Cited by 606Estrogen and related hormone effectsBreast Cancer Treatment StudiesAdvanced Breast Cancer Therapies

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Influence of Letrozole and Anastrozole on Total Body Aromatization and Plasma Estrogen Levels in Postmenopausal Breast Cancer Patients Evaluated in a Randomized, Cross-Over Study

Geisler, Jürgen, Haynes, Ben, Anker, Gun, Dowsett, Mitch, Lønning, Per Eystein·2002·Journal of Clinical Oncology

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Abstract

PURPOSE: To compare the effects of the two novel, potent, nonsteroidal aromatase inhibitors anastrozole and letrozole on total-body aromatization and plasma estrogen levels. PATIENTS AND METHODS: Twelve postmenopausal women with estrogen receptor–positive, metastatic breast cancer were treated with anastrozole 1 mg orally (PO) and letrozole 2.5 mg PO once daily, each given for a time interval of 6 weeks in a randomized sequence. Total-body aromatization was determined before treatment and at the end of each treatment period using a dual-label isotopic technique involving isolation of the metabolites with high-performance liquid chromatography. Plasma levels of estrone (E 1 ), estradiol (E 2 ), and estrone sulfate (E 1 S) were determined in samples obtained before each injection using highly sensitive radioimmunoassays. RESULTS: Pretreatment aromatase levels ranged from 1.68% to 4.27%. On-treatment levels of aromatase were detectable in 11 of 12 patients during treatment with anastrozole (mean percentage inhibition in the whole group, 97.3%) but in none of the 12 patients during treatment with letrozole (> 99.1% suppression in all patients; Wilcoxon, P = .0022, comparing the two drug regimens). Treatment with anastrozole suppressed plasma levels of E 1 , E 2 , and E 1 S by a mean of 81.0%, 84.9%, and 93.5%, respectrively, whereas treatment with letrozole caused a corresponding decrease of 84.3%, 87.8% and 98.0%, respectively. The suppression of E 1 and E 1 S was found to be significantly better during treatment with letrozole compared with anastrozole (P = .019 and .0037, respectively). CONCLUSION: This study revealed letrozole (2.5 mg once daily) to be a more potent suppressor of total-body aromatization and plasma estrogen levels compared with anastrozole (1 mg once daily) in postmenopausal women with metastatic breast cancer.

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Authors: Geisler, J., Haynes, B., Anker, G., Dowsett, M., & Lønning, P. E.
Affiliations: Haukeland University Hospital (NO)
ORCID: Geisler, Jürgen
Dowsett, Mitch
Lønning, Per Eystein
Venue: Journal of Clinical Oncology
Publisher: American Society of Clinical Oncology (ASCO)
Published: 2002-02-01
Volume: 20
Issue: 3
Pages: 751-757
ISSN: 0732-183X (ISSN-L)
1527-7755
DOI: 10.1200/jco.20.3.751
OpenAlex: W2145819414
Cited by: 604
References: 37
Citations by year: 2026: 8 · 2025: 3 · 2024: 8 · 2023: 15 · 2022: 10 · 2021: 11 · 2020: 14 · 2019: 14 · 2018: 12 · 2017: 18 · 2016: 25 · 2015: 23 · 2014: 26 · 2013: 22 · 2012: 16
FWCI: 25.01
Type: journal article
Language: en
Open access: closed
Locations: Journal of Clinical Oncology (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
Health Sciences › Medicine › Oncology › Advanced Breast Cancer Therapies
Keywords: letrozole, anastrozole, aromatase inhibitors, aromatization, plasma estrogen, estrone, estradiol, estrone sulfate, metastatic breast cancer, postmenopausal women, estrogen receptor-positive breast cancer, aromatase inhibition
MeSH terms: Letrozole, Anastrozole, Aged, Antineoplastic Agents, Aromatase, Breast Neoplasms, Chromatography, High Pressure Liquid, Enzyme Inhibitors, Estradiol, Estrogens, Estrone, Female, Humans, Middle Aged, Nitriles, Radioimmunoassay, Triazoles, Postmenopause, Cross-Over Studies, Antineoplastic Agents, Hormonal, Aromatase Inhibitors

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Influence of Letrozole and Anastrozole on Total Body Aromatization and Plasma Estrogen Levels in Postmenopausal Breast Cancer Patients Evaluated in a Randomized, Cross-Over Study

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