Inhibition of Testosterone Metabolism in the Human Prostate+

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Abstract
The conversion of 14C-testosterone (T) to 5α-dihydrotestosterone (DHT) and androstanediol (A-diol) was studied in vitro using a crude homogenate of prostate from patients with benign prostatic hypertrophy. Under standard conditions, the mean conversion to DHT was 70 ± 1 (se)% and to A-diol 14 ± 1 (se)% Addition of various antiandrogens and other substances decreased the T → DHT conversion to 0–55% and the T → A-diol to 0–10%. The most potent inhibitors were desoxycorticosterone and progesterone. Estradiol-17β, cyproterone acetate, medrogestone, medroxyprogesterone acetate, estriol and 4′-nitro-3′-trifluoromethylisobutyramilide were also effective inhibitors. To determine whether this effect might be significant in vivo, similar conversion studies were carried out on prostatic tissue obtained from 3 patients who had received oral medrogestone for 1 to 2 weeks. T → DHT was reduced to 12.2 ± 2.8 (se)% and T → A-diol to 6.5 ± 1.0 (se)%. The ability of such compounds to inhibit DHT formation represents one mode of action which may account at least in part for their efficacy in the treatment of benign prostatic hypertrophy.

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