Anastrozole

Products

Anastrozole is commercially available in the form of film-coated tablets (Arimidex, generic). It has been approved in many countries since 1996.

Structure and properties

Anastrozole (C17H19N5, Mr = 293.4 g/mol) exists as a white powder that is very sparingly soluble in water. It is a triazole derivative with a non-steroidal structure.

Effects

Anastrozole (ATC L02BG03) has antitumor and antiproliferative properties. The effects are due to competitive inhibition of the enzyme aromatase, which catalyzes the biosynthesis of estrogens from androgens such as androstenedione. This lowers serum estradiol concentrations. Anastrozole has a long half-life of 40 to 50 hours.

Indications

For adjuvant treatment of breast cancer and for treatment of advanced breast cancer in postmenopausal women.

Dosage

According to the SmPC. Tablets are taken once daily at the same time of day, regardless of meals.

Abuse

Anastrozole can be abused as a doping agent and for bodybuilding. It is prohibited during and outside of athletic competition.

Contraindications

  • Hypersensitivity
  • Pregnancy, lactation

Full precautions can be found in the drug label.

Interactions

Estrogens may reverse the effects of anastrozole and should not be administered concomitantly.

Adverse effects

Adverse effects are largely a result of reduced estrogen levels and resemble menopausal symptoms. The most common possible adverse effects include: