seviteronel

Seviteronel is an orally available, non-steroidal small molecule that acts as a selective inhibitor of the enzyme cytochrome P450 17A1 (CYP17A1), specifically targeting its 17,20 lyase activity. By inhibiting this enzyme in the testes and adrenal glands, seviteronel reduces androgen production, which can decrease androgen-dependent growth signaling and inhibit proliferation of androgen-dependent tumor cells. Seviteronel is approximately tenfold more selective for 17,20 lyase over 17α-hydroxylase compared to other CYP17 inhibitors like abiraterone acetate, resulting in less interference with corticosteroid production and potentially eliminating the need for concomitant glucocorticoid therapy. In addition to its role as an androgen synthesis inhibitor, seviteronel also acts as a competitive antagonist of the androgen receptor (AR), including both wild-type and certain mutated forms. It has demonstrated anti-tumor activity in preclinical models of prostate cancer and breast cancer—including triple-negative breast cancer—and is currently under investigation primarily for castration-resistant prostate cancer (CRPC) and advanced breast cancers[1][2][3][4][5][6].

Other names

seviteronel