154229-19-3

溶解度:Unknown

储存条件:-20C 2 years

生物活性

ABIRATERONE(CB-7598), a steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase inhibitor (CYP17), is currently undergoing phase II clinical trials as a potential drug for the treatment of androgen-dependent prostate cancer.In preclinical studies, ABIRATERONE(CB-7598) has demonstrated the ability to selectively inhibit the target enzyme (IC50 4 nM for hydroxylase), resulting in inhibition of testosterone production in both the adrenals and the testes. Clinical studies demonstrated that CYP17 blockade by ABIRATERONE(CB-7598) acetate is safe and has significant antitumor activity in CRPC (castration-resistant prostate cancer).In 2008, enrolment had commenced into a Phase I/II trial of CB7630 (ABIRATERONE acetate) in patients with advanced breast cancer.

参考文献

Potter, G.A.; et al.; Novel steroidal inhibitors of human cytochrome P450(17alpha) (17alpha-hydroxylase-C17,20-lyase): Potential agents for the treatment of prostatic cancer. J Med Chem 1995, 38, 13, 2463.