Aromasin (exemestane) represents a significant advancement in endocrine therapy for hormone-sensitive breast cancer in postmenopausal women. As a third-generation, irreversible steroidal aromatase inhibitor, it offers targeted estrogen suppression with a distinct mechanism of action compared to non-steroidal inhibitors. This medication works by permanently binding to the aromatase enzyme, effectively blocking the conversion of androgens to estrogen throughout body tissues. Clinical evidence demonstrates its efficacy in both adjuvant and advanced settings, providing healthcare professionals with a powerful tool for managing estrogen receptor-positive malignancies while maintaining a generally favorable safety profile.

Features

• Contains 25mg exemestane per tablet
• Irreversible, steroidal aromatase inhibition
• Once-daily oral administration
• Bioavailability of approximately 42% following oral administration
• Mean terminal elimination half-life of approximately 24 hours
• Extensive metabolism primarily via CYP3A4 isoenzyme
• Excretion primarily through hepatobiliary routes

Benefits

• Significantly reduces circulating estrogen levels in postmenopausal women
• Demonstrates proven efficacy in reducing cancer recurrence in adjuvant therapy
• Provides effective treatment for advanced breast cancer in postmenopausal women
• Offers irreversible enzyme inhibition for sustained therapeutic effect
• Maintains bone mineral density better than some alternative therapies
• Generally well-tolerated with manageable side effect profile

Common use

Aromasin is primarily indicated for the treatment of estrogen receptor-positive early breast cancer in postmenopausal women who have received 2-3 years of tamoxifen and are switched to complete a total of 5 consecutive years of adjuvant endocrine therapy. It is also approved for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy. The medication may be used in combination with ovarian suppression in premenopausal women with hormone receptor-positive early breast cancer, though this represents an off-label application requiring careful clinical consideration.

Dosage and direction

The recommended dosage of Aromasin is 25mg administered orally once daily after a meal. Treatment should continue until tumor progression is observed in advanced disease settings. For adjuvant treatment of early breast cancer, the recommended duration is 2-3 years following initial tamoxifen therapy to complete 5 years of total endocrine therapy. Tablets should be swallowed whole with water and may be taken at any time of day, though consistency in timing is recommended to maintain stable drug levels. No dosage adjustment is necessary for elderly patients, but careful monitoring is advised in those with hepatic or renal impairment.

Precautions

Patients should undergo comprehensive baseline assessment including bone mineral density evaluation before initiating therapy due to the potential for accelerated bone loss. Regular monitoring of lipid profiles is recommended as aromatase inhibitors may affect cholesterol metabolism. Hepatic function should be assessed periodically, particularly in patients with pre-existing liver conditions. Caution is advised in patients with osteoporosis or those at increased risk of fractures. Vitamin D and calcium supplementation should be considered, along with regular weight-bearing exercise to maintain bone health. Patients should be advised about potential effects on cholesterol levels and cardiovascular health.

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 unless they are receiving concomitant luteinizing hormone-releasing hormone (LHRH) agonist therapy. The medication is contraindicated in pregnant women due to potential fetal harm and should not be used during breastfeeding. Patients with severe hepatic impairment should avoid Aromasin therapy unless closely monitored by a healthcare professional. Concomitant use with estrogen-containing medications is contraindicated as it may interfere with pharmacological activity.

Possible side effects

The most frequently reported adverse reactions include hot flashes (approximately 22% of patients), fatigue (16%), arthralgia (15%), headache (13%), insomnia (11%), and increased sweating (10%). Musculoskeletal pain and stiffness affect approximately 29% of patients, while nausea occurs in approximately 13% of cases. Less common but potentially serious side effects include osteoporosis and fractures (occurring in approximately 10% of patients after extended therapy), cardiovascular events, and elevated cholesterol levels. Dermatological reactions such as rash may occur in approximately 8% of patients. Regular monitoring can help detect and manage these effects early.

Drug interaction

Aromasin is primarily metabolized by CYP3A4, and coadministration with strong CYP3A4 inducers such as rifampicin, phenytoin, or St. John’s Wort may significantly decrease exemestane concentrations. Conversely, strong CYP3A4 inhibitors like ketoconazole may increase exemestane levels. Estrogen-containing therapies may interfere with Aromasin’s pharmacological action and should be avoided. Caution is advised when administering with other medications that affect bone metabolism, such as corticosteroids. The medication may interact with drugs that affect cholesterol metabolism, requiring closer monitoring of lipid profiles when used concomitantly with statins or other lipid-lowering agents.

Missed dose

If a dose is missed, patients should take it as soon as remembered unless it is nearly time for the next scheduled dose. In such cases, the missed dose should be skipped and the regular dosing schedule resumed. Patients should never take a double dose to make up for a missed one. Maintaining a consistent dosing schedule is important for optimal therapeutic effect, and patients may benefit from using pill organizers or reminder systems to improve adherence. Healthcare providers should discuss missed dose management during patient education sessions.

Overdose

There is limited experience with Aromasin overdose in humans. Single doses up to 800mg have been administered without significant adverse effects. In case of suspected overdose, symptomatic and supportive care is recommended. Gastric lavage may be considered if performed soon after ingestion. Since exemestane is highly protein-bound, dialysis is unlikely to be effective. Medical supervision should be provided with particular attention to potential gastrointestinal effects. There is no specific antidote for exemestane overdose, and treatment should focus on managing symptoms while providing supportive care.

Storage

Aromasin tablets should be stored at room temperature between 15°C and 30°C (59°F and 86°F) in their original container. The medication must be protected from light and moisture and kept in a tightly closed container. Tablets should not be stored in bathroom cabinets or other areas prone to humidity fluctuations. Keep out of reach of children and pets. Do not use tablets that appear discolored, damaged, or beyond their expiration date. Proper storage conditions help maintain drug stability and efficacy throughout the treatment period.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Aromasin is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Individual patient responses may vary, and treatment decisions should be based on comprehensive clinical evaluation. Patients should consult their healthcare provider for personalized medical advice and report any adverse effects promptly. The information presented here reflects current medical knowledge but may not encompass all recent developments or individual variations in response.

Reviews

Clinical studies demonstrate that Aromasin achieves significant reductions in disease recurrence compared to continued tamoxifen therapy. The Intergroup Exemestane Study showed a 32% reduction in the risk of recurrence when patients were switched to exemestane after 2-3 years of tamoxifen. Patients generally report manageable side effects, with musculoskeletal symptoms being the most commonly cited challenge in long-term therapy. Healthcare providers note the medication’s efficacy in estrogen suppression while appreciating its distinct steroidal structure and irreversible mechanism of action. Ongoing research continues to explore optimal sequencing strategies and combination approaches in endocrine therapy regimens.