Clinical trial NCT01981694: A Phase I Trial to Investigate the Safety and Tolerability of PF-06649751
Official title: A Phase 1, Double Blind, Sponsor Open, Randomized, Placebo Controlled, Crossover, Single Oral Dose Escalation Study to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of PF-06649751 in Healthy Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Keywords: Phase 1
Randomized
Double Blind
Placebo-Controlled
Single-Dose Escalation
Safety
Tolerability
PK
PD
PF-06649751
Lead sponsor: Pfizer
Sponsor class: INDUSTRY
First posted: 2013-11-11
Enrollment: 18
Sex: ALL
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: BASIC_SCIENCE

Brief summary: This study will determine the safety and tolerability of PF-06649751 given orally to healthy volunteers. To determine the optimal dose for future studies, the concentration of the drug over time will be determined by periodic blood samples. The rate of eye blinks will be measured as an indicator of PF-06649751 action on the receptors of interest in the brain.


Eligibility criteria: Inclusion Criteria:

* Healthy male and/or female subjects of non-childbearing potential between the ages of 18 and 55 years
* Female subjects of non childbearing potential that meet at least one of the following criteria: Achieved postmenopausal status, defined as: 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 postmenopausal status; Have undergone a documented hysterectomy and/or bilateral oophorectomy; Have medically confirmed ovarian failure.

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).
* Any condition possibly affecting drug absorption.
* Subjects with epilepsy, or history of epilepsy, or conditions that lower seizure threshold, seizures of any etiology (including substance or drug withdrawal), or who have increased risk of seizures as evidenced by history of EEG with epileptiform activity. Subjects with a history of childhood seizures, and history of head trauma with loss of consciousness requiring hospitalization overnight will be excluded as well.

Primary outcomes:
measure: Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
timeFrame: 0, 0.5, 1, 1.5, 2, 4, 6, 8, 10, 12, 16, 24, 32, 48, 72 hours post-dose
measure: Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - 8)]
timeFrame: 0, 0.5, 1, 1.5, 2, 4, 6, 8, 10, 12, 16, 24, 32, 48, 72 hours post-dose
measure: Maximum Observed Plasma Concentration (Cmax)
timeFrame: 0, 0.5, 1, 1.5, 2, 4, 6, 8, 10, 12, 16, 24, 32, 48, 72 hours post-dose
measure: Time to Reach Maximum Observed Plasma Concentration (Tmax)
timeFrame: 0, 0.5, 1, 1.5, 2, 4, 6, 8, 10, 12, 16, 24, 32, 48, 72 hours post-dose
measure: Plasma Decay Half-Life (t1/2)
timeFrame: 0, 0.5, 1, 1.5, 2, 4, 6, 8, 10, 12, 16, 24, 32, 48, 72 hours post-dose
measure: Apparent Oral Clearance (CL/F)
timeFrame: 0, 0.5, 1, 1.5, 2, 4, 6, 8, 10, 12, 16, 24, 32, 48, 72 hours post-dose
measure: Apparent Volume of Distribution (Vz/F)
timeFrame: 0, 0.5, 1, 1.5, 2, 4, 6, 8, 10, 12, 16, 24, 32, 48, 72 hours post-dose
measure: Eye Blink Rate
timeFrame: 0, 0.5, 1, 1.5, 2, 4, 6, 8, 10, 12, 16, 24 hours post-dose
Secondary outcomes:
Other outcomes:
Locations:
city: New Haven
country: United States
facility: Pfizer Investigational Site
state: Connecticut
Study officials:
affiliation: Pfizer
name: Pfizer CT.gov Call Center
role: STUDY_DIRECTOR
References: