Formestane
Product Name:Formestane
Synonyms:Lentaron;4-hydroxy-androst-4-ene-17-dione;4-hydroxy-delta(sub4)-androstenedione;4-Hydroxyandrost-4-Ene-3,17-Dione;4-Hydroxyandrostenedione;4-Hydroxy-4-Androstene-3,17-Dione;4-Androsten-4-Ol-3,17-Dione;4-OHA;CGP-32349
CAS:566-48-3
MF:C19H26O3
MW:302.41
Chemical Properties:Crystallized from aqueous methanol, m.p. 199 ~ 202 ℃; crystallized from ethyl acetate, m.p. 203.5 ~ 206 ℃. UV absorption maximum (99.5% ethanol): 278nm (ε11030). [α] D20 + 181 ° (C = 7.7, chloroform).
Uses: aromatase inhibitors ,it is used for progressive breast cancer. male hormones, assimilating protein class.
Anti-Cancer Drugs
Formestane also known as lentaron,is an anti-cancer drug, it is primarily used for the treatment of postmenopausal women with advanced breast cancer, it is also effective in prostate cancer.
Formestane is a androstenedione derivative, and it belongs to an aromatase inhibitor with aminoglutethimide, it is a hormone antineoplastic agent. In physiological conditions, it may competitively inhibit the synthesis of the enzyme leading to estrogen biosynthesis decrease in tissues, then it plays its role in cancer. When the tumor tissue growth relies on the presence of estrogen, in order to inhibit tumor growth, the elimination of tumor estrogen-mediated growth stimulation is necessary. This product is more selective than aminoglutethimide while its activity is 100 to 1000 times of aminoglutethimide, and it does not inhibit the synthesis of adrenal hormones，without having to recharge cortisone, etc . The in vitro inhibition of aromatase enzyme of this product is 60 times stronger than aminoglutethimide.
While it is used alone, the drug can not significantly reduce the pre-menopausal estrogen levels in the blood of women,when it is combined with goserelin (gonadotropin-releasing hormone agonist)， its inhibitory effect of estrogen in premenopausal women is greater than goserelin used alone. Formestane has no cross-resistance with other aromatase inhibitors , it has no side effects of aminoglutethimide. After oral administration，it is rapidly absorbed by gastrointestinal, its peak plasma concentration time is 1 to 1.5 hours, but the peak concentration of individual is of great difference; after intramuscular injection，it can be accumulated at the injection site and be slowly absorbed. It performs Biphasic elimination process, the initial elimination half-life is 2 to 4 days, the terminal elimination half-life is 5 to 10 days. It is mainly metabolized in the liver after oral administration, in the form of glycosides acid metabolites excreted in the urine.
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