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

A Phase 1, Randomized, Double Blind, Sponsor Open, Placebo Controlled, Single Dose Escalating Study To Assess The Safety, Tolerability And Pharmacokinetics Of PF-06282999 Administered Orally In Healthy Adult Subjects

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: PF-06282999; Drug: Placebo; Drug: PF-06282999; Drug: Placebo; Drug: PF-06282999; Drug: PF-06282999; Drug: PF-06282999

• Study Type: Interventional
• Enrollment (Actual): 42
• Phase: Phase 1

Contacts and Locations

Study Locations

• Belgium
  • Bruxelles, Belgium, B-1070
    • Pfizer Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: Double

Number of Arms

5

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Cohort 1	Drug: PF-06282999; Solution, doses range from 20 to 200 mg, single dose; Drug: Placebo; Solution, single dose; Drug: PF-06282999; Methylcellulose suspension, doses range 125 to 500 mg, single dose; Drug: Placebo; suspension, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, doses range 200 to 500 mg, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, 500 mg dose, single dose; Drug: PF-06282999; Simethicone or methylcellulose suspension, up to 1500 mg, single dose
Experimental: Cohort 2	Drug: PF-06282999; Solution, doses range from 20 to 200 mg, single dose; Drug: Placebo; Solution, single dose; Drug: PF-06282999; Methylcellulose suspension, doses range 125 to 500 mg, single dose; Drug: Placebo; suspension, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, doses range 200 to 500 mg, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, 500 mg dose, single dose; Drug: PF-06282999; Simethicone or methylcellulose suspension, up to 1500 mg, single dose
Experimental: Cohort 3	Drug: PF-06282999; Solution, doses range from 20 to 200 mg, single dose; Drug: Placebo; Solution, single dose; Drug: PF-06282999; Methylcellulose suspension, doses range 125 to 500 mg, single dose; Drug: Placebo; suspension, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, doses range 200 to 500 mg, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, 500 mg dose, single dose; Drug: PF-06282999; Simethicone or methylcellulose suspension, up to 1500 mg, single dose
Experimental: Cohort 4	Drug: PF-06282999; Solution, doses range from 20 to 200 mg, single dose; Drug: Placebo; Solution, single dose; Drug: PF-06282999; Methylcellulose suspension, doses range 125 to 500 mg, single dose; Drug: Placebo; suspension, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, doses range 200 to 500 mg, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, 500 mg dose, single dose; Drug: PF-06282999; Simethicone or methylcellulose suspension, up to 1500 mg, single dose
Experimental: Cohort 5	Drug: PF-06282999; Solution, doses range from 20 to 200 mg, single dose; Drug: Placebo; Solution, single dose; Drug: PF-06282999; Methylcellulose suspension, doses range 125 to 500 mg, single dose; Drug: Placebo; suspension, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, doses range 200 to 500 mg, single dose; Drug: PF-06282999; Methylcellulose or simethicone suspension, 500 mg dose, single dose; Drug: PF-06282999; Simethicone or methylcellulose suspension, up to 1500 mg, single dose

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
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 temperature	0, 1, 2, 4, 8, 12,16, 24, 48 hours post-dose

Collaborators and Investigators

• Sponsor: Pfizer

Publications and helpful links

Helpful Links

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

Study record dates

Study Major Dates

• Study Start: June 1, 2012
• Primary Completion (Actual): March 1, 2013
• Study Completion (Actual): March 1, 2013

Study Registration Dates

• First Submitted: May 30, 2012
• First Submitted That Met QC Criteria: June 20, 2012
• First Posted (Estimate): June 25, 2012

Study Record Updates

• Last Update Posted (Estimate): March 13, 2013
• Last Update Submitted That Met QC Criteria: March 12, 2013
• Last Verified: March 1, 2013

More Information

Terms related to this study

• Keywords: tolerability; safety; pharmacokinetics; healthy subjects; oral; single ascending dose; placebo-controlled
• Other Study ID Numbers: B5211001