Premium
Pharmacodynamics of MK‐0963, a new 5α‐reductase inhibitor: Effects on serum androgen concentrations
Author(s) -
Schwartz Jules I,
Laskin Oscar L,
Meeter Carol A,
Patterson Patricia M,
Schneider Stephen H,
Lasseter Kenneth C,
Seibold James R
Publication year - 1994
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1994.9
Subject(s) - dihydrotestosterone , testosterone (patch) , endocrinology , medicine , pharmacodynamics , androgen , hormone , serum concentration , placebo , clinical pharmacology , pharmacokinetics , pharmacology , chemistry , alternative medicine , pathology
The hormonal effects after a 10‐day administration of a 4‐azasteroid inhibitor of 5α‐reductase, MK‐0963 (previously L‐654,066), were evaluated in 35 healthy male volunteers in an increasing‐dose, five‐panel design. Marked suppression of serum dihydrotestosterone was observed after the once‐daily administration at each active dose level (placebo, 0.1, 0.5, 1.0, 10, and 25 mg). Maximum dihydrotestosterone suppression occurred at doses greater than or equal to 10 mg. The mean percentage (±SE) decreases in dihydrotestosterone at 24 hours after the last dose in the groups treated with the 10 and 25 mg doses were 78% ± 4.9% and 80% ± 2.9%, respectively. The 25 mg dose maintained a dihydrotestosterone suppression of at least 70% for more than 6 days after the last dose. No consistent changes in serum testosterone were noted. This study shows that administration of multiple doses of MK‐0963 results in a substantial suppression of serum dihydrotestosterone with no consistent influence on serum testosterone concentrations. Clinical Pharmacology and Therapeutics (1994) 55, 50–54; doi: 10.1038/clpt.1994.9