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A Phase 1 Study To Evaluate Tolerability, Safety, And Pharmacokinetics Of Topical PF-06263276 In Healthy Subjects

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Placebo
Registration Number
NCT01981681
Lead Sponsor
Pfizer
Brief Summary

PF-06263276 is a first in class inhibitor of the Janus kinase (JAK) enzymes 1, 2, 3 and tyrosine kinase 2 (TYK2) that is being developed for the treatment of chronic plaque psoriasis. The goal of the study is to assess the safety, local tolerability, and pharmacokinetics in healthy subjects.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
47
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.
  • Subjects who are willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures.
  • Subjects willing to avoid tanning beds and sun exposure of the back during the study.
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 application).
  • Subjects with any active skin condition at the application site possibly affecting drug absorption (e.g. rash, sun burn, scars, tattoos).
  • Subjects with a Draize score >0 of the test area (back) immediately prior to first treatment application.
  • Subjects using topical prescription or nonprescription drugs/over the counter preparations on the back within 14 days of the first treatment application.
  • Subjects not willing to avoid application of treatmentssuch as lotions or creams to the back throughout the study until follow-up.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Cohort 1 Experimental ArmPF-06263726-
Cohort 4 Placebo ArmPlacebo-
Cohort 3 Experimental ArmPF-06263726-
Cohort 2 Experimental ArmPF-06263726-
Cohort 3 Placebo ArmPlacebo-
Cohort 4 Experimental ArmPF-06263726-
Primary Outcome Measures
NameTimeMethod
Changes from baseline in 12 lead electrocardiogram (ECG) parameters.Day 23, Day 28

Quantitative changes in ECG intervals.

Incidence and severity of treatment emergent adverse events and withdrawals due to treatment emergent adverse events.Day 23, Day 28
Incidence and magnitude of treatment emergent clinical laboratory abnormalities including hematology, chemistry, fasting glucose, urinalysis.Day 23, Day 28
Draize toxicity assessment score.Day 8, Day 28

Changes from baseline on Draize toxicity assessment score.

Changes from baseline vital signs (blood pressure, pulse rate, oral temperature and respiration rate) and physical examinations.Day 23, Day 28
Secondary Outcome Measures
NameTimeMethod
Cohorts 3 and 4: Maximum Observed Plasma Concentration (Cmax)Day 1, Day 14
Cohorts 3 and 4: Dose-Normalized Maximum Observed Plasma Concentration [Cmax (dn)]Day 1, Day 14
Cohorts 3 and 4: Time to Reach Maximum Observed Plasma Concentration (Tmax)Day 1, Day 14
Cohorts 3 and 4: Apparent Oral Clearance (CL/F)Day 14

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.

Cohorts 3 and 4: Area Under the Curve From Time Zero to 12 hours [AUC (0-12)]Day 1, Day 14

AUC (0-t)= Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t)

Cohorts 3 and 4: Dose-Normalized Area Under the Curve From Time Zero to 12 hours [AUC (0-12)]Day 1, Day 14

AUC (0-t)= Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t)

Cohorts 3 and 4: Plasma Decay Half-Life (t1/2)Day 14

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

Cohorts 3 and 4: Apparent Volume of Distribution (Vz/F)Day 14

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.

Trial Locations

Locations (1)

Pfizer Investigational Site

🇧🇪

Brussels, Belgium

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