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OtherIntermediateMedium Risk

Letrozole

Also known as: Femara, Letro

Letrozole is the most potent of the third-generation aromatase inhibitors, capable of suppressing estradiol by up to 98%. It is FDA-approved for breast cancer and used off-label for ovulation induction in fertility treatment, as well as estrogen control during anabolic steroid cycles.

Evidence84/100 — Strong

Risk Level

Medium Risk

Difficulty

Intermediate
CAS Number112809-51-5
Molecular FormulaC17H11N5
ClassOther
CategorySERMs & AIs

Mechanism of Action

Letrozole competitively and reversibly inhibits aromatase (CYP19A1) with approximately 150-fold greater potency than anastrozole in vitro. It suppresses plasma estradiol to near-undetectable levels at clinical doses. Its potency makes it effective for emergency gynecomastia flare management, but also increases the risk of estrogen over-suppression.

Dosing Research

Breast cancer: 2.5 mg/day orally. Ovulation induction: 2.5-7.5 mg/day on cycle days 3-7. On-cycle estrogen management: 0.25-0.5 mg every other day or twice weekly. Half-life is approximately 2 days. Due to its potency, lower doses are generally recommended for estrogen management.

Side Effects & Risks

Joint and musculoskeletal pain are very common. Accelerated bone loss with chronic use. Hot flashes, fatigue, headache. Significant lipid disruption possible. High risk of estrogen crash symptoms (lethargy, depression, erectile dysfunction, dry skin) if overdosed. Should be used with regular blood work monitoring.

Research Studies

Disclaimer

CompoundIQ publishes research summaries for informational and educational purposes only. Nothing on this site constitutes medical advice, diagnosis, or treatment recommendations. Always consult a licensed healthcare provider. Many compounds listed are research chemicals not approved for human use.

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