Pharmacodynamics and tolerability of L-654,066, a steroid 5α-reductase inhibitor, in men

Autor: Depré, Marleen, Meeter, Carol, Van Hecken, Anne, Laskin, Oscar L, Buntinx, Agnes, De Schepper, Paul J
Zdroj: Clinical Pharmacology & Therapeutics; October 1992, Vol. 52 Issue: 4 p409-412, 4p
Abstrakt: A four-period, two-panel single rising-dose study (0.1 to 100 mg) was conducted in healthy men to investigate the pharmacodynamics and tolerability of L-654,066, a steroid 5α-reductase inhibitor. Within each panel, six subjects received L-654,066 and two subjects received placebo at each dose level; the placebo subjects changed between periods so that each subject received placebo once. Testosterone and dihydrotestosterone were measured in serum at 0, 4, 24, and 48 hours after each treatment. L-654,066 was associated with a significant reduction in serum dihydrotestosterone concentrations, which was maximal at 48 hours after dose. Forty-eight hours after treatment, mean percentage of inhibition was 24% and 39% for the 0.1 and 0.5 mg doses, respectively, and ranged from 50% to 65% at doses from 1 to 25 mg and from 70% to 75% at doses from 50 to 100 mg. Testosterone serum levels did not show any significant difference between the various treatments, including placebo.Clinical Pharmacology and Therapeutics (1992) 52, 409–412; doi:10.1038/clpt.1992.163
Databáze: Supplemental Index