The novel drug CS-891 inhibits 5alpha-reductase activity in freshly isolated dermal papilla of human hair follicles.
The local conversion of testosterone (T) to the more potent androgen dihydrotestosterone (DHT) by 5alpha-reductase (5aR) is implicated in the pathogenesis of androgenetic alopecia (AGA). Recently, the clinical effectiveness of finasteride, a selective type II 5aR inhibitor, in treating AGA has been documented, and these clinical studies have shown that circulating DHT is lowered by 60-70% in men taking finasteride. The source of the residual circulating DHT is presumed to be due to type I 5aR activity which is not affected by finasteride. Several novel compounds with potent dual inhibitory activity on both isoenzymes have been described and CS-891 is one of them. This compound may be likewise effective in the prevention or treatment of AGA. As a prerequisite for such an action CS-891 should be able to inhibit 5aR activity in its target tissue: the hair follicles (HF). Here we report on the capability of CS-891 to inhibit 5aR activity in dermal papillae (DP) of human HF.
Niiyama
S
S
Department of Dermatology, Philipp University, Deutschhausstrasse 9, D-35033 Marburg, Germany. niiyama@mailer.uni-marburg.de
Kojima
K
K
Hamada
T
T
Happle
R
R
Hoffmann
R
R
D000328:Adult; D000505:Alopecia / Q000188:drug therapy* / Q000473:pathology; D000736:Androstenes / Q000494:pharmacology*; D042944:Cholestenone 5 alpha-Reductase; D046508:Culture Techniques; D015507:Drugs, Investigational / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005260:Female; D018859:Hair Follicle / Q000187:drug effects*; D006801:Humans; D010088:Oxidoreductases / Q000187:drug effects*; D012016:Reference Values; D012680:Sensitivity and Specificity
D000736:Androstenes; D015507:Drugs, Investigational; D004791:Enzyme Inhibitors; C112526:PNU 157706; D010088:Oxidoreductases; D042944:Cholestenone 5 alpha-Reductase