Formestane

Formestane
Systematic (IUPAC) name
(8R,9S,10R,13S,14S)-4-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-3,17-dione
Clinical data
AHFS/Drugs.com International Drug Names
Identifiers
566-48-3 Yes
L02BG02
PubChem CID 11273
ChemSpider 10799 Yes
UNII PUB9T8T355 Yes
KEGG D07260 Yes
ChEBI CHEBI:75172 
ChEMBL CHEMBL132530 Yes
Synonyms 4-hydroxyandrost-4-ene-3,17-dione
Chemical data
Formula C19H26O3
302.408 g/mol
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Formestane (Lentaron) is a type I, steroidal aromatase inhibitor. It is used in the treatment of estrogen-receptor positive breast cancer in post-menopausal women. It is available as an intramuscular depot injection.

Formestane is often used to suppress estrogen production from anabolic steroids or prohormones. It also acts as a prohormone to 4-hydroxytestosterone, an active steroid which displays weak androgenic activity in addition to acting as a mild aromatase inhibitor.

Formestane has poor oral bioavailability and as such is no longer popular as many orally active aromatase inhibitors have been identified.

It is selective.[1]

References

  1. ↑ Pérez Carrión R, Alberola Candel V, Calabresi F et al. (1994). "Comparison of the selective aromatase inhibitor formestane with tamoxifen as first-line hormonal therapy in postmenopausal women with advanced breast cancer". Ann. Oncol. 5 Suppl 7: S19–24. PMID 7873457.