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

NCT04044053 | Completed Phase 1 FDA Drug

• 2 other identifiers: C25410122019-001426-96
• Study Type: interventional
• Target: 12
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Healthy Participants

Keywords

PF-06865571; Relative bioavailability; Modified release; Diacylglycerol acyltransferase; DGAT2; Japanese

Outcome Measures

Primary Outcomes (4)

• Single Dose Maximum Observed Plasma Concentration (Cmax) of PF-06865571 in Healthy Participants

  All study participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

• Single Dose Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-06865571 in Healthy Participants

  All study participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

• Single Dose Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC(last)] of PF-06865571 in Healthy Participants

  All study participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

• Single Dose Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC(0-∞)] of PF-06865571 in Healthy Participants

  All study participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

Secondary Outcomes (12)

• Single Dose Cmax of PF-06865571 in Healthy Japanese Participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

• Single Dose Tmax of PF-06865571 in Healthy Japanese Participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

• Single Dose AUC(last) of PF-06865571 in Healthy Japanese Participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

• Single Dose AUC(0-∞) of PF-06865571 in Healthy Japanese Participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

• Fasted State Single Dose Cmax of Modified-Release (MR) Formulation of PF-06865571 in Healthy Participants

  Hour 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, 48 hours post-dose

Study Arms (2)

Relative Bioavailability

EXPERIMENTAL

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

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

Fasted State

EXPERIMENTAL

Comparison of 400 mg MR in fed and fasted states

Drug: PF-06865571 400 mg MR in Fed State; Drug: PF-06865571 400 mg MR in Fasted State

Interventions

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

400 mg IR dose in fed state

Relative Bioavailability

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

50 mg MR in fed state

Relative Bioavailability

PF-06865571 400 mg MR in Fed State DRUG

400 mg MR in fed state

Fasted State; Relative Bioavailability

PF-06865571 400 mg MR in Fasted State DRUG

400 mg MR in fasted state

Fasted State; Relative Bioavailability

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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.

You may not qualify if:

• 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.

Sponsors & Collaborators

• Pfizer: lead

Study Sites (1)

Brussels Clinical Research Unit

Brussels, Be-bru, B-1070, Belgium

Location

Related Links

• To obtain contact information for a study center near you, click here.

MeSH Terms

Interventions

ervogastat

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 1, 2019
• First Posted: August 2, 2019
• Study Start: August 13, 2019
• Primary Completion: October 31, 2019
• Study Completion: October 31, 2019
• Last Updated: November 27, 2019

Record last verified: 2019-11

Data Sharing

• IPD Sharing: Will not share

Locations

BE (1)