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HE-3235 is an orally active 3β-androstanediol analog. HE-3235 reduces the expression of androgen receptor (Androgen receptor) and decreases intratumoral androgen levels. HE-3235 exhibits anticancer activity against castration-resistant prostate cancer.

HE-3235 (2 h) can bind to recombinant androgen receptor (IC₅₀ 1500 nM) and estrogen receptor alpha (IC₅₀ 200 nM).
HE-3235 can trans activate mutant androgen receptor (EC₅₀ 0.48 nM), androgen/glucocorticoid receptor (EC₅₀ 11.4 nM), estrogen receptor alpha/beta (EC₅₀ 0.8 nM), and estrogen receptor beta (EC₅₀ 164 nM) in corresponding transfected cell lines.
HE-3235 can effectively inhibit the proliferation of LNCaP prostate cancer cells in vitro, with an EC₅₀ of 6 nM.
HE-3235 (1-50 nM; 3 d) dose dependently inhibits the proliferation of castration resistant prostate cancer C4-2B cells.

HE-3235 (20-200 mg/kg; oral; Daily administration of medication; Continuous exposure to testosterone, androstenedione, and dehydroepiandrosterone (DHEA) for 28 days can lead to a dose-dependent and time-dependent decrease in plasma testosterone, androstenedione, and dehydroepiandrosterone (DHEA) concentrations in male beagle dogs.
HE-3235 (160 mg/kg; intraperitoneal injection; Once a day, 5 days a week, for 4 weeks) can inhibit the growth of subcutaneous castration resistant prostate cancer in castrated male CB-17 SCID mice by 43%. At the same time, the levels of androgen, AR mRNA, and nuclear AR localization in the tumor are significantly reduced, and the serum PSA level briefly increases.