Prostate cancer is one of the leading causes of death in men in the U.S. and Europe. Current treatments involving the use of androgen ablation therapy via orchidectomy or chemical castration have had limited success due to their focus only on inhibiting androgens produced by the testes, which comprises 90% of circulating androgens.  Low levels of androgens produced by the adrenals are sufficient to fuel prostate cancer growth, ultimately leading to castration-resistant prostate cancer.  Our approach to addressing this unmet medical need has been to identify and develop a reversible inhibitor of CYP17 lyase, a dual function P450 enzyme expressed in the testes and adrenals, for complete suppression of androgen biosynthesis and with an additional focus on minimal glucocorticoid and mineralcorticoid perturbation.  Herein, we describe the identification of a small molecule inhibitor of CYP17 lyase with specificity over hydroxylase and selectivity against CYP11B1 and CYP21.

CYP17 lyase inhibitors as therapeutic agents for the treatment of prostate cancer

245th National Meeting (2013)

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