Anastrozole – A New Generation in Aromatase Inhibition: Clinical Pharmacology
Abstract
Use of the aromatase inhibitor aminoglutethimide is limited by its lack of selectivity for aromatase and its toxicity. Newer agents are more selective, but do not always offer improved inhibition of aromatase. Indirect comparison of their activity in inhibiting aromatase and suppressing plasma oestrogens indicates that aminoglutethimide, rogletimide, formestane, and fadrozole inhibited aromatase activity by 74-91%, with reported falls in oestradiol level of 58-76%. In contrast, the new-generation oral once-daily aromatase inhibitors anastrozole (Arimidex) and letrozole were of a similar activity, inhibiting aromatase activity by over 96%, with a concomitant fall in oestradiol and oestrone levels of at least 80%. Anastrozole at the recommended clinical dose of 1 mg daily also suppressed oestrone sulphate levels by 93.5%; activity with anastrozole 10 mg daily was not statistically significantly different. The new generation of aromatase inhibitors, as typified by anastrozole, thus offers effective and convenient aromatase inhibition which correlates well with decreases in the levels of plasma oestrogens.
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At doses of 1-5 mg, anastrozole and letrozole decrease E levels by 97%-99%.
“Their intrinsic potency is considerably greater than that of aminoglutethimide, and at doses of 1-5 mg decreases E levels by 97%-Ͼ99%.”
From A new era in ovulation induction (2006) · cites this paper as [38]
Anastrozole and letrozole are selective aromatase inhibitors; they are reversible and highly potent.
“Anastrozole and letrozole are selective aromatase inhibitors.They are reversible and highly potent.”
From A new era in ovulation induction (2006) · cites this paper as [38]
Letrozole and anastrazole are completely absorbed after oral administration, with a mean half-life of approximately 45 hours (range, 30-60 hours).
“Letrozole and anastrazole are completely absorbed after oral administration, with a mean half-life of approximately 45 hours (range, 30 -60 hours).”
From A new era in ovulation induction (2006) · cites this paper as [38]
Aromatase inhibitors are orally administered, easy to use, and relatively inexpensive, with minor side effects.
“They are orally administered, easy to use, and relatively inexpensive, with minor side effects.”
From A new era in ovulation induction (2006) · cites this paper as [38]
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Anastrozoleof its Use in the Management of Postmenopausal Women with Advanced Breast Cancer
Wiseman, L. R., & Adkins, J. (1998)
- Authors
- Dowsett, M., & Lonning, P. E.
- Affiliations
- Royal Marsden Hospital (GB)
- ORCID
- Dowsett, M.
- Venue
- Oncology
- Publisher
- S. Karger AG
- Published
- 2009-06-30
- Volume
- 54 Suppl 2
- Pages
- 11-14
- ISSN
- 0030-2414 (ISSN-L)
- 1423-0232
- OpenAlex
- W2049586953
- Cited by
- 21
- References
- 0
- Citations by year
- 2022: 1 · 2019: 1 · 2016: 1 · 2013: 2
- FWCI
- 0.58
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Oncology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Advanced Breast Cancer Therapies
- Keywords
- anastrozole, aromatase inhibitors, clinical pharmacology, aminoglutethimide, letrozole, formestane, fadrozole, estradiol suppression, estrone sulfate, aromatase inhibition, breast cancer hormone therapy
- MeSH terms
- Anastrozole, Breast Neoplasms, Enzyme Inhibitors, Estrogens, Female, Humans, Nitriles, Triazoles, Antineoplastic Agents, Hormonal, Aromatase Inhibitors
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