Anastrozole

Aromatase inhibitor (non-steroidal), Antineoplastic, Endocrine therapy

Anastrozole

Arimidex

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Summary

Classes

Aromatase inhibitor (non-steroidal), Antineoplastic, Endocrine therapy

Common uses

Adjuvant treatment of hormone receptor-positive breast cancer in postmenopausal women▲0▼, Advanced ER-positive breast cancer (postmenopausal)▲0▼, Breast cancer risk reduction (selected high-risk postmenopausal women)▲0▼

Pharmacy

Starting dose

1 mg PO once daily

Preparations

1 mg tablets

US FDA Max

1 mg/d

Pharmacology

Routes

Oral

Onset

Estrogen suppression within days; clinical effect over months

Duration

24 hours

Half-life

~50 hours

Bioavailability

High (oral; not significantly affected by food)

Pregnancy

Contraindicated in pregnancy (only used in postmenopausal women); D class historically.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Anastrozole is a selective non-steroidal aromatase inhibitor; it reversibly binds the CYP19 (aromatase) enzyme that converts adrenal androgens to estrogens in peripheral tissues (the principal source of estrogen after menopause), producing >97% estrogen suppression in postmenopausal women.▲0▼ Not effective in premenopausal women because ovarian aromatase is gonadotropin-driven and not adequately suppressed by AI alone. Adverse effects reflect estrogen withdrawal: hot flashes, arthralgias (the "AI joint syndrome"), vaginal dryness, accelerated bone loss (DEXA monitoring; bisphosphonate/denosumab co-therapy common), and modestly increased ischemic CV events in some analyses.