Aromasin (exemestane) is a potent, steroidal aromatase inactivator indicated for the adjuvant treatment of postmenopausal women with estrogen receptor-positive early breast cancer. It functions by irreversibly binding to the aromatase enzyme, leading to a significant and sustained reduction in circulating estrogen levels—a key driver in hormone-sensitive tumor proliferation. This agent represents a critical component in the endocrine therapy arsenal, offering a well-tolerated and effective strategy for long-term disease management. Clinical evidence supports its use both in extended adjuvant settings and for advanced breast cancer, establishing it as a cornerstone in modern hormonal treatment protocols.

Features

• Active ingredient: Exemestane 25 mg
• Pharmacological class: Irreversible, steroidal aromatase inactivator
• Administration: Oral tablet
• Bioavailability: Approximately 42% following oral administration
• Half-life: 24 hours
• Metabolism: Primarily hepatic via CYP3A4
• Excretion: Urinary and fecal
• FDA-approved for adjuvant and advanced breast cancer therapy

Benefits

• Significantly reduces the risk of cancer recurrence in hormone-sensitive early breast cancer
• Demonstrates superior efficacy compared to tamoxifen in extended adjuvant settings
• Offers a favorable side effect profile with lower incidence of thromboembolic events compared to antiestrogens
• Does not require concomitant corticosteroid replacement
• Provides convenient once-daily dosing supporting long-term adherence
• Shows no evidence of cumulative toxicity with extended use

Common use

Aromasin is primarily prescribed for the treatment of estrogen receptor-positive breast cancer in postmenopausal women. It is indicated both as adjuvant therapy following 2–3 years of tamoxifen treatment and as first-line therapy for advanced or metastatic disease. Clinicians may also utilize it as extended adjuvant therapy beyond the initial 5 years of endocrine treatment. Off-label uses include estrogen suppression in fertility treatments and management of gynecomastia, though these applications require careful risk-benefit assessment.

Dosage and direction

The recommended dosage is one 25 mg tablet taken orally once daily after a meal. Administration with food enhances bioavailability by approximately 40%. Treatment should continue for the duration prescribed, typically 5 years in adjuvant settings or until disease progression in advanced cases. Tablets should be swallowed whole and not crushed or divided. Dosage adjustment is generally not required for elderly patients but should be considered in those with severe hepatic impairment.

Precautions

Patients should undergo comprehensive bone density assessment before initiation and during treatment due to the accelerated bone mineral density loss associated with estrogen suppression. Regular monitoring of lipid profiles is recommended. Caution is advised in patients with pre-existing hepatic or renal impairment. Patients should be advised that Aromasin is not indicated for premenopausal women and may reduce the effectiveness of estrogen-containing therapies. Driving or operating machinery should be avoided if dizziness occurs.

Contraindications

Aromasin is contraindicated in patients with known hypersensitivity to exemestane or any component of the formulation. It must not be administered to premenopausal women, pregnant women, or nursing mothers. Concomitant use with estrogen-containing therapies is contraindicated. Patients with severe hepatic impairment (Child-Pugh Class C) should not receive this medication without careful risk assessment.

Possible side effects

Most common adverse reactions (≥10%) include hot flashes (21%), fatigue (16%), arthralgia (15%), headache (13%), insomnia (12%), and increased sweating (11%). Less frequent but clinically significant effects may include:

• Osteoporosis and fractures (5-10%)
• Elevated cholesterol (6%)
• Nausea (9%)
• Depression (6%)
• Carpal tunnel syndrome (2%) Rare but serious side effects include hepatitis, anaphylaxis, and severe cutaneous reactions.

Drug interaction

Strong CYP3A4 inducers (rifampicin, phenytoin, carbamazepine) may significantly reduce exemestane concentrations. Concomitant use with estrogen-containing therapies may diminish efficacy. Caution is advised with other medications that affect bone metabolism (corticosteroids, thyroid replacement). No clinically significant interactions have been observed with warfarin, though monitoring is recommended.

Missed dose

If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. Doubling of doses is not recommended. Patients should maintain regular dosing schedule and contact their healthcare provider if multiple doses are missed.

Overdose

No specific antidote exists for exemestane overdose. Single doses up to 800 mg have been tolerated without severe effects. Management should include symptomatic and supportive care. Gastric lavage may be considered if ingestion occurred within 2 hours. Dialysis is unlikely to be effective due to high protein binding.

Storage

Store at room temperature (15-30°C or 59-86°F) in the original container. Protect from light and moisture. Keep out of reach of children and pets. Do not use after the expiration date printed on packaging.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made exclusively by qualified healthcare professionals based on individual patient characteristics. Actual product packaging and inserts contain the most current prescribing information.

Reviews

Clinical trials demonstrate Aromasin’s significant efficacy in breast cancer management. The TEAM trial showed superior disease-free survival compared to tamoxifen, while the MA-17 trial established its benefit in extended adjuvant therapy. Patients report generally good tolerability, though management of arthralgia and bone health requires attention. Oncology guidelines consistently recommend Aromasin as a standard of care in appropriate patient populations.