The inhibitors of 5 alpha -reductase isoenzymes (1 and 2) can be schematica
lly divided in three groups according they substrate specificity: a) pure o
r preferential inhibitor of 5 alpha -reductase 1; b) pure or preferential i
nhibitor of 5 alpha -reductase 2; c) dual inhibitors. Despite the fact that
several steroidal and non-steroidal inhibitors have been synthesized and e
xperimented in pharmacological models, only finasteride has been extensivel
y used for clinical purposes. The largest application of finasteride in man
has been human benign prostative hyperplasia (BPH). In addition, finasteri
de has been recently used for treatment of male baldness with a 50% of obje
ctive response. In women, finasteride has been used in some control trials
for treatment of hirsutism with an objective favorable response. In conclus
ion, finasteride appears be useful for BPH, baldness and hirsutism (with ca
ution) treatment. On the basis of experimental observations on distribution
of 1 and 2 isoenzymes in human skin, scalp and prostate, the dual inhibito
rs should be more indicated for treatment of BPH and baldness. Similarly, t
he dual inhibitors seem indicated in attempting to prevent prostatic cancer
. The pure 5a-reductase 1 inhibitors seem the ideal drugs for treatment of
acne and hirsutism.