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| Description | Finasteride is a potent, reversible inhibitor of the rat type 1 5 alpha-reductase with Ki of 10.2 nM, used in the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB). | ||
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| In vitro | Finasteride binds to the type 2 isozyme-NADPH complex to form a ternary complex with Ki of 1.19 nM, which then rearranges to a high affinity complex (E:I) with a pseudo first order rate constant of 1.62 ms. [1] Finasteride dose-dependently inhibits the growth rate of the LnCap cell line. [2] Finasteride markedly inhibits prostate-specific antigen (PSA) secretion and expression in LNCaP cells. [3] | ||
| In vivo | Finasteride induces dosage-related incidences of hypospadias (penischisis) in male offspring with a threshold dosage level near 0.1 mg/kg/day and a 100% effect level of 100 mg/kg/day in male rats. Finasteride also causes decreased anogenital distance in male offspring in male rats. [4] Finasteride and castration decreases prostate weight at day 21 by 65% and 93%, respectively, in rats. Finasteride has no significant effect on DNA content after 4 days and decreases DNA content by a maximum of 52% at 14 days in rats. Finasteride causes a less intense increase in staining in which 16% of epithelial cells stained for tissue transglutaminase on day 9 with a return to baseline by day 14 in rats. Finasteride-induced staining is less intense with peak staining at day 4 (0.7% of epithelial cells) and a return to control values by day 9 in rats. [5] |
| Quantity | 5 G, 1 G |
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