Ethynylandrostanediol
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Ethynylandrostanediol (developmental code name HE-3235), or 17α-ethynyl-5α-androstane-3α,17β-diol, also known as Apoptone, is a synthetic, orally active, 17α-substituted analogue of the androstanediols which was under development for the treatment of prostate cancer and breast cancer but was discontinued.[1][2][3] It has very low affinity for steroid receptors, including the AR, ERα, ERβ, PR, and GR, and its mechanism of action is not well-characterized.[1][4] It produces 5α-dihydroethisterone as an active metabolite, which may contribute importantly to its biological activity.[1]
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Contributors: Prab R. Tumpati, MD
