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Femara

Letrozole (Femara®) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant treatment of hormonally-responsive breast cancer. more...

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Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Letrozole blocks this activity by competitive, reversible binding to the heme of its cytochrome p450 unit. The action is specific, and letrozole does not reduce production of mineralo- or corticosteroids. In contrast, Tamoxifen, the major medical therapy prior to the arrival of aromatase inhibitors, does effect its antiestrogenic action by interfering with the estrogen receptor, not the estrogen production.

Letrozole is approved by the FDA for the treatment of local or metastatic breast cancer that is hormone receptor positive or has an unknown receptor status. Side effects include signs and symptoms of hypoestrogenism. There is concern that long term use may lead to osteoporosis.

A related agent is anastrozole.

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Femara Approved as First-Line Breast Cancer Therapy - Brief Article
From FDA Consumer, 5/1/01

The Food and Drug Administration has approved a new use for the breast cancer drug Femara (letrozole). Femara had been approved to treat women with advanced breast cancer who had not responded to anti-estrogen drugs. The FDA's latest action approves the drug for use as a first-line treatment for postmenopausal women with advanced, metastatic, or hormone receptor positive or hormone receptor unknown breast cancers. Hormone receptor positive tumors are those that may grow when exposed to estrogen.

Femara was shown to be more effective than tamoxifen in a multinational study of more than 900 postmenopausal women whose locally advanced or metastatic breast cancers were not treatable by surgery or radiation.

Among those in the study, Femara significantly slowed the the time to progression of disease when compared to tamoxifen. With Femara, the median time to disease progression was 9.4 months, compared to 6 months with tamoxifen.

The incidence of side effects for Femara and tamoxifen was similar in the study. Side effects reported most frequently included bone pain, hot flushes, back pain, nausea, joint pain, and labored breathing.

Novartis Pharmaceuticals Corp., East Hanover, N.J., manufactures Femara.

COPYRIGHT 2001 U.S. Government Printing Office
COPYRIGHT 2004 Gale Group

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