receive them will be different.

There are six groups based on the order: ABC, ACB, BAC, BCA, CAB, or CBA. Participants have an equal chance of being assigned to any of these groups.

For each treatment period, participants will:

• fast overnight
• receive the assigned treatment with or without food
• have a small tube of blood drawn prior to treatment
• after dosing, additional blood samples will be drawn at 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 14, 22, 24, 28, 32, 36, 48, 54, 60, 72, 84, 96, 108, 120, 132, and 144 hours
• have a break from treatment for 6 days between each treatment period

All participants must reside in the clinic for a total of 20 days.

Full description

The primary objectives of this study are:

• To assess the effect of low-fat food on the pharmacokinetics (PK) of pexidartinib following a single oral dose of 400 mg administered in healthy subjects
• To assess the PK of pexidartinib following a single oral dose of 200 mg administered with low-fat food in healthy subjects

The secondary objective of this study is:

• To characterize the safety and tolerability of pexidartinib in healthy subjects following administration of a single oral dose of pexidartinib with low fat food and without food

Enrollment: 24 patients

Sex: All

Ages: 18 to 60 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Is healthy at screening visit

• Is not pregnant or lactating

• Is surgically or naturally unable to reproduce, or agrees to remain sexually abstinent or to use double barrier methods of contraception from check-in until 90 days after the final dose of pexidartinib

• Has a Body Mass Index (BMI) of 18-30 kg/m^2, inclusive

• Has negative test results for protocol-defined drugs and diseases at screening and/or check-in

• Is willing to avoid food or beverages before check-in until the end of the study:

  1. containing caffeine/xanthine or alcohol from 48 hours before check-in
  2. containing grapefruit or Seville oranges 6 days before check-in

Exclusion criteria

• Per protocol or in the opinion of the investigator at screening and/or check-in, has something that would preclude participation:

  1. has a clinically significant disorder, disease or lab value
  2. consumes a prohibited drug, drink or food
  3. is unable to consume the standard meal

• Is an employee of the clinic or their family member

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Sequential Assignment

Masking: None (Open label)

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24 participants in 6 patient groups

Sequence ABC

Experimental group

Description:

Healthy volunteers will receive Treatments A, then B, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days

Treatment:

Drug: Treatment C - 200 mg Fed

Drug: Treatment B - 400 mg Fed

Drug: Treatment A - 400 mg Fasting

Sequence ACB

Experimental group

Description:

Healthy volunteers will receive Treatments A, then C, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days

Treatment:

Drug: Treatment C - 200 mg Fed

Drug: Treatment B - 400 mg Fed

Drug: Treatment A - 400 mg Fasting

Sequence BAC

Experimental group

Description:

Healthy volunteers will receive Treatments B, then A, and then C, with a 6-day washout between treatments, during a stay at the clinic of 20 days

Treatment:

Drug: Treatment C - 200 mg Fed

Drug: Treatment B - 400 mg Fed

Drug: Treatment A - 400 mg Fasting

Sequence BCA

Experimental group

Description:

Healthy volunteers will receive Treatments B, then C, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days

Treatment:

Drug: Treatment C - 200 mg Fed

Drug: Treatment B - 400 mg Fed

Drug: Treatment A - 400 mg Fasting

Sequence CAB

Experimental group

Description:

Healthy volunteers will receive Treatments C, then A, and then B, with a 6-day washout between treatments, during a stay at the clinic of 20 days

Treatment:

Drug: Treatment C - 200 mg Fed

Drug: Treatment B - 400 mg Fed

Drug: Treatment A - 400 mg Fasting

Sequence CBA

Experimental group

Description:

Healthy volunteers will receive Treatments C, then B, and then A, with a 6-day washout between treatments, during a stay at the clinic of 20 days

Treatment:

Drug: Treatment C - 200 mg Fed

Drug: Treatment B - 400 mg Fed

Drug: Treatment A - 400 mg Fasting