Two compounds induce tumor regression in mouse models
Chris Tran, from Memorial Sloan-Kettering Cancer Center in New York City, and colleagues screened for non-steroidal anti-androgens that bound to androgen receptors with high sensitivity and specificity, particularly in cells expressing high levels of androgen receptor, a hallmark of castration-resistant prostate cancer. The researchers identified the diarylthiohydantoins RD162 and MDV3100, which had a higher affinity for androgen receptors than the clinically used anti-androgen bicalutamide and blocked the downstream effects of the receptor. In mouse models of castration-resistant prostate cancer, both compounds were able to induce tumor regression when given orally. Of 30 men with castration-resistant prostate cancer who had failed first-line anti-androgens, 43 percent of those treated with MDV3100 had declines of more than 50 percent in the levels of prostate-specific antigen, the authors report. "These compounds thus appear to be promising candidates for treatment of advanced prostate cancer," Tran and colleagues conclude.
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