Drug Interaction, Healthy
Conditions
Brief summary
The primary purpose of this study is to evaluate the pharmacokinetics, safety and tolerability of a single dose of PF-04991532 in healthy adult subjects with and without co-administration of cyclosporine.
Interventions
DRUGPF-04991532 alone
a single dose of 150 mg PF-04991532, fasted
DRUGPF-04991532 + cyclosporine
a single dose of 150 mg PF-04991532 + a single dose of 600 mg cyclosporine, fasted
Sponsors
Pfizer
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male and/or female (non-childbearing potential) subjects between the ages of 18 and 55 years, 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. Women must be of non childbearing potential as defined in Lifestyle Guidelines. Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight \>50 kg (110 lbs). * An informed consent document signed and dated by the subject or a legally acceptable representative. * Subjects who are willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures.
Exclusion criteria
* Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, sychiatric, neurologic, or allergic (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing) disease or clinical findings at Screening. * Subjects with clinically significant infections within the past 3 months (for example, those requiring hospitalization, or as judged by the Investigator), or evidence of any infection within the past 7 days. * Screening supine blood pressure \>=140 mm Hg (systolic) or \>=90 mm Hg (diastolic), on a single measurement \[confirmed by a single repeat, if necessary\] following at least 5 minutes of rest.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Area under the plasma concentration versus time profile (AUC) | predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 36, 48, 72 hrs postdose |
| Max observed plasma concentration (Cmax) | predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 36, 48, 72 hrs postdose |
Secondary
| Measure | Time frame |
|---|---|
| Total amount of unchanged drug excreted in the urine over 24 hours (Ae24) | 0-8, and 8-24hr postdose |
| Time of Cmax (Tmax) | predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 36, 48, 72 hrs postdose |
| Total amount of unchanged drug excreted in the urine over 24 hours, expressed as percent of dose (Ae24(% excreted)) | 0-24hr |
| Renal clearance (CLR) | 0-24hr |
| Terminal elimination half-life (t1/2) | predose, 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24, 36, 48, 72 hrs postdose |
Countries
Belgium
Outcome results
None listed