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What Is Anastrozole?

Anastrozole is a prescription aromatase inhibitor used in postmenopausal women with certain types of breast cancer. It is approved as adjuvant treatment for hormone receptor-positive early breast cancer, first-line treatment for hormone receptor-positive or hormone receptor-unknown locally advanced or metastatic breast cancer, and treatment of advanced breast cancer that progresses after tamoxifen therapy.

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What Is Anastrozole?

Anastrozole is a prescription aromatase inhibitor used in postmenopausal women with certain types of breast cancer. It is approved as adjuvant treatment for hormone receptor-positive early breast cancer, first-line treatment for hormone receptor-positive or hormone receptor-unknown locally advanced or metastatic breast cancer, and treatment of advanced breast cancer that progresses after tamoxifen therapy.

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How Does Anastrozole Lower Estrogen?

After menopause, much of the body's estrogen is produced when the aromatase enzyme converts adrenal androgens into estrone and estradiol. Anastrozole inhibits aromatase and lowers estrogen production in peripheral tissues and breast cancer tissue. Lower estrogen levels reduce stimulation of hormone-sensitive breast cancer cells.

When Is Anastrozole Used for Breast Cancer?

Anastrozole is used in postmenopausal women for hormone receptor-positive early breast cancer after initial treatment. It is also used as first-line treatment for hormone receptor-positive or hormone receptor-unknown locally advanced or metastatic disease. Another labeled use covers advanced breast cancer that has progressed after tamoxifen therapy.

How Are Anastrozole Tablets Taken?

The recommended dose is one 1 mg tablet by mouth once daily. The tablet can be taken with or without food. Dose adjustment is not required for kidney impairment or stable liver cirrhosis under current labeling. Anastrozole has not been studied in people with severe liver impairment.

What Safety Concerns Are Linked to Anastrozole?

Anastrozole lowers estrogen and can decrease bone mineral density, increasing fracture risk. Other concerns include elevated cholesterol, ischemic cardiovascular events in women with pre-existing ischemic heart disease, and fetal harm. Common reactions include hot flashes, joint pain, weakness, nausea, headache, osteoporosis, and back pain. Tamoxifen and estrogen-containing products can reduce anastrozole activity.

Frequently Asked Questions About Anastrozole

Is anastrozole an aromatase inhibitor?

Yes. Anastrozole blocks aromatase, an enzyme involved in estrogen production after menopause.

How often is anastrozole taken?

The labeled dose is one 1 mg tablet by mouth once daily.

Can anastrozole affect bone density?

Yes. Lower estrogen levels during treatment can decrease bone mineral density and raise fracture risk.

Is anastrozole used with tamoxifen?

No. Current labeling states that tamoxifen should not be used together with anastrozole.

References

Anastrozole. MedlinePlus. https://medlineplus.gov/druginfo/meds/a696018.html. Date Accessed September 14, 2026.

Anastrozole. National Cancer Institute. https://www.cancer.gov/about-cancer/treatment/drugs/anastrozole. Date Accessed September 14, 2026.

DailyMed - ANASTROZOLE tablet. https://www.dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ca9d4aff-ffdf-4a46-ad20-e47e5886a19e. Date Accessed September 14, 2026.

DailyMed - ARIMIDEX (anastrozole) tablet. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=acbfaaa9-503c-4691-9828-76a7146ed6de. Date Accessed September 14, 2026.

FDALabel - Anastrozole. https://nctr-crs.fda.gov/fdalabel/ui/spl-summaries/criteria/388033. Date Accessed September 14, 2026.