Healthy
Conditions
Keywords
safety, tolerability, pharmacokinetics, oral, single ascending dose, placebo-controlled, healthy subjects
Brief summary
This is the first-in-human study for an oral investigational compound, PF-06282999, in order to assess its safety, tolerability and pharmacokinetics in humans across a wide range of dose levels.
Interventions
DRUGPF-06282999
Solution, doses range from 20 to 200 mg, single dose
DRUGPlacebo
Solution, single dose
Sponsors
Pfizer
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
DOUBLE (Subject, Investigator)
Eligibility
Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male and/or female 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. * Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight \>50 kg (110 lbs).
Exclusion criteria
* Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including clinically significant drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing). * Use of prescription or nonprescription drugs and dietary supplements within 7 days or 5 half-lives (whichever is longer) prior to the first dose of study medication. Herbal supplements and hormone replacement therapy must be discontinued 28 days prior to the first dose of study medication. As an exception, acetaminophen/paracetamol may be used at doses of ≤1 g/day. Limited use of non-prescription medications that are not believed to affect subject safety or the overall results of the study may be permitted on a case-by-case basis following approval by the sponsor.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUCinf] | 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose |
| Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) | 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose |
| Area Under the Curve From Time Zero to 24 hour [AUC24] | 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24 hours post-dose |
| Maximum Observed Plasma Concentration (Cmax) | 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose |
| Time to Reach Maximum Observed Plasma Concentration (Tmax) | 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose |
| Apparent Oral Clearance (CL/F) | 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose |
| Plasma Decay Half-Life (t1/2) | 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose |
| Apparent Volume of Distribution (Vz/F) | 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 hours post-dose |
| Amount of Unchanged Drug Excretion in Urine from Zero to 24 hours (Ae24) | 0 to 24 hours post-dose |
| Percent of Dose Excreted in Urine as Unchanged Drug from Zero to 24 hours (Ae24%) | 0 to 24 hours post-dose |
| Renal Clearance (CLr) | 0 to 24 hours post-dose |
| Oral temperature | 0, 1, 2, 4, 8, 12,16, 24, 48 hours post-dose |
Countries
Belgium
Outcome results
None listed