Anastrozole

Anastrozole, sold under the brand name Arimidex among others, is an antiestrogenic medication used in addition to other treatments for breast cancer. Specifically it is used for hormone receptor-positive breast cancer. It has also been used to prevent breast cancer in those at high risk. It is taken by mouth.

Anastrozole
Clinical data
Trade namesArimidex, Aremed, others
Other namesAnastrazole; anastrozol; ICI-D1033; ZD-1033
AHFS/Drugs.comMonograph
MedlinePlusa696018
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth
Drug classAromatase inhibitor; Antiestrogen
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
BioavailabilityUnknown (but well-absorbed in animals)
Protein binding40%
MetabolismLiver (~85%) (N-dealkylation, hydroxylation, glucuronidation)
Elimination half-life40–50 hours
ExcretionUrine (11%)
Identifiers
  • 2,2'-[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropanenitrile)
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.129.723
Chemical and physical data
FormulaC17H19N5
Molar mass293.374 g·mol−1
3D model (JSmol)
SMILES
  • N#CC(C)(C)c1cc(Cn2cncn2)cc(c1)C(C)(C)C#N
  • InChI=1S/C17H19N5/c1-16(2,9-18)14-5-13(8-22-12-20-11-21-22)6-15(7-14)17(3,4)10-19/h5-7,11-12H,8H2,1-4H3 Y
  • Key:YBBLVLTVTVSKRW-UHFFFAOYSA-N Y
  (verify)

Common side effects of anastrozole include hot flashes, altered mood, joint pain, and nausea. Severe side effects include an increased risk of heart disease and osteoporosis. Use during pregnancy may harm the baby. Anastrozole is in the aromatase-inhibiting family of medications. It works by blocking the production of estrogens in the body, and hence has antiestrogenic effects.

Anastrozole was patented in 1987 and was approved for medical use in 1995. It is on the World Health Organization's List of Essential Medicines. Anastrozole is available as a generic medication. In 2021, it was the 182nd most commonly prescribed medication in the United States, with more than 2 million prescriptions.

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