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What Is Letrozole?

Letrozole is a prescription aromatase inhibitor used in postmenopausal women with selected hormone-sensitive breast cancers. Current tablets contain 2.5 mg. Labeling includes adjuvant treatment of hormone receptor-positive early breast cancer, extended adjuvant treatment after prior tamoxifen, and first- or second-line treatment of selected advanced breast cancer.

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What Is Letrozole?

Letrozole is a prescription aromatase inhibitor used in postmenopausal women with selected hormone-sensitive breast cancers. Current tablets contain 2.5 mg. Labeling includes adjuvant treatment of hormone receptor-positive early breast cancer, extended adjuvant treatment after prior tamoxifen, and first- or second-line treatment of selected advanced breast cancer.

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How Does Letrozole Lower Estrogen?

Letrozole inhibits aromatase, the enzyme that converts adrenal androgens to estrogens in peripheral tissues. Lower estrogen concentrations reduce stimulation of estrogen-dependent breast cancer cells.

Who Is Treated With Letrozole?

Letrozole is used in postmenopausal women with hormone receptor-positive early breast cancer, selected early breast cancer after prior adjuvant tamoxifen, or hormone receptor-positive or unknown advanced breast cancer under current labeling. Pregnancy and known hypersensitivity are contraindications.

How Is Letrozole Dosed?

The recommended dose is 2.5 mg by mouth once daily with or without food. Patients with cirrhosis and severe hepatic impairment receive 2.5 mg every other day. Advanced breast cancer treatment continues until tumor progression.

What Serious Risks Are Linked to Letrozole?

Letrozole can reduce bone mineral density and increase fracture and osteoporosis risk. It can also increase cholesterol and cause fatigue, dizziness, and somnolence. Letrozole can cause fetal harm and is contraindicated during pregnancy.

Frequently Asked Questions About Letrozole

What conditions does letrozole treat?

Letrozole treats selected early and advanced breast cancers in postmenopausal women.

What is the usual letrozole dose?

The recommended dose is 2.5 mg once daily.

Does severe hepatic impairment change the dose?

Yes. Patients with cirrhosis and severe hepatic impairment receive 2.5 mg every other day.

Can letrozole affect bone density?

Yes. Letrozole can reduce bone mineral density and increase osteoporosis and fracture risk.

References

DailyMed - LETROZOLE tablet, film coated. https://www.dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cb1da0ac-8db1-4482-824d-430511d1b7a0. Date Accessed October 12, 2026.

Letrozole. LiverTox. https://www.ncbi.nlm.nih.gov/books/NBK548381/. Date Accessed October 12, 2026.

Letrozole. MedlinePlus. https://www.medlineplus.gov/druginfo/meds/a698004.html. Date Accessed October 12, 2026.

Letrozole. National Cancer Institute. https://www.cancer.gov/about-cancer/treatment/drugs/letrozole. Date Accessed October 12, 2026.

Letrozole. PubChem. https://pubchem.ncbi.nlm.nih.gov/compound/Letrozole. Date Accessed October 12, 2026.