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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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Drug cuts recurrence of breast cancer - Biomedicine - Letrozole - Brief Article
From Science News, 11/29/03

Letrozole, a drug that derails the body's production of estrogen, reduces breast cancer recurrences in women who have exhausted the usefulness of the anticancer drug tamoxifen, a new drug trial has revealed.

Tamoxifen stops breast cancers in many women by interfering with estrogen's proliferative effect on tumor cells. But taking tamoxifen for more than 5 years provides no additional benefit, compared with going off the drug after that period.

Researchers identified 5,157 post-menopausal women who had taken tamoxifen for about 5 years and randomly assigned them to take either an inert pill or letrozole, which wipes out nearly all estrogen in the body.

The scientists stopped the study when it became clear that the group receiving letrozole had roughly three-fifths as many breast cancer recurrences as did women getting the placebo, says study coauthor Paul E. Goss, a medical oncologist at Princess Margaret Hospital in Toronto. Researchers then offered letrozole to all participants, each of whom had been followed for 2.4 years on average. The report appears in the Nov. 6 New England Journal of Medicine.

Letrozole disables an enzyme called aromatase, which the body needs to make estrogen. Another aromatase inhibitor, the drug anastrozole, is also being tested for cancer-fighting abilities (SN: 11/24/01, p. 327).

Although tamoxifen's anticancer effect levels out at 5 years, there's no question that the drug imparts a residual benefit even after long-term users stop taking it. Indeed, no one knows how long the benefits of tamoxifen or the aromatase inhibitors might linger. That and the question of whether the drugs might interact in good or bad ways when given simultaneously are the topics of several studies now under way.

Letrozole is marketed as Femara by Novartis in New York, which was a sponsor of the newly reported trial.--S.P.

COPYRIGHT 2003 Science Service, Inc.
COPYRIGHT 2003 Gale Group

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