Exemestane

Product Name: Exemestane

Synonyms: ExeMestane (USP);ExeMestane(AroMasin);1,4-Androstadien-3,17-dione-6-Methylene-d2;(8R,9S,10R,13S,14S)-10,13-Dimethyl-6-methylene-7,8,9,11,12,13,15,16-octahydro-6H-cyclopenta[a]phenanthrene-3,17(10H,14H)-dione;ExeMestine;(8R,9S,10R,13S,14S)-10,13-diMethyl-6-Methylene-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione;ExeMestane SynonyMs 6-Methylenandrosta-1,4-diene-3,17-dione;PNU155971

CAS: 107868-30-4

MF: C20H24O2

MW: 296.4

Description

Exemestane was launched in US and other countries for the treatment of estrogendependent tumors and postmenopausal breast cancer. It is a novel steroidal compound structurally related to the natural substrate for the biosynthesis of estrogen, androstanedione, and can be synthesized by methylidenation of androsta-1, 4-dien- 17beta-ol-3-one in 6 position then oxidation of the alcohol function. Exemestane is an irreversible inactivator of the aromatase enzyme system, so inducing in vivo a dose-related sustained suppression of serum estrogen and minimal endocrine activity. It is the first steroidal representative of the third-generation of orally active aromatase inhibitors with a highly potent and selective mechanism of action, displaying good tolerability and safety profile. In rats with DMBA-induced mammary tumors, 10 to 100 mglkg of exemestan administered po twice-daily for 4 weeks resulted in 76 to 88% regression. In women failing anti-estrogen therapy with tamoxifen, this agent has demonstrated high activity in locally advanced or metastatic disease. In addition, it may also have potential for breast cancer prevention.