CGP-53153

CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC₅₀s of 36 and 262 nM in rat and human prostatic tissue, respectively. IC50 & Target: IC50: 36 nM (rat 5 alpha reductase), 262 nM (human 5 alpha reductase)^[1] In Vitro: CGP-53153 competitively inhibits rat microsomal 5 alpha reductase from prostate with an IC₅₀ of 36 nM compared to the reference compound finasteride (IC₅₀=11 nM). CGP 53153 is approximately one order of magnitude more potent in inhibiting rat compared to human 5 alpha reductase, with IC₅₀ values of 36 and 262 nM, respectively In Vivo: CGP-53153 can significantly reduce T-propionate-mediated prostate growth at oral doses of 0.01 mg/kg. CGP-53153 significantly reduces prostate weight at 3 and 10 mg/kg by 31% and 37%, respectively. Treatment for 12 weeks with both CGP-53153 reduces prostate volume by more than 70% in individual dogs. Neither body weight nor the weight of any organ tested is affected by CGP-53153^[1].