Healthy
Conditions
Keywords
hyperlipidemia, positron emission tomography
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.
Interventions
DRUG[11C]PF-06427878
Single administration via intravenous infusion of 20 ug \[11C\]PF-06427878 on Day 1 of all 3 Periods
DRUGPF-06427878 10 mg
Single oral administration of 10 mg PF-06427878 on Day 1 of Period 2 or 3, at approximately 2.5 hours prior to \[11C\]PF-06427878 administration
DRUGPF-06427878 600 mg
Single oral administration of 600 mg PF-06427878 on Day 1 of Period 2 or 3, at approximately 2.5 hours prior to \[11C\]PF-06427878 administration
Sponsors
Pfizer
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
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
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| 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
| Measure | Time frame | Description |
|---|---|---|
| % 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: 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 | — |
| 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: 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 | — |
| 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 |
| 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 | — |
| 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 | — |
| Plasma PK of PF-06427878: Tmax, 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 gall bladder, if this region is identifiable | All Periods;Day 1;0-2hr | — |
Countries
United States
Outcome results
None listed