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Completed

NCT Number: NCT01914796

A Phase I Trial to Investigate the Safety and Tolerability of PF-06412562

This study will determine the safety and tolerability of PF-06412562 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-06412562 action on the receptors of interest in the brain.

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Key information

Conditions

Healthy

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Pfizer Investigational Site

New Haven, Connecticut, 06511, United States

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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 .

Treatment and study plan

PF-06412562

Drug

Single doses, given by oral solution, starting at 0.5 mg up to a possible maximum of 150 mg. The subject will have been fasted for 10 hours prior to the single dose. Two doses, 120 mg and 150 mg, will be split into 3 doses such that the total dose is given over 8 hours (i.e. t = 0, 4, and 8 hours). For each dosing period, 2 subjects will be given a placebo as a comparator. One dose will be given in the fed state.

Primary outcomes

  1. Plasma Decay Half-Life (t1/2)

    Time frame: 0, 0.5, 1, 1.5, 2, 4, 5, 6, 8, 9, 10, 12, 16, 24, 32 hours post-dose

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

  2. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)

    Time frame: 0, 0.5, 1, 1.5, 2, 4, 5, 6, 8, 9, 10, 12, 16, 24, 32 hours post-dose

    Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast)

  3. Maximum Observed Plasma Concentration (Cmax)

    Time frame: 0, 0.5, 1, 1.5, 2, 4, 5, 6, 8, 9, 10, 12, 16, 24, 32 hours post-dose

  4. Area Under the Curve From Time Zero to Extrapolated Infinite Time

    Time frame: 0, 0.5, 1, 1.5, 2, 4, 5, 6, 8, 9, 10, 12, 16, 24, 32 hours post-dose

    AUC = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time. It is obtained from AUC (0 - t) plus AUC (t - 8).

  5. Apparent Oral Clearance (CL/F)

    Time frame: 0, 0.5, 1, 1.5, 2, 4, 5, 6, 8, 9, 10, 12, 16, 24, 32 hours post-dose

    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.

  6. Apparent Volume of Distribution (Vz/F)

    Time frame: 0, 0.5, 1, 1.5, 2, 4, 5, 6, 8, 9, 10, 12, 16, 24, 32 hours post-dose

    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.

  7. Measurement of Cognitive Decline by Means of a Computerized Battery of Neuropsychologic Tests

    Time frame: 0, 1, 4, 8, 12 hours post-dose

    Change from baseline cognitive performance

  8. Eye Blink Rate

    Time frame: 0, 1, 2, 4 and 8 hours

    Measurement of eye blink rate for a given dose at time of predicted maximum blood concentration of the compound.

  9. Area Under the Curve From Time Zero to 24 hours

    Time frame: 0, 0.5, 1, 1.5, 2, 4, 5, 6, 8, 9, 10, 12, 16, 24 hours post-dose

    Area under the plasma concentration time-curve from zero to 24 hours

Sponsors and collaborators

Lead sponsor

Pfizer

Industry

Registry information

Official study 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-06412562 In Healthy Subjects

Important dates

Study start
2013
Primary completion
2013
Study completion
2013
First posted
Aug 2, 2013
Registry last updated
May 23, 2014

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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