orteronel

Orteronel is a nonsteroidal, orally bioavailable small molecule that acts as a selective inhibitor of the enzyme CYP17A1, specifically targeting its 17,20-lyase activity with weak inhibition of its 17α-hydroxylase activity. By inhibiting CYP17A1, orteronel suppresses the synthesis of androgens such as testosterone and dehydroepiandrosterone sulfate (DHEA-s), which are implicated in the progression of prostate cancer. This selectivity was designed to reduce androgen production while minimizing effects on cortisol synthesis, potentially lowering the risk of mineralocorticoid-related side effects compared to less selective inhibitors. Orteronel was developed primarily for metastatic hormone-sensitive and castration-resistant prostate cancer but did not demonstrate an overall survival benefit in phase III trials; as a result, its development was discontinued[2][3][5][9].

Other names

orteronel