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Basic information

  • Name:

  • Letrozole

  • CAS No.:

  • 112809-51-5

  • Formula:
  • C17H11N5
  • Synonyms:
  • 4,4-(1H-1,2,4-Triazol-1-ylmethylene)dibenzonitrile;4,4'-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile;Benzonitrile,4,4'-(1H-1,2,4-triazol-1-ylmethylene) bis-;Benzonitrile, 4,4-(1H-1,2,4-triazol-1-ylmethylene)bis-;Femara (TN);Femara;Letrozole [USAN:INN];4,4'-(1H-1,2,4-triazol-1-ylmethylene) bis-Benzonitrile;Letrozole & int;CGS 20267;CGS-20267;Lelrozol;4-[1-(1,2,4-Triazolyl)-methyl]-Benzonitrile;4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile;

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Chemistry

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

Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Letrozole blocks production of estrogens in this way 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, the antiestrogenic action of tamoxifen, the major medical therapy prior to the arrival of aromatase inhibitors, is due to its interfering with the estrogen receptor, rather than inhibiting estrogen production.

Uses

Letrozole is approved by the United States Food and Drug Administration (FDA) for the treatment of local or metastatic breast cancer that is hormone receptor positive or has an unknown receptor status in postmenopausal women. Side effects include signs and symptoms of hypoestrogenism. There is concern that long term use may LEAD to osteoporosis, which is why prescriptions of Letrozole are often accompanied by prescriptions of osteoporosis-fighting medications such as bisphosphonates.

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