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First In Human Study Of Increasing Oral Doses Of PF-04634817

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT01098877
Lead Sponsor
Pfizer
Brief Summary

The study will evaluate the hypothesis that at doses and plasma concentrations which affect pharmacodynamic markers of activity at the chemokine receptors, CCR2 and CCR5, the compound is safe and well tolerated. It will also evaluate the hypothesis that the pharmacokinetic profile is robust and consistent with a once or twice a day therapeutic administration.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
27
Inclusion Criteria
  • Healthy male or female (of non-child bearing potential) subjects between 18 and 55 years of age.
  • Body mass index of 17.5 to 30.5 kg/m2 and total body weight > 50kg.
Exclusion Criteria
  • Evidence or history of any clinically significant disease.
  • Treatment with an investigational drug within 30 days of study start
  • Use of prescription and non-prescription medicines within 7 days of study start

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
PlaceboPF-04634817 Placebo-
Cohort 3, placebo (fed)PF-04634817 Placebo-
Cohort 3, 600mgPF-04634817-
Cohort 2, 100mgPF-04634817-
Cohort 1, 3mgPF-04634817-
Cohort 1, 1mgPF-04634817-
Cohort 1, 10mgPF-04634817-
Cohort 2, 30mgPF-04634817-
Cohort 2, 300mgPF-04634817-
Cohort 3, up to 900mg (fed)PF-04634817-
Cohort 3, 900mgPF-04634817-
Primary Outcome Measures
NameTimeMethod
Safety and toleration: adverse events, supine and standing vital sign measurements, telemetry, 12-lead ECGs, blood and urine tests0-3 days
Plasma pharmacokinetics: Cmax, Tmax, AUClast, AUCinf, AUC0-24, CL/F, Vz/F and T1/20-4 days
Urinary pharmacokinetics: Aet (mount excreted in urine), Aet% and CLr0-2 days
p-ERK inhibition in human monocytes0-3 days
Change in circulating monocytes0-3 days
Secondary Outcome Measures
NameTimeMethod
Change from baseline in plasma MCP-10-3 days
MIP 1B stimulated CCR5 receptor internalization0-3 days
MCP-1 stimulated CCR5 receptor internalization0-3 days

Trial Locations

Locations (1)

Pfizer Investigational Site

🇺🇸

New Haven, Connecticut, United States

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