Basic Info.
Product name: Formestane
Other name: Lentaron; FORMESTAQNE; Hydroxyandrostenedione
CAS Registry Number: 566-48-3
Assay: 98%Packing: 1kg/aluminum foil bag
Molecular Formula: C19H26O3
Molecular Weight: 302.41
Appearance: White crystalline powder
Product Description:
Formestane was the first selective, type I, steroidal aromatase inhibitor used in the treatment of estrogen-receptor positive breast cancer 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US FDA approved, and the intramuscular injection form of formestane (Lentaron) which was approved in Europe has been withdrawn.
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-hydroxytestosteron, 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.
Applications:
Formestane is a second generation, irreversible, steroidal aromatase inhibitor. It inhibits the aromatase enzyme responsible for converting androgens to estrogens, thereby preventing estrogen production. Breast cancer may be estrogen sensitive or insensitive. A majority of breast cancers are estrogen sensitive. Estrogen sensitive breast cancer cells depend on estrogen for viability. Thus removal of estrogen from the body can be an effective treatment for hormone sensitive breast cancers. Formestane has been targeted specifically for the treatment of postmenopausal women. Unlike premenopausal women who produce most estrogen in the ovaries, postmenopausal women produce most estrogen in peripheral tissues with the help of the aromatase enzyme. Formestane, an aromatase inhibitor, can thus help to decrease the local production of estrogen by blocking the aromatase enzyme in peripheral tissues (ie. Adispose tissue of the breast) to treat hormone sensitive breast cancer.
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