Prostate cancer growth requires the male androgen testosterone. When testosterone, or its metabolite dihydrotestosterone, binds to its natural receptor, the androgen receptor moves into the nucleus of the prostate cancer cell (nuclear translocation), binds DNA and stimulates prostate cancer growth. MDV3100, an oral androgen receptor signaling inhibitor (ARSI) has been shown in preclinical studies to provide more complete suppression of the androgen receptor pathway than bicalutamide, the most commonly used anti-androgen.

MDV3100 slows growth and induces cell death in bicalutamide-resistant cancers via three complementary actions – MDV3100 competitively inhibits androgen (eg, testosterone) binding to the androgen receptor, inhibits nuclear translocation, and binding to DNA. Preclinical data published in Science demonstrated that MDV3100 is superior to bicalutamide in each of these three actions. Click here for Science article.

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