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Letrozole

FEMARA

Pronunciation: LET-roe-zoel

Letrozole ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Letrozole ballicule
Letrozole FEMARA mascot mnemonic cartoon
Visual mnemonic: Letrozole mascot
“Let Rose show Femme aura”

What it isAromatase inhibitor; hormone receptor-positive breast cancer, and off label for ovulation induction.

Why this oneSuperior disease-free survival to tamoxifen after menopause, and in PCOS it induces ovulation more effectively than clomiphene.

What limits itAccelerated bone loss and arthralgia. Ineffective before menopause unless ovarian function is suppressed.

Letrozole molecular structure (skeletal formula)
Molecular structure: Letrozole

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Breast cancer — adjuvant, extended adjuvant, or advanced (ER+ postmenopausal)Adults2.5 mg QD2.5 mg QD2.5 mg QD

Renal No adjustment if CLcr ≥10 mL/min.

Hepatic No adjustment for mild–moderate; cirrhosis with severe hepatic impairment: reduce 50% to 2.5 mg every other day.

Instructions

Available strengths

Contraindications

Cautions

Adverse reactions

Pregnancy Contraindicated — can cause fetal harm (spontaneous abortion, congenital defects).

Lactation Unknown if in human milk; advise not to breastfeed during and for ≥3 weeks after last dose.

Cost

Letrozole (FEMARA)
What pharmacies pay · NADAC 9/30/26
Strength#/mogeneric $/moCostPlus
2.5 mgtab30 qd$4.35offered

Generic entry2008

NO BOXED WARNINGS

Principal riskAccelerated bone loss and arthralgia

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk3 / 4

Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent

Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.

Open Letrozole in the interactive console ↗

Memory aids: interaction avatars

Letrozole CYP2D6 substrate avatar mnemonic
CYP2D6 substrate
Letrozole CYP3A4 substrate avatar mnemonic
CYP3A4 substrate

Open Letrozole in the interactive console ↗