Formestane ,Lentaron;4-hydroxy-androst-4-ene-17-dione

English name: Formestane.

4-hydroxy-androst-4-ene-17-dione; 4 - hydroxy - delta (sub4) - androstenedione; 4 - HYDROXYANDROST - 4 - ENE - 3 in 2 - DIONE; 4 - HYDROXYANDROSTENEDIONE; 4 - HYDROXY - 4 - ANDROSTENE - 3 in 2 - DIONE. 4 - ANDROSTEN - 4 - OL - 3 in 2 - DIONE. 4 - smaller companies; CGP - 32349.

CAS no. : 566-48-3

Molecular formula: C19H26O3.

Molecular weight: 302.41.

EINECS no. :

Related category: Pharmaceutical Raw Materials; Miscellaneous Biochemicals. Inhibitors; Intermediates and Fine Chemicals. Pharmaceuticals; Steroids; Antitumor drugs; Other anti-tumor drugs; Drugs; Steroid; Cell biology; Pharmaceutical intermediates; Anti - cancer&immunity; Pharmaceutical ingredients; Nonsteroidal; Small molecule inhibitors; Enzyme inhibitors; Active pharmaceutical ingredients

Mol file: 566-48-3. Mol.

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Formesan property.

The melting point of 199-202 ° C

Than polarimetric D20 + 181 ° c = 7.7 in chloroform)

2-8 ° C storage conditions

Solid form

InChIKey OSVMTWJCGUFAOD KZQROQTASA - N

The CAS DataBase is 56-48-3 (CAS DataBase Reference)

Use and synthesis method of formesan.

The anti-cancer drug formestane, also known as fumetan, lantalon, and lantalon, is an anti-cancer drug that is mainly used to treat postmenopausal breast cancer and is also effective for prostate cancer.

Fumestane is a derivative of androstenedione, which is an aromatic enzyme inhibitor, and is a hormone antitumor agent. In physiological conditions, it can competitively inhibit the synthesis of estrogens in the tissues and reduce the biosynthesis of estrogen in the tissues, thus exerting its anti-cancer effect. When the growth of tumor tissues depends on the presence of estrogen, it is necessary to inhibit the growth of the tumor and eliminate the estrogen-mediated growth stimulation of the tumor. This product is more selective than aminomide and is 100 ~ 1000 times more active than aminomide, and it does not inhibit the synthesis of adrenal cortical hormones, and it does not need to supply cortisone. In vitro the inhibitory effect on aromatase was 60 times greater than that of aminobamite.

This medicine alone can't significantly reduce the premenopausal women estrogen levels in the blood, combination goserelin (gonadotropin-releasing hormone agonist) of premenopausal women estradiol inhibition effect is greater than goserelin alone. Formesan and other aromatase inhibitors have no cross-drug resistance, and the side effects of aminotromide. After oral administration, the gastrointestinal tract was rapidly absorbed, and the concentration of blood drug was 1 ~ 1.5 hours, but the peak concentration was significantly different. Intramuscular injection can be deposited in the injection site and slowly absorbed. The initial elimination half-life is 2-4 days, and the half-life is 5-10 days. After oral administration, it is mainly metabolized in the liver and excreted from urine in the form of glycosidic acid metabolites.

Andy editor of chemical engineering.

Chemical properties from aqueous methanol crystallization, melting point of 199 ~ 202 ℃. From the ethyl acetate crystallization, melting point of 203.5 ~ 206 ℃. UV maximum absorption (99.5% ethanol) : 278nm(11030). [alpha] D20 + 181 ° C = 7.7, chloroform).

Use aromatase inhibitors. For progressive breast cancer.

Use male hormone, assimilate protein.

Use is used as an aromatase inhibitor.

 

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