This single and multiple ascending dose study is the first evaluation of PF-0626414, a Selective Androgen Receptor Modulator in humans. The goal is to assess the safety, tolerability, pharmacokinetics and pharmacodynamics in healthy western and Japanese male subjects .
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
DOUBLE
Enrollment
72
Subjects will receive single doses of 1,3,6,30,100,200, 400 mg of PF-06260414 (solution) in a dose escalating format
Subjects will receive single doses of PF-06260414 matching placebo (solution) in a dose escalation format
Subjects will receive PF-06260414 doses (solution) twice daily for 14 days
New Haven Clinical Research Unit
New Haven, Connecticut, United States
Changes from baseline vital signs (blood pressure, pulse rate, oral temperature and respiration rate)
Time frame: 6 weeks
Changes from baseline in 12-lead ECG parameters
Quantitative changes in ECG intervals
Time frame: 6 weeks
Incidence and severity of treatment emergent adverse events and withdrawals due to treatment emergent adverse events
Time frame: 6 weeks
Incidence and magnitude of treatment emergent clinical laboratory abnormalities including hematology (including total Hb and hematocrit), chemistry, fasting glucose, urinalysis
Time frame: 6 weeks
24 hour creatinine clearance (baseline and day 14).
Time frame: Baseline, Day 14
Changes from baseline in total testosterone, free testosterone, estradiol, LH, FSH, SHBG.
Time frame: 6 weeks
Changes from baseline in Prostate Specific Antigen (PSA).
Time frame: 6 weeks
Changes from baseline in total cholesterol, HDL cholesterol, LDL cholesterol, triglycerides.
Time frame: 6 weeks
Single Dose: Cmax, Tmax, AUClast, AUCinf, CL/F, Vz/F, and t½,Cmax(dn), AUCinf(dn), AUClast(dn), t½.
Time frame: 6 weeks
Multiple Dose: Cmax, Tmax Ctrough, C,av,AUC,CL/F, Vz/F, Rac , Rac,Cmax , PTR, Cmax(dn),AUCτ(dn), t½.
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Subjects will receive PF-06260414 matching placebo doses (solution) of 3, 10, 30, 100mg BID and 60 mg QD for 14 days
Japanese subjects may receive the highest dose of PF-06460414 tested in non Japanese cohort twice daily for 14 days
Japanese subjects may receive PF-06260414 matching placebo doses (solution) twice daily for 14 days
Time frame: 6 weeks
Urinary Pharmacokinetics: Amount of PF 06260414 excreted unchanged (AE and AE%), renal clearance (CLr).
Time frame: 6 weeks
Single Dose: AUC(hormone or PSA), C0(hormone or PSA), Maximum PCB, Cmax(hormone or PSA), Cmin(hormone or PSA), Tmax(hormone or PSA), Tmin(hormone or PSA).
The effects of PF- 06260414 on sex hormones (total testosterone, free testosterone, estradiol, SHBG, LH and FSH) will be evaluated according to the scheduled timepoints in single ascending dose study
Time frame: 6 weeks
Multiple Dose: AUC(hormone or PSA), C0(hormone or PSA), Cmax(hormone or PSA), Cmin(hormone or PSA), Tmax(hormone or PSA), Tmin(hormone or PSA).
Time frame: 6 weeks