タイトルまたは説明

Biological Activity:
ABIRATERONE(CB****8), a steroidal cytochrome P**0 *7alpha-hydroxylase**7,**-lyase inhibitor (CYP*7), is currently undergoing phase II clinical trials as a potential drug for the treatment of androgen-dependent prostate cancer.In preclinical studies, ABIRATERONE(CB****8) has demonstrated the ability to selectively inhibit the target enzyme (IC*0 4 nM for hydroxylase), resulting in inhibition of testosterone production in both the adrenals and the testes. Clinical studies demonstrated that CYP*7 blockade by ABIRATERONE(CB****8) acetate is safe and has significant antitumor activity in CRPC (castration-resistant prostate cancer).In ***8, enrolment had commenced into a Phase I/II trial of CB***0 (ABIRATERONE acetate) in patients with advanced breast cancer.

References:
Potter, G.A.; et al.; Novel steroidal inhibitors of human cytochrome P**0(*7alpha) (*7alpha-hydroxylase-C*7,**-lyase): Potential agents for the treatment of prostatic cancer. J Med Chem ***5, *8, *3, ***3.