Anastrozole
ARIMIDEX
What it isAromatase inhibitor blocking peripheral estrogen synthesis; hormone receptor-positive breast cancer in postmenopausal women.
Why this oneUnlike steroidal exemestane, it is reversible and nonsteroidal; it lacks tamoxifen's endometrial-cancer and thrombosis liabilities.
What limits itAccelerated bone loss and arthralgia; monitor density. It is ineffective before menopause unless ovarian function is suppressed.
FDA-approved for
- breast cancer (1995)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Breast cancer (adjuvant early-stage, or advanced) in postmenopausal women | Postmenopausal women | 1 mg QD | 1 mg QD | 1 mg QD |
Renal No adjustment needed
Hepatic Mild-to-moderate impairment: no change; severe impairment: not studied.
Instructions
- Take with or without food
- Advanced breast cancer: continue until tumor progression
Cautions
- Increased ischemic cardiovascular events in women with pre-existing ischemic heart disease
- Decreases in bone mineral density
- Increases in total cholesterol
- Embryo-fetal toxicity
Adverse reactions
- Hot flashes
- Arthralgia/arthritis
- Asthenia
- Back pain
- Nausea
- Hypertension
- Depression
- Osteoporosis / bone fractures
- Rash
Pregnancy May cause fetal harm based on animal findings and mechanism of action; embryo-fetal toxicities in rats; advise effective contraception.
Lactation No data on presence in human milk; because of tumorigenicity in animal studies, breastfeeding is not recommended.
NO BOXED WARNINGS
Principal riskAccelerated bone loss and arthralgia
Cost, est. cash$10–$1,000/month
Generic entry2010
Classes and tags
Clinical profile
Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent
Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.
Mechanism of action: Anastrozole ballicule
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