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Letrozole

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.

Read more at Wikipedia.org


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Letrozole Therapy for Breast Cancer
From Nurse Practitioner, 2/1/04 by Risser, Nancy

ONCOLOGY * Letrozole Therapy for Breast Cancer Goss PE, Ingle JN, Martina S, et al: A randomized trial ofletrozole in postmenopausal women after five years of tamoxifen therapy for early-stage breast cancer. N Engl J Med 2003;349(19): 1793-802.

Bryant J, Wolmark N: Letrozole after tamoxifen for breast cancer- what is the price of success? N Engl J Med 2003;349l19):1855-57 (editorial).

Burstein HF: Beyond tamoxifen-extending endocrine treatment for early-stage breast cancer. N Engl J Med 2003;349(WI: 1857-59 (editorial).

In hormone-dependent breast cancer, 5 years of postoperative treatment with tamoxifen, an antagonist of the estrogen receptor, prolongs disease-free and overall survival, but more than 5 years of therapy does not provide added benefit. Goss and coauthors investigated the benefits of extended therapy with the aromatase inhibitor letrozole, which suppresses estrogen production. More than 5,000 women were recruited and an interim analysis was conducted after a median of 2.4 years of follow-up. There were 207 local or metastatic recurrences of breast cancer or new primary cancers, 75 in the letrozole group and 132 in the placebo group, with an estimated 4-year disease-free survival rate of 93% and 87% respectively (p

Copyright Springhouse Corporation Feb 2004
Provided by ProQuest Information and Learning Company. All rights Reserved

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