VT-464

VT-464 is a nonsteroidal antiandrogen (NSAA) which is under development by Innocrin Pharmaceuticals for the treatment of prostate cancer. It is a CYP17A1 inhibitor and by extension a steroidogenesis inhibitor that is structurally related to the approved medication abiraterone acetate, but that, unlike abiraterone acetate, does not increase mineralocorticoid production.

Pharmacology

VT-464 is a lyase-selective CYP17A1 inhibitor, meaning that it selectively inhibits the lyase activity of CYP17A1. This is in contrast to non-selective CYP17A1 inhibitors like abiraterone acetate, which inhibit both the hydroxylase and lyase activities of CYP17A1. As a result of its selectivity for inhibition of CYP17A1 lyase, VT-464 does not increase mineralocorticoid production, and hence, does not require concomitant administration of a glucocorticoid like prednisone to prevent mineralocorticoid excess syndrome.

Clinical trials

As of 2016, VT-464 is in phase II clinical trials for prostate cancer. Preliminary results have been promising, with a high rate of biochemical response and a favorable safety profile.

See also

• List of investigational antiandrogens