Reference

Exemestane: treatment of breast cancer with selective inactivation of aromatase

Exemestane: treatment of breast cancer with selective inactivation of aromatase. Higa, Gerald M. (Department of Clinical Pharmacy and Mary Babb Randolph Cancer Center, West Virginia University, Morgantown, WV 26506-9520, USA). American Journal of Health-System Pharmacy, 59(22), 2194-2204 (English) 2002 American Society of Health-System Pharmacists. CODEN: AHSPEK. ISSN: 1079-2082. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. The mechanism of action, pharmacol., and clin. efficacy and safety of exemestane in the treatment of metastatic breast cancer are reviewed. Endocrine strategies that deprive tumor cells of estrogens are effective therapeutic modalities for patients with hormone-dependent breast cancer. The efficacy and toxicities assocd. with tamoxifen and aminoglutethimide have contributed to the development of agents that selectively target aromatase, the enzyme responsible for conversion of androgens to estrogens. Exemestane, an orally active irreversible inhibitor of aromatase, was recently approved as second-line endocrine therapy of advanced hormone-sensitive postmenopausal breast cancer. Compared with megestrol acetate in patients with disease progressing on tamoxifen, a no. of clin. endpoints, including a survival advantage, were significantly better in the exemestane-treated group. Preliminary data also indicate that cross-resistance is incomplete between exemestane and the reversible aromatase inhibitors. Even though suppression of aromatase activity is quant. similar regardless of the interactive mechanism between drug and enzyme, clin. relevant differences may become apparent with further application of these two types of aromatase inhibitors. Exemestane is effective as a second- or third-line treatment of advanced, estrogen-receptor pos.Except for chemicals metioned above, 107868-30-4 and 9039-48-9 are also used. breast cancer in postmenopausal patients. .

Synthesis of novel aromatase inhibitors from bromosteroidal intermediates

Synthesis of novel aromatase inhibitors from bromosteroidal intermediates. Longo, A.; Colombo, M.; Orzi, F.; Lombardi, P.; Buzzetti, F. (Farmitalia Carlo Erba S.r.l., Milan 20159, Italy). Ind. Chem. 107868-30-4 and 64395-40-0 are cas registry numbers of chemicals which are used as reagents here. Libr., 3(Adv. Organobromine Chem. 1), 119-25 (English) 1991. CODEN: ICHLE6. DOCUMENT TYPE: Journal CA Section: 32 (Steroids) The prepn. of FCE 24304 (I), FCE 24928 (II), and FCE 24210 (III) from bromosteroidal intermediates is discussed. .