- Hormone receptor-positive (HR+) early breast cancer
- In postmenopausal women after 2–3 years of tamoxifen → complete 5 years total of adjuvant therapy
- Advanced or metastatic HR+ breast cancer in postmenopausal women
- After progression on tamoxifen or other antiestrogens
Dose: 25 mg orally once daily, after a meal,Continue treatment until disease progression or unacceptable toxicity
- In early breast cancer: typically 24–36 months, following tamoxifen
For advanced breast cancer: until progression
- Tablets: 25 mg
- Take after food (improves absorption)
- Take at the same time each day
- Do not crush or chew tablet
- Used only in postmenopausal women
- Ensure menopausal status is confirmed before use
- Class: Irreversible steroidal aromatase inhibitor (aka “suicide inhibitor”)
- Mechanism of Action:
- Blocks conversion of androgens to estrogens in peripheral tissues
- ↓ Estrogen levels → starves estrogen-dependent tumor cells
- Pharmacokinetics:
- Oral bioavailability: ↑ with food
- Metabolized by liver (CYP3A4, aldoketoreductases)
- Half-life: ~24 hours
- Excretion: Urine and feces
- Hot flashes
- Fatigue
- Sweating
- Nausea
- Dizziness
- Headache
- Arthralgia/myalgia
- Insomnia
- Premenopausal women
- Pregnancy or lactation
- Hypersensitivity to exemestane or components
- CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine): may ↓ exemestane levels
- Estrogen-containing therapies (e.g., HRT) antagonize effect—should be avoided
- Does not inhibit CYP enzymes significantly, so minimal interactions
Drug Status
Availability | |
Pregnancy | |
Breastfeeding | |
Schedule |
BRAND NAME | STRENGTH | FORMULATION | PACK SIZE | MANUFACTURER | DISTRIBUTOR |
---|---|---|---|---|---|
Aromasin | 25mg | Tablet | 30’s | Pfizer Labs | Pfizer Labs |