Formestane

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Formestane
Formestane.svg
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
Trade names Lentaron
AHFS/Drugs.com International Drug Names
Identifiers
CAS Number 566-48-3 YesY
ATC code L02BG02 (WHO)
PubChem CID: 11273
ChemSpider 10799 YesY
UNII PUB9T8T355 YesY
KEGG D07260 YesY
ChEBI CHEBI:75172 N
ChEMBL CHEMBL132530 YesY
Synonyms 4-hydroxyandrost-4-ene-3,17-dione
Chemical data
Formula C19H26O3
Molecular mass 302.408 g/mol
  • O=C4C(/O)=C3/CC[C@@H]2[C@H](CC[C@@]1(C(=O)CC[C@H]12)C)[C@@]3(C)CC4
  • InChI=1S/C19H26O3/c1-18-10-8-15(20)17(22)14(18)4-3-11-12-5-6-16(21)19(12,2)9-7-13(11)18/h11-13,22H,3-10H2,1-2H3/t11-,12-,13-,18+,19-/m0/s1 YesY
  • Key:OSVMTWJCGUFAOD-KZQROQTASA-N YesY
 NYesY (what is this?)  (verify)

Formestane (trade name Lentaron) is a type I, steroidal, selective aromatase inhibitor.[1] It is used in the treatment of estrogen receptor-positive breast cancer in postmenopausal women. The drug is not active orally, and is instead available only as an intramuscular depot injection. Because of this, it is no longer popular as many orally active aromatase inhibitors have been identified and introduced. Formestane is an analogue of androstenedione.

Formestane is often used to suppress the production of estrogens 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 weak aromatase inhibitor.

References

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