Formestane

Research use only, not for human use.

Formestane was the first selective, type I, steroidal aromatase inhibitor used in the treatment of estrogen-receptor positive breast Y in post-menopausal women.

Formestane was the first selective, type I, steroidal aromatase inhibitor used in the treatment of estrogen-receptor positive breast Y in post-menopausal women. Formestane suppresses 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. It is listed as a prohibited substance by the World Anti-Doping Agency for use in athletes. Formestane has poor oral bioavailability, and thus must be administered forthnightly (bi-weekly) by intramuscular injection. Some clinical data has suggested that the clinically recommended dose of 250mg was too low. With the discovery of newer, non-steroidal and steroidal, aromatase inhibitors which were orally active and less expensive than formestane, formestane lost popularity. Currently, formestane (categorized as an anti-estrogenic agent) is prohibited from use in sports in accordance to the regulations of the World Anti-Doping Agency. It is not US FDA approved, and the intramuscular injection form of formestane (Lentaron) which was approved in Europe has been withdrawn.

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CGP 32349 | Formestane | 4-HAD | 4-Hydroxy-androst-4-ene-3,17-dione | Lentaron | NSC 282175

Endocrinology/Hormones

Aromatase

Aromatase

Cancer

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566-48-3

302.41

C19H26O3

>98% (HPLC)

DMSO: 61 mg/mL (201.71 mM)

O=C(C(O)=C1CC[C@@]2([H])[C@]3([H])CC4)CC[C@]1(C)[C@@]2([H])CC[C@]3(C)C4=O

(8R,9S,10R,13S,14S)-4-hydroxy-10,13-dimethyl-7,8,9,10,11,12,13,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-3,17(2H,6H)-dione

(-20℃)

With Ice Pack

≥ 2 years