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A Study To Understand Safety And Plasma Concentrations Of PF-06669571 During And Following The Oral Administration Of Single And Multiple Doses Of PF-06669571 In Healthy Volunteers Under Fasted And Fed Conditions

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02184429
Lead Sponsor
Pfizer
Brief Summary

This study is designed to evaluate the safety and plasma concentrations of PF-06669571 in healthy volunteers following single and multiple ascending doses of PF-06669571. Effect of food on PF-06669571 plasma concentrations will be be evaluated after a single dose of PF-06669571. During multiple dose phase, PF-06669571 will be administered daily for 14 days

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
56
Inclusion Criteria
  • Healthy male and/or female subjects of non-childbearing potential between the ages of 18 and 55 years, inclusive (Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12-lead ECG and clinical laboratory tests).

Female subjects of non-childbearing potential must meet at least one of the following criteria:

  1. Achieved postmenopausal status, defined as follows: cessation of regular menses for at least 12 consecutive months with no alternative pathological or physiological cause; and have a serum follicle-stimulating hormone (FSH) level confirming the post-menopausal state;

  2. Have undergone a documented hysterectomy and/or bilateral oophorectomy;

  3. Have medically confirmed ovarian failure. All other female subjects (including females with tubal ligations and females that do NOT have a documented hysterectomy, bilateral oophorectomy and/or ovarian failure) will be considered to be of childbearing potential.

    • Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).
    • Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study.
    • Subjects who are willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures.
Exclusion Criteria
  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
  • Treatment with an investigational drug within 30 days (or as determined by the local requirement) or 5 half-lives preceding the first dose of study medication (whichever is longer).
  • Screening supine blood pressure >= 140 mm Hg (systolic) or >=90 mm Hg (diastolic), following at least 5 minutes of rest. If BP is >=140 mm Hg (systolic) or >=90 mm Hg (diastolic), repeat per local standard operating procedures (SOP). If orthostatic changes are present and deemed to be clinically significant by the investigator, Subject can be excluded.
  • For subjects who answer "Yes" to the Columbia Suicide Severity Rating Scale (C-SSRS) questions 4 or 5, a risk assessment should be done by a qualified mental health professional (MHP: a psychiatrist or licensed PhD level clinical psychologist) to assess whether it is safe for the subject to participate in the study. In addition, subjects deemed by the investigator to be at significant risk of suicidal or violent behavior should be excluded.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Multiple Ascending Dose-3PF-06669571Daily dose of PF-06669571 in healthy volunteers
Single Ascending Dose-1PF-06669571Single ascending doses of PF-06669571 administered to healthy volunteers in a cross over study design
Single Ascending Dose-2PF-06669571Single ascending doses of PF-06669571 administered to healthy volunteers in a cross over study design
Multiple Ascending Dose-1PF-06669571Daily dose of PF-06669571 in healthy volunteers
Multiple Ascending Dose-2PF-06669571Daily dose of PF-06669571 in healthy volunteers
Multiple Ascending Dose-4PF-06669571Daily dose of PF-06669571 in healthy volunteers
Multiple Ascending Dose-5PF-06669571Daily dose of PF-06669571 in healthy volunteers
Primary Outcome Measures
NameTimeMethod
Number of Participants with categorical scores on the Columbia Suicide Severity Rating Scale (C-SSRS)screening,Day 28

C-SSRS assessed whether participant experienced following: completed suicide (1), suicide attempt (2) (response of "Yes" on "actual attempt"), preparatory acts toward imminent suicidal behavior (3)("Yes" on "preparatory acts or behavior"), suicidal ideation (4) ("Yes" on "wish to be dead", "non-specific active suicidal thoughts", "active suicidal ideation with methods without intent to act or some intent to act, without specific plan or with specific plan and intent), any suicidal behavior or ideation, self-injurious behavior (7)("Yes" on "Has subject engaged in non-suicidal self-injurious behavior").

Secondary Outcome Measures
NameTimeMethod
Maximum Observed Plasma Concentration (Cmax) after single dose0-Day 5

Cmax after a single dose

Accumulation ratio (Rac) for Cmax on days 7 and 14 after multiple daily doses0-Day 18
Pre dose concentrations (Ctrough) on days 7 and 14 after multiple daily doses0-Day 18
Minimum Observed Plasma Trough Concentration (Cmin) on days 7 and 14 after multiple daily doses0-Day 18
Accumulation ratio (Rac) for AUCtau on days 7 and 14 after multiple daily doses0-day 18
Apparent Oral Clearance (CL/F) on day 7 and 14 after multiple daily doses0-Day 18

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population pharmacokinetic (PK) modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.

Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) after single dose0-Day 5

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) after single dose

Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - inf)] after single dose0-Day 5

AUC (0 - inf)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - inf). It is obtained from AUC (0 - t) plus AUC (t - inf) after single dose

Time to Reach Maximum Observed Plasma Concentration (Tmax) after single dose0-Day 5

Tmax after single dose

Plasma Decay Half-Life (t1/2) after single dose0-Day 5

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half after single dose

Apparent Oral Clearance (CL/F) after single dose0-Day 5

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population pharmacokinetic (PK) modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood after single dose

Apparent Volume of Distribution (Vz/F) after single dose0-Day 5

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.

Maximum Observed Plasma Concentration (Cmax) on Days 1, 7 and 14 after multiple daily dose0-Day 18
Area Under the Curve from Time Zero to end of dosing interval (AUCtau) on days 1,7,14 after multiple daily doses0-Day 18
Time to Reach Maximum Observed Plasma Concentration (Tmax) on days 1,7 14 after multiple daily doses0-Day 18
Plasma Decay Half-Life (t1/2) on day 14 after multiple daily doses0-Day 18

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.

Apparent Volume of Distribution (Vz/F) on day 14 after multiple daily doses0-Day 18

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.

Renal clearance (CLr) on day 140-Day 18
Amount of unchanged drug recovered in urine during the dosing interval (AEtau) on Day 14 after multiple daily doses0-Day 18
Percent of dose recovered unchanged in urine during the dosing interval (AEtau%) on Day 14 after multiple daily doses0-Day 18
Peak to Trough ratio at Steady State (PTR)0-Day 18

Cmax to Cmin ratio at steady state

Trial Locations

Locations (1)

New Haven Clinical Research Unit

🇺🇸

New Haven, Connecticut, United States

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