Apoptone

Apoptone (HE3235) is an orally bioavailable synthetic analogue of 3β-androstanediol and an adrenal steroid derivative with potential antineoplastic activity. It acts primarily as an androgen receptor antagonist and has been shown to induce apoptosis in cancer cells by inhibiting the BCL2 gene (which encodes proteins that prevent apoptosis) and stimulating the expression of pro-apoptotic proteins such as caspases. Apoptone also downregulates ABCG2 (BCRP1), a gene encoding a multi-drug resistance protein. Preclinical studies demonstrated activity in rodent models of prostate and breast cancer. Clinical development reached Phase I/II trials for hormone-refractory prostate cancer but was discontinued[1][2][3][4].

Brand names

Apoptone

Other names

apoptone17α-ethynyl-5α-androstane-3α,17β-diol