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A Study To Assess The Safety, Tolerability And Pharmacokinetics Of PF-06282999 Administered Orally In Healthy Adult Subjects

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Placebo
Registration Number
NCT01626976
Lead Sponsor
Pfizer
Brief Summary

This is the first-in-human study for an oral investigational compound, PF-06282999, in order to assess its safety, tolerability and pharmacokinetics in humans across a wide range of dose levels.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
42
Inclusion Criteria
  • Healthy male and/or female subjects 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).
  • Women must be of non-childbearing potential.
  • Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).
Exclusion Criteria
  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including clinically significant drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
  • Use of prescription or nonprescription drugs and dietary supplements within 7 days or 5 half-lives (whichever is longer) prior to the first dose of study medication. Herbal supplements and hormone replacement therapy must be discontinued 28 days prior to the first dose of study medication. As an exception, acetaminophen/paracetamol may be used at doses of ≤1 g/day. Limited use of non-prescription medications that are not believed to affect subject safety or the overall results of the study may be permitted on a case-by-case basis following approval by the sponsor.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Cohort 2Placebo-
Cohort 3PF-06282999-
Cohort 3Placebo-
Cohort 4PF-06282999-
Cohort 4Placebo-
Cohort 5PF-06282999-
Cohort 1PF-06282999-
Cohort 1Placebo-
Cohort 2PF-06282999-
Cohort 5Placebo-
Primary Outcome Measures
NameTimeMethod
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUCinf]0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose
Area Under the Curve From Time Zero to 24 hour [AUC24]0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24 hours post-dose
Maximum Observed Plasma Concentration (Cmax)0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose
Time to Reach Maximum Observed Plasma Concentration (Tmax)0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose
Apparent Oral Clearance (CL/F)0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose
Plasma Decay Half-Life (t1/2)0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose
Apparent Volume of Distribution (Vz/F)0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose
Amount of Unchanged Drug Excretion in Urine from Zero to 24 hours (Ae24)0 to 24 hours post-dose
Percent of Dose Excreted in Urine as Unchanged Drug from Zero to 24 hours (Ae24%)0 to 24 hours post-dose
Renal Clearance (CLr)0 to 24 hours post-dose
Oral temperature0, 1, 2, 4, 8, 12,16, 24, 48 hours post-dose
Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (1)

Pfizer Investigational Site

🇧🇪

Bruxelles, Belgium

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