Anastrozole (Arimidex)

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.
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, Medscape, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• Breast cancer
• Endometrial cancer

Patient drug information

• Anastrozole (Arimidex) package insert
• Anastrozole (Arimidex) patient drug information (Chemocare)
• Anastrozole (Arimidex) patient drug information (UpToDate)

History of changes in FDA indication

• 12/27/1995: Initial approval for treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. (Based on Buzdar et al. 1996 & Jonat et al. 1996)
• 9/5/2002: Accelerated approval for adjuvant treatment of postmenopausal women with hormone receptor-positive early breast cancer. (Based on ATAC)
  • 9/16/2005: Converted to regular approval.
• Uncertain date: Approved for first-line treatment of postmenopausal women with hormone receptor-positive or hormone receptor-unknown locally advanced or metastatic breast cancer. (Based on Arimidex Study Group 2000 & TARGET)

Also known as

• Brand names: Altraz, Anabrez, Anastraze, Anastrazol Rontag, Anastrol, Arimidex, Asiolex, Karomex, Leprofen, RUI SI YI, RUI Ting, Trozolet, Trozolite.