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Updated: Aug 18, 2026

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
Published on: February 6, 2015
Focus on anastrozole and breast cancer
1St George's Hospital and Medical School, London, UK. kefahmokbel@hotmail.com
Abstract:
This commentary article provides an overview of recent clinical research trials involving anastrozole and its evolving role in the management of breast cancer. Anti-aromatase agents inhibit the cytochrome P-450 component of the aromatase enzyme complex responsible for the final step of estrogen biosynthesis in peripheral tissues which are the main source of estrogen in postmenopausal women. Anastrozole is a third-generation non-steroidal aromatase inhibitor. It has been shown to be superior to megestrol acetate, in terms of survival and adverse effects, as a second-line therapy in postmenopausal women with estrogen receptor (ER)- and/or progesterone receptor (PgR)-positive advanced breast cancer. Phase III clinical trials have also demonstrated that anastrozole significantly prolongs the time to tumour progression compared with tamoxifen as a first-line therapy for ER- and/or PgR-positive advanced breast cancer in postmenopausal women. Furthermore, the preliminary results of the Arimidex, Tamoxifen, Alone and in Combination (ATAC) study have shown that adjuvant anastrozole is superior to tamoxifen in terms of disease-free survival (DFS), non-musculoskeletal adverse effects and prevention of contralateral breast cancer in postmenopausal women with early, ER-positive breast cancer. Although longer follow-up is required to assess the long-term effects of anastrozole on bone mineral density, cognitive function and overall survival, the drug has been recently approved for adjuvant use in postmenopausal women with early, ER-positive breast cancer who are unable to tolerate tamoxifen or at an increased risk of developing thromboembolism or endometrial cancer. The potential role of anastrozole in the neoadjuvant setting, the management of DCIS, premenopausal breast cancer and breast cancer prevention is currently being investigated.
Insights
Anastrozole, an aromatase inhibitor, shows improved survival and fewer side effects compared to megestrol acetate and tamoxifen for postmenopausal breast cancer patients. It is now approved for adjuvant use in early-stage breast cancer.
Area of Science:
- Oncology
- Endocrinology
- Pharmacology
Background:
- Estrogen biosynthesis in postmenopausal women primarily occurs in peripheral tissues.
- Aromatase inhibitors block the final step of estrogen production.
- Anastrozole is a third-generation non-steroidal aromatase inhibitor.
Purpose of the Study:
- To review clinical research on anastrozole in breast cancer management.
- To evaluate anastrozole's efficacy and safety compared to other therapies.
- To discuss anastrozole's current and potential future roles.
Main Methods:
- Review of clinical research trials involving anastrozole.
- Comparison of anastrozole with megestrol acetate and tamoxifen.
- Analysis of data from Phase III trials and the ATAC study.
Main Results:
- Anastrozole is superior to megestrol acetate as second-line therapy for advanced breast cancer.
- Anastrozole prolongs progression-free survival compared to tamoxifen as first-line therapy.
- Adjuvant anastrozole shows improved disease-free survival and fewer adverse effects than tamoxifen in early breast cancer.
Conclusions:
- Anastrozole is an effective treatment for postmenopausal breast cancer, demonstrating superiority over existing therapies.
- Anastrozole is approved for adjuvant use in early, ER-positive breast cancer.
- Ongoing research is exploring anastrozole's role in neoadjuvant therapy, DCIS, premenopausal cancer, and prevention.
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