A Study Testing A Radioactive Compound Given Through A Vein With And Without The Non-Radioactive Compound, Given By Mouth, To Characterize Tissue Distribution Using Positron Emission Tomography Scanning

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: PF-06427878 10 mg; Drug: [11C]PF-06427878; Drug: PF-06427878 600 mg

• Registration Number: NCT02410525
• Lead Sponsor: Pfizer

Brief Summary

In this study, radioactive PF-06427878 will be administered, through a vein, alone and with 2 different oral doses of non-radioactive PF-06427878 to healthy, adult, male subjects. Positron emission tomography will be used to characterize tissue distribution. The study will also characterize how the study drug behaves in the body, its safety, and how the body tolerates it.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2015-04-02
• Study First Submitted QC: 2015-04-02
• Study First Posted: 2015-04-07
• Study Start: 2015-05
• Primary Completion: 2015-09
• Study Completion: 2015-09
• Status Verified: 2015-10
• Last Update Submitted: 2015-10-27
• Last Update Posted: 2015-10-29

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 8

Inclusion Criteria

• healthy males
• body mass index 17.5-30.5 kg/m2 ; body weight >50 kg
• signed and dated informed consent document
• willing and able to comply with study requirements

Exclusion Criteria

• tobacco/nicotine containing products > equivalent of 5 cigarettes per day
• history of cumulative ionizing radiation exposure in the past year, including anticipated exposure in this study, and subjects with current, past or anticipated exposure to radiation in the workplace
• severe claustrophobia
• unable to lie still for the required period to acquire images

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
PF-06427878 10 mg	PF-06427878 10 mg	Single oral dose of 10 mg PF-06427878 in Period 2 or 3 to investigate the liver and plasma radioactivity, radioactivity in organs relative to plasma, pharmacokinetics, and safety and tolerability
[11C]PF-06427878	[11C]PF-06427878	Single intravenous infusion of \[11C\]PF-06427878 in Periods 1, 2 and 3 to investigate the liver and plasma radioactivity, radioactivity in organs relative to plasma, pharmacokinetics, and safety and tolerability
PF-06427878 600 mg	PF-06427878 600 mg	Single oral dose of 600 mg PF-06427878 in Period 2 or 3 to investigate the liver and plasma radioactivity, radioactivity in organs relative to plasma, pharmacokinetics, and safety and tolerability

Primary Outcome Measures

Name	Time	Method
Percent injected radioactivity (per gram) over time in the liver	All Periods;Day 1;0-120min
Percent injected radioactivity (per gram) over time in the plasma	All Periods;Day 1;0hr,1,2,3,4,5,5.5,6,6.5,7,8,9,10,12,15,20,25,30,40,50,60,75,90,105,120min

Secondary Outcome Measures

Name	Time	Method
Relative radioactivity in liver versus plasma	All Periods;Day 1;0hr,1,2,3,4,5,5.5,6,6.5,7,8,9,10,12,15,20,25,30,40,50,60,75,90,105,120min	Ratio of AUC of percent injected radioactivity (per gram) over time in liver to AUC of percent injected radioactivity (per gram) over time in plasma
Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the gall bladder, if this region is identifiable	All Periods;Day 1;0-2hr
Plasma PK of PF-06427878: AUClast, as data permit	Period 1;Day 1;0,3,5,15,30,60,90,120,135min
Plasma PK of PF-06427878: AUClast, as data permit.	Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min
Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the biliary tree, if this region is identifiable	All Periods;Day 1;0-2hr
Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the abdominal fat, if this region is identifiable	All Periods;Day 1;0-2hr
Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the kidney, if this region is identifiable	All Periods;Day 1;0-2hr
% of parent in plasma over time	All Periods;Day 1;0hr,1,2,3,4,5,5.5,6,6.5,7,8,9,10,12,15,20,25,30,40,50,60,75,90,105,120min	Parent is study drug PF-06427878
Plasma PK of PF-06427878: AUCinf, as data permit	Period 1;Day 1;0,3,5,15,30,60,90,120,135min
Plasma PK of PF-06427878: Cmax, as data permit	Period 1;Day 1;0,3,5,15,30,60,90,120,135min
Plasma PK of PF-06427878: Tmax, as data permit	Period 1;Day 1;0,3,5,15,30,60,90,120,135min
Plasma PK of PF-06427878: t½, as data permit	Period 1;Day 1;0,3,5,15,30,60,90,120,135min
Plasma PK of PF-06427878: CL, as data permit	Period 1;Day 1;0,3,5,15,30,60,90,120,135min
Plasma PK of PF-06427878: Vss, as data permit	Period 1;Day 1;0,3,5,15,30,60,90,120,135min
Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the urinary bladder, if this region is identifiable	All Periods;Day 1;0-2hr
Time-course of total radioactivity as percentage of injected radioactivity (per gram) in the thigh muscle, if this region is identifiable	All Periods;Day 1;0-2hr
Plasma PK of PF-06427878: Vss, as data permit.	Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min
Plasma PK of PF-06427878: AUCinf, as data permit.	Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min
Plasma PK of PF-06427878: Cmax, as data permit.	Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min
Plasma PK of PF-06427878: Tmax, as data permit.	Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min
Plasma PK of PF-06427878: t½, as data permit.	Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min
Plasma PK of PF-06427878: CL/F, as data permit.	Periods 2 & 3;Day 1;prebreakfast,-90,-60,0,120min

Trial Locations

Locations (3)

New Haven Clinical Research Unit; 🇺🇸 New Haven, Connecticut, United States

Anylan Center; 🇺🇸 New Haven, Connecticut, United States

Yale University School of Medicine; 🇺🇸 New Haven, Connecticut, United States