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| Clinical data | |
|---|---|
| Trade names | Arimidex, Aremed, others[1] |
| Other names | Anastrazole; anastrozol; ICI-D1033; ZD-1033 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a696018 |
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| Routes of administration | By mouth |
| Drug class | Aromatase inhibitor; Antiestrogen |
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| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | Unknown (but well-absorbed in animals)[3] |
| Protein binding | 40%[4][5] |
| Metabolism | Liver (~85%) (N-dealkylation, hydroxylation, glucuronidation)[4][3][5] |
| Elimination half-life | 40–50 hours[4][3][5] |
| Excretion | Urine (11%)[4][3][5] |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.129.723 |
| Chemical and physical data | |
| Formula | C17H19N5 |
| Molar mass | 293.374 g·mol−1 |
| 3D model (JSmol) | |
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Anastrozole, sold under the brand name Arimidex among others, is an antiestrogenic medication used in addition to other treatments for breast cancer.[7][8] Specifically it is used for hormone receptor-positive breast cancer.[8] It has also been used to prevent breast cancer in those at high risk.[8] It is taken orally.[8]
Common side effects of anastrozole include hot flashes, altered mood, joint pain, and nausea.[8][7] Severe side effects include an increased risk of heart disease and osteoporosis.[8] Use during pregnancy may harm the baby.[8] Anastrozole is in the aromatase-inhibiting family of medications.[8] It works by blocking the production of estrogens in the body, and hence has antiestrogenic effects.[8]
Anastrozole was patented in 1987 and was approved for medical use in 1995.[9][10] It is on the World Health Organization's List of Essential Medicines.[11] Anastrozole is available as a generic medication.[8] In 2022, it was the 179th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[12][13]
- ^ Cite error: The named reference
Drugs.comwas invoked but never defined (see the help page). - ^ "Arimidex Product information". Health Canada. 25 January 2002. Retrieved 16 February 2025.
- ^ a b c d Cite error: The named reference
Lønning2003was invoked but never defined (see the help page). - ^ a b c d Cite error: The named reference
Lonning2003was invoked but never defined (see the help page). - ^ a b c d Cite error: The named reference
SanfordPlosker2008was invoked but never defined (see the help page). - ^ "anastrozole". Chemical Entities of Biological Interest (ChEBI). European Molecular Biology Laboratory. Archived from the original on 22 September 2011. Retrieved 14 August 2011.
- ^ a b "Highlights of Prescribing Information Anastrozole" (PDF). FDA. Archived from the original (PDF) on 31 July 2019. Retrieved 31 July 2019.
- ^ a b c d e f g h i j "Anastrozole". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
- ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 516. ISBN 9783527607495. Archived from the original on 20 December 2016.
- ^ Dukes M (1997). "The relevance of preclinical models to the treatment of postmenopausal breast cancer". Oncology. 54 (2): 6–10. doi:10.1159/000227748. PMID 9394853.
- ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
- ^ "Anastrozole Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.