Bone mineral density loss (osteoporosis):
Causes progressive reduction in bone density due to oestrogen suppression.
Assess baseline bone mineral density (BMD) prior to treatment and monitor periodically.
Initiate bisphosphonate or calcium/vitamin D therapy if at risk.
Menopausal symptoms / oestrogen deprivation effects:
Common: Hot flushes, fatigue, insomnia, mood changes.
Manage symptomatically; consider lifestyle adjustments or non-hormonal therapies.
Hepatic and renal impairment:
Exposure increases 2–3 fold in hepatic impairment and up to 2-fold in severe renal impairment.
Use with caution and monitor LFTs and renal function regularly.
CYP3A4 interaction potential:
Avoid potent CYP3A4 inducers (e.g., rifampicin, phenytoin, carbamazepine) — may reduce efficacy.
Strong CYP3A4 inhibitors (e.g., ketoconazole) have no significant effect but caution advised.
Pregnancy and lactation:
Contraindicated — teratogenic risk.
Discontinue immediately if taken accidentally during pregnancy.
Generic name: Exemestane
Brand name: Aromasin®
Drug class: Steroidal aromatase inhibitor
Formulation: Sugar-coated tablet
Strength: 25 mg
Mechanism of Action:
Irreversible, steroidal aromatase inhibitor that blocks the conversion of androgens to oestrogens in peripheral tissues, reducing circulating oestrogen levels by >90% in postmenopausal women. No oestrogenic or progestogenic activity; slight androgenic activity at high doses.
Oncology indications:
Advanced oestrogen receptor-positive breast cancer in postmenopausal women whose disease has progressed following anti-oestrogen therapy (e.g., tamoxifen).
Adjuvant treatment of postmenopausal women with oestrogen receptor-positive early breast cancer who have completed at least 2 years of initial adjuvant tamoxifen therapy.
Note: Not for use in premenopausal women.
Recommended dose: 25 mg once daily after a meal.
Duration of therapy:
Advanced breast cancer: Continue until disease progression.
Early breast cancer: Continue until completing a total of 5 years of adjuvant endocrine therapy (tamoxifen followed by Aromasin) or until tumour relapse occurs.
Renal or hepatic impairment: No formal dose adjustment; monitor closely.
Do not use in children.
Hepatic/renal impairment: Monitor for increased toxicity; adjust if required.
Severe adverse reactions (e.g., intolerable fatigue, bone pain, mood changes): Consider temporary interruption or discontinuation.
Progressive disease: Stop therapy.
Avoid with:
CYP3A4 inducers (e.g., rifampicin, phenytoin, carbamazepine, St John’s Wort) — may reduce plasma levels and efficacy.
Oestrogen-containing medicines — antagonise exemestane’s action.
Ketoconazole and other strong CYP3A4 inhibitors: No clinically significant effect, but monitor.
Hypersensitivity to exemestane or excipients
Premenopausal women
Pregnancy and breastfeeding
Concurrent use of oestrogen-containing medications
Baseline and periodic assessments:
Bone mineral density (DEXA scan)
Liver and renal function tests
Menopausal status (LH, FSH, estradiol levels to confirm postmenopausal state)
Clinical review for fatigue, arthralgia, and mood disturbances
| Frequency | Adverse Effect | Management |
|---|---|---|
| Very common (>10%) | Hot flushes, fatigue, insomnia, sweating, headache | Supportive care, lifestyle measures |
| Common (1–10%) | Depression, nausea, diarrhoea, joint pain, dizziness, alopecia | Symptomatic management |
| Uncommon (<1%) | Somnolence, rash, oedema, bone pain | Monitor and treat symptomatically |
| Rare | Hepatic enzyme elevation, lymphopenia | Monitor LFTs and CBC |
Long-term use may cause or worsen osteoporosis — monitor BMD and treat as indicated.
Elderly: No adjustment required.
Hepatic impairment: Increased exposure — monitor closely.
Renal impairment: Increased exposure — use with caution.
Pregnancy/Lactation: Contraindicated.
Premenopausal women: Contraindicated (ineffective and unsafe).
Continue until:
Completion of indicated endocrine treatment duration, or
Disease progression, or
Unacceptable toxicity.
Discontinue if:
Recurrence of cancer during adjuvant use
Severe intolerance or adverse reaction (e.g., significant hepatic enzyme rise or bone fracture)
| Trade Name | |
|---|---|
| Drug Class | Aromatase Inhibitor |
| Cost | |
| Company | |
|---|---|
| Drug Rep | Admin |
| Indications | Breast Cancer |
| Dosage |