Investigation Of The Metabolism, And Excretion Of [14c]-PF-05212384 In Healthy Male Volunteers

A Phase One, Open-Label Single-Radiolabeled Dose Study To Investigate The Metabolism, And Excretion Of [14c]-PF-05212384 In Healthy Male Volunteers

The purpose of the study is to characterize how PF-05212384 is metabolized in the body following a single intravenous dose of radioactively labeled drug ([14C]-PF-05212384).

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: PF-05212384

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • Nottingham
    • Ruddington Fields, Nottingham, United Kingdom, NG11 6JS
      • Pfizer Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 30 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy male subjects between the ages of 30- 65 years vasectomised or >40 with no desire to father children in the near future (12 months), 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).
• Body Mass Index (BMI) of 17.5 to 35 kg/m2; and a total body weight >50 kg (110 lbs).
• Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study.
• Subjects who are willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures.
• Subjects agree to use an adequate method of contraception

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).
• A positive urine drug screen or history of drug or alcohol abuse in the past 2 years.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: [14C] PF 05212384; Receive PF-05212384 89 mg Dose	Drug: PF-05212384; Single 89 mg Dose via 30 minute IV infusion

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Maximum Observed Plasma Concentration (Cmax)	0.5 hours
Time to Reach Maximum Observed Plasma Concentration (Tmax)	0.5 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)	Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast)	9 Days
Area under the Concentration-Time Curve (AUC)	AUC is a measure of the serum concentration of the drug over time. It is used to characterize drug absorption.	9 days
Plasma Decay Half-Life (t1/2)	Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.	9 days
Systemic Clearance (CL)	CL is a quantitative measure of the rate at which a drug substance is removed from the body.	9 days
Volume of Distribution at Steady State (Vss)	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 blood concentration of a drug. Steady state volume of distribution (Vss) is the apparent volume of distribution at steady-state.	9 days

Collaborators and Investigators

• Sponsor: Pfizer

Publications and helpful links

General Publications

• Houk BE, Alvey CW, Visswanathan R, Kirkovsky L, Matschke KT, Kimoto E, Ryder T, Obach RS, Durairaj C. Distribution, Metabolism, and Excretion of Gedatolisib in Healthy Male Volunteers After a Single Intravenous Infusion. Clin Pharmacol Drug Dev. 2019 Jan;8(1):22-31. doi: 10.1002/cpdd.615. Epub 2018 Sep 26.

Helpful Links

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

Study record dates

Study Major Dates

• Study Start: July 1, 2014
• Primary Completion (Actual): August 1, 2014
• Study Completion (Actual): August 1, 2014

Study Registration Dates

• First Submitted: May 13, 2014
• First Submitted That Met QC Criteria: May 16, 2014
• First Posted (Estimate): May 20, 2014

Study Record Updates

• Last Update Posted (Estimate): September 4, 2014
• Last Update Submitted That Met QC Criteria: September 2, 2014
• Last Verified: September 1, 2014

More Information

Terms related to this study

• Keywords: Healthy Volunteers
• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Protein Kinase Inhibitors; Gedatolisib
• Other Study ID Numbers: B2151006