Ethynylandrostanediol
| Ethynylandrostanediol | |
|---|---|
| |
| INN | |
| Drug class | |
| Routes of administration | |
| Pregnancy category | |
| Bioavailability | |
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| CAS Number | 183387-50-0 |
| PubChem | 42611099 |
| DrugBank | |
| ChemSpider | 32698509 |
| KEGG | |
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.<ref name="pmid20814732">,
17α-alkynyl 3α, 17β-androstanediol non-clinical and clinical pharmacology, pharmacokinetics and metabolism, Invest New Drugs, 2012, Vol. 30(Issue: 1), pp. 59–78, DOI: 10.1007/s10637-010-9517-0, PMID: 20814732,</ref><ref name="pmid19337256">, Inhibition of androstenediol-dependent LNCaP tumour growth by 17alpha-ethynyl-5alpha-androstane-3alpha, 17beta-diol (HE3235), Br. J. Cancer, 2009, Vol. 100(Issue: 7), pp. 1068–72, DOI: 10.1038/sj.bjc.6604987, PMID: 19337256, PMC: 2669987,</ref><ref name="AdisInsight">http://webcache.googleusercontent.com/search?q=cache:Jy1DYIHEUtQJ:adisinsight.springer.com/drugs/800025305</ref> 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.<ref name="pmid20814732" /><ref name="pmid19881957">,
HE3235 inhibits growth of castration-resistant prostate cancer, Neoplasia, 2009, Vol. 11(Issue: 11), pp. 1216–25, DOI: 10.1593/neo.09960, PMID: 19881957, PMC: 2767223,</ref> It produces 5α-dihydroethisterone as an active metabolite, which may contribute importantly to its biological activity.<ref name="pmid20814732" />
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