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GTx-758 (brand name Capesaris) is an orally available, synthetic nonsteroidal small molecule that acts as a selective estrogen receptor alpha (ERα) agonist. It was developed for the treatment of advanced prostate cancer, particularly castration-resistant prostate cancer (CRPC). GTx-758 works by selectively activating ERα, which increases hepatic production of sex hormone-binding globulin (SHBG), thereby reducing free testosterone levels in the blood to castrate levels. This mechanism suppresses androgen-driven tumor growth while potentially avoiding some side effects associated with traditional androgen deprivation therapy such as bone loss and hot flashes. The drug completed phase II clinical trials but development was discontinued after these studies[1][3][7].
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