Letrozole (Femara)

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General information

Class/mechanism: Selective non-steroidal aromatase inhibitor. The aromatase enzyme converts adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) in peripheral tissues. Letrozole competitively binds to and inhibits the aromatase by binding to the heme of the enzyme's cytochrome P450.[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

  • 1/10/2001 (earliest label available at Drugs @ FDA): indicated for first-line treatment of postmenopausal women with hormone receptor positive or hormone receptor unknown locally advanced or metastatic breast cancer. Femara is also indicated for the treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen therapy.
  • 10/29/2004: Label expanded for the extended adjuvant treatment of early breast cancer in postmenopausal women who have received 5 years of adjuvant tamoxifen therapy. (Indication expanded to adjuvant setting after prior therapy)
  • 12/28/2005: Label expanded for the adjuvant treatment of postmenopausal women with |hormone receptor positive early breast cancer. (Indication expanded to adjuvant setting)
  • 3/2/2010: Label simplified to:
    • Adjuvant treatment of postmenopausal women with hormone receptor positive early breast cancer (No change)
    • Extended adjuvant treatment of postmenopausal women with early breast cancer who have received prior standard adjuvant tamoxifen therapy (Years requirement removed)
    • First and second-line treatment of postmenopausal women with hormone receptor positive or unknown advanced breast cancer

Also known as

  • Brand names: Femara, Fempro, Gynotril, Latrotal, Lerozol, Letoval, Letpro, Letromina, Letroplex, Letroz, Letrozol, Lexel, Lezole

References