Disease relevance of CB 7598

• Abiraterone is an oral, selective, steroidal inhibitor of cytochrome P450(17alpha) being developed by Cougar Biotechnology Inc for the potential treatment of prostate cancer [1].
• Chen and colleagues report that a T878A androgen receptor mutation occurs in a subset of patients progressing while receiving abiraterone, suggesting that this may be a therapeutically exploitable mechanism of abiraterone resistance in castration-resistant prostate cancer [2].

High impact information on CB 7598

• Abiraterone (17-(3-pyridyl)androsta-5,16-dien-3beta-ol, 1) is a potent inhibitor (IC50 4 nM for hydroxylase) of human cytochrome P45017alpha [3].
• Abiraterone. Cougar Biotechnology [1].
• This method will be applied to a clinical trial investigating the pharmacokinetics of abiraterone acetate and abiraterone in patients with prostate cancer [4].
• A validated liquid chromatographic-tandem mass spectroscopy method for the quantification of abiraterone acetate and abiraterone in human plasma [4].

Associations of CB 7598 with other chemical compounds

• The T878A mutation appeared to be less common in the subset of patients with CRPC treated with abiraterone plus dutasteride, and transfection studies showed that dutasteride was a more potent direct antagonist of the T878A versus the wild-type AR [5].

Analytical, diagnostic and therapeutic context of CB 7598

• Phase I clinical trials of abiraterone have been conducted and the design of phase I/II clinical trials is being finalized [1].

References