Relative Bioavailability Study of a Modified-Release Formulation of PF-06865571 in Healthy Adult Participants

Pfizer

Status and phase: Completed; Phase 1

Conditions: Healthy Participants

Treatments: Drug: PF-06865571 400 mg MR in Fed State; Drug: PF-06865571 400 mg MR in Fasted State; Drug: PF-06865571 50 mg Modified Release (MR) in Fed State; Drug: PF-06865571 400 mg Immediate Release (IR) in Fed State

Study type: Interventional

Funder types: Industry

Identifiers

NCT04044053

2019-001426-96 (EudraCT Number)

C2541012

Details and patient eligibility

About

This study is an open-label, randomized, single-dose, 4-period, 4-sequence, crossover study in a single cohort of approximately 12 healthy adult participants. The purpose of this study is to evaluate the relative bioavailability of a newly developed modified release (MR) tablet formulation of PF-06865571 relative to an immediate release (IR) tablet formulation of PF-06865571 under fed conditions. In addition, this study will also assess the relative bioavailability of the MR formulation under fasted conditions relative to fed conditions, in healthy adult participants. Study results will be used to determine if the new MR formulation may be suitable for use in future clinical studies with PF-06865571. Healthy adult Japanese participants will also be enrolled in this study to support inclusion of Japanese participants in future clinical studies.

Enrollment: 12 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Female participants of non-childbearing potential and male participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac tests.
• Body mass index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
• Participants enrolling as Japanese must have 4 biological Japanese grandparents who were born in Japan.

Exclusion criteria

• Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
• Use of prescription or nonprescription drugs and dietary and herbal supplements within 7 days or 5 half-lives (whichever is longer) prior to the first dose of investigational product.
• Previous administration with an investigational drug within 30 days (or as determined by the local requirement) or 5 half-lives preceding the first dose of investigational product used in this study (whichever is longer).
• Screening supine blood pressure (BP) ≥140 mm Hg (systolic) or ≥90 mm Hg (diastolic), following at least 5 minutes of supine rest.
• Baseline 12-lead electrocardiogram (ECG) that demonstrates clinically relevant abnormalities that may affect participant safety or interpretation of study results (eg, baseline corrected QT (QTc) interval >450 msec, complete left bundle branch block [LBBB], signs of an acute or indeterminate-age myocardial infarction, ST-T interval changes suggestive of myocardial ischemia, second- or third-degree atrioventricular [AV] block, or serious bradyarrhythmias or tachyarrhythmias).
• Participants with any of the following abnormalities in clinical laboratory tests at screening: Aspartate aminotransferase (AST) or alanine aminotransferase (ALT) level ≥1.25× upper limit of normal (ULN); Total bilirubin level ≥1.5× ULN; participants with a history of Gilbert's syndrome may have direct bilirubin measured and would be eligible for this study provided the direct bilirubin level is ≤ ULN.

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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12 participants in 2 patient groups

Relative Bioavailability

Experimental group

Description:

Each participant will receive 400 mg IR, 400 mg MR, and 50 mg MR in the fed state, and 400 mg MR in the fasted state

Treatment:

Drug: PF-06865571 50 mg Modified Release (MR) in Fed State

Drug: PF-06865571 400 mg Immediate Release (IR) in Fed State

Drug: PF-06865571 400 mg MR in Fasted State

Drug: PF-06865571 400 mg MR in Fed State

Fasted State

Experimental group

Description:

Comparison of 400 mg MR in fed and fasted states

Treatment:

Drug: PF-06865571 400 mg MR in Fasted State

Drug: PF-06865571 400 mg MR in Fed State