Clinical Study to Evaluate Pharmacokinetics and Safety of PF-06700841 After Single and Multiple Oral Doses as Modified Release Formulations

Phase 1

Completed

• Conditions: Healthy Participants
• Interventions: Drug: PF-06700841 IR; Drug: PF-06700841 MR3; Drug: PF-06700841 MR1; Other: Placebo; Drug: PF-06700841 MR2

• Registration Number: NCT04580797
• Lead Sponsor: Pfizer

Brief Summary

The purpose of the study is to evaluate the pharmacokinetics (PK), safety, and tolerability of PF-06700841 following single and multiple oral doses as modified release (MR) formulations in healthy, adult participants under fasted and fed conditions. The objective of Part A is to evaluate the relative bioavailability and food effect of 2 new MR formulations, MR1 and MR2. The objective of Part B is to evaluate the PK and safety/tolerability of MR3 formulation following multiple dose administration over a 7-day period. Overall, results from both parts will facilitate further development of an MR formulation for future clinical studies.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2020-09-25
• Study Start: 2020-10-02
• Study First Submitted QC: 2020-10-05
• Study First Posted: 2020-10-08
• Primary Completion: 2021-01-11
• Study Completion: 2021-01-11
• Status Verified: 2021-03
• Last Update Submitted: 2021-03-04
• Last Update Posted: 2021-03-08

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 36

Inclusion Criteria

• Healthy male and female participants between 18 -55 years of age.
• BMI of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
• Participants who are willing and able to comply with all scheduled visits, treatment
• plan, laboratory tests, lifestyle considerations, and other study procedures.

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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).
• Conditions that affect drug absorption (e.g., gastrectomy cholecystectomy)
• History of venous and arterial thrombosis (ie, deep venous thrombosis, pulmonary embolism) or hereditary clotting disorders (in first degree immediate relatives)
• Positive urine drug test.
• History of human immunodeficiency virus (HIV) infection, hepatitis B, or hepatitis C; positive testing for HIV, hepatitis B surface antigen (HBsAg), hepatitis B core antibody (HBcAb) or hepatitis C antibody (HCVAb). Hepatitis B vaccination is allowed.
• History of alcohol abuse or binge drinking and/or any other illicit drug use or dependence within 6 months of Screening. Binge drinking is defined as a pattern of 5 (male) and 4 (female) or more alcoholic drinks in about 2 hours

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
PF-06700841: IR, MR1, MR2, MR1_fed	PF-06700841 IR	Participants receive single doses of immediate release (IR) followed by modified release (MR) MR1 and MR2, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: MR2, IR, MR1, MR1_fed	PF-06700841 MR1	Participants receive single doses of MR2 followed by IR and MR1, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: IR, MR1, MR2, MR2_fed	PF-06700841 IR	Participants receive single doses of IR followed by MR1 and MR1, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841: IR, MR1, MR2, MR1_fed	PF-06700841 MR2	Participants receive single doses of immediate release (IR) followed by modified release (MR) MR1 and MR2, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: MR1, MR2, IR, MR1_fed	PF-06700841 MR1	Participants receive single doses of MR1 followed by MR2 and IR, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: MR2, IR, MR1, MR1_fed	PF-06700841 MR2	Participants receive single doses of MR2 followed by IR and MR1, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: MR2, IR, MR1, MR2_fed	PF-06700841 IR	Participants receive single doses of MR2 followed by IR and MR1, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841: IR, MR1, MR2, MR2_fed	PF-06700841 MR1	Participants receive single doses of IR followed by MR1 and MR1, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841: MR1, MR2, IR, MR2_fed	PF-06700841 MR2	Participants receive single doses of MR1 followed by MR2 and IR, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841: IR, MR1, MR2, MR2_fed	PF-06700841 MR2	Participants receive single doses of IR followed by MR1 and MR1, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841: MR2, IR, MR1, MR2_fed	PF-06700841 MR1	Participants receive single doses of MR2 followed by IR and MR1, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841 MR3 (Dose A) or matching placebo	PF-06700841 MR3	Participants receive dosing regimen 1 of MR3 (Dose A) or matching placebo for 7 days under fasted condition
PF-06700841: IR, MR1, MR2, MR1_fed	PF-06700841 MR1	Participants receive single doses of immediate release (IR) followed by modified release (MR) MR1 and MR2, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: MR1, MR2, IR, MR1_fed	PF-06700841 MR2	Participants receive single doses of MR1 followed by MR2 and IR, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: MR1, MR2, IR, MR2_fed	PF-06700841 IR	Participants receive single doses of MR1 followed by MR2 and IR, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841: MR1, MR2, IR, MR1_fed	PF-06700841 IR	Participants receive single doses of MR1 followed by MR2 and IR, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: MR2, IR, MR1, MR2_fed	PF-06700841 MR2	Participants receive single doses of MR2 followed by IR and MR1, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841 MR3 (Dose B) or matching placebo	PF-06700841 MR3	Participants receive dosing regimen 1 of MR3 (Dose B) or matching placebo for 7 days under fasted condition
PF-06700841 MR3 (Dose B) or matching placebo	Placebo	Participants receive dosing regimen 1 of MR3 (Dose B) or matching placebo for 7 days under fasted condition
PF-06700841: MR2, IR, MR1, MR1_fed	PF-06700841 IR	Participants receive single doses of MR2 followed by IR and MR1, all in fasted condition followed by MR1 in fed condition in Periods 1-4
PF-06700841: MR1, MR2, IR, MR2_fed	PF-06700841 MR1	Participants receive single doses of MR1 followed by MR2 and IR, all in fasted condition followed by MR2 in fed condition in Periods 1-4
PF-06700841 MR3 (Dose A) or matching placebo	Placebo	Participants receive dosing regimen 1 of MR3 (Dose A) or matching placebo for 7 days under fasted condition
PF-06700841 MR3 (Dose C) or matching placebo	Placebo	Participants receive dosing regimen 1 of MR3 (Dose C) or matching placebo for 7 days under fasted condition
PF-06700841 MR3 (Dose C) or matching placebo	PF-06700841 MR3	Participants receive dosing regimen 1 of MR3 (Dose C) or matching placebo for 7 days under fasted condition

Primary Outcome Measures

Name	Time	Method
Time to reach maximum observed plasma concentration (Tmax) of PF-06700841 in Part A	pre-dose, 1,2,4,6,8,10,12,16,24,36,48,72 hours post dose
Maximum Observed Plasma Concentration (Cmax) of PF-06700841 in Part A	pre-dose, 1,2,4,6,8,10,12,16,24,36,48,72 hours post dose
Area under the plasma concentration-time curve from time zero to extrapolated infinite time (AUCinf) of PF-06700841 if data permit in Part A	pre-dose, 1,2,4,6,8,10,12,16,24,36,48,72 hours post dose
Number of participants with Treatment- Emergent Adverse Events (AEs), Serious Adverse Events (SAEs) and Discontinuation due to AEs in Part B	Baseline to Day 10
Area under the plasma concentration-time curve from time zero to the last measured concentration (AUClast) of PF-06700841 in Part A	pre-dose, 1,2,4,6,8,10,12,16,24,36,48,72 hours post dose

Secondary Outcome Measures

Name	Time	Method
Maximum Observed Plasma Concentration (Cmax) of PF-06700841 in Part B on Day 1	pre-dose, 1,2,3,4,6,8,10,12,16 hours post dose on Day 1
Area under the plasma concentration-time curve from time zero to 24 hours (AUC24) of PF-06700841 in Part B on Day 1	pre-dose, 1,2,4,6,8,10,12,16 hours post dose on Day 1, pre-dose on Day 3 and Day 5, pre-dose on Day 7, 1,2,3,4,6,8,12,16,24,48,72 hours post dose on Day 7
Area under the plasma concentration-time curve from time zero to 24 hours (AUCtau) of PF-06700841 in Part B on Day 7	pre-dose, 1,2,4,6,8,10,12,16 hours post dose on Day 1, pre-dose on Day 3 and Day 5, pre-dose on Day 7, 1,2,3,4,6,8,12,16,24,48,72 hours post dose on Day 7
Number of subjects with clinically relevant changes in vital signs in Part A	Pre-dose and 96 hours post dose
Time to reach maximum observed plasma concentration (Tmax) of PF-06700841 in Part B on Day 7	pre-dose on Day 7, 1,2,3 4,6,8,12,16,24,48,72 hours post dose on Day 7
Number of participants with Treatment- Emergent Adverse Events (AEs), Serious Adverse Events (SAEs) and Discontinuation due to AEs in Part A	Baseline to Day 4
Number of subjects with clinically relevant changes in Electrocardiogram (ECG) parameters in Part A	Pre-dose and 96 hours post dose
Number of participants with clinically relevant changes in clinical laboratory tests in Part A	Baseline and 96 hours post dose
Time to reach maximum observed plasma concentration (Tmax) of PF-06700841 in Part B on Day 1	pre-dose, 1,2,4,6,8,10,12,16 hours post dose on Day 1
Maximum Observed Plasma Concentration (Cmax) of PF-06700841 in Part B on Day 7	pre-dose on Day 7, 1,2,3 4,6,8,12,16,24,48,72 hours post dose on Day 7
Terminal half-life of PF-06700841 in Part B	pre-dose, 1,2,4,6,8,10,12,16 hours post dose on Day 1, pre-dose on Day 3 and Day 5, pre-dose on Day 7, 1,2,3,4,6,8,12,16,24,48,72 hours post dose on Day 7

Trial Locations

Locations (2)

Quotient Sciences; 🇺🇸 Coral Gables, Florida, United States

Quotient Sciences-Miami; 🇺🇸 Miami, Florida, United States