Aromasin: Advanced Estrogen Control for Breast Cancer Therapy
Aromasin
| Product dosage: 25mg | |||
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Synonyms | |||
Aromasin (exemestane) is a potent, steroidal aromatase inactivator specifically designed for the treatment of estrogen receptor-positive breast cancer in postmenopausal women. As a third-generation aromatase inhibitor, it irreversibly binds to the aromatase enzyme, leading to a significant and sustained reduction in circulating estrogen levels—a key driver in hormone-sensitive tumor growth. Its selective mechanism offers a targeted approach to endocrine therapy, making it a cornerstone in both adjuvant and advanced settings. Clinical evidence supports its efficacy in reducing recurrence risk and improving survival outcomes, establishing it as a critical component in modern oncology 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 elimination
Benefits
- Significantly reduces estrogen synthesis by permanently disabling the aromatase enzyme
- Lowers the risk of breast cancer recurrence in adjuvant therapy
- Improves progression-free survival in advanced metastatic disease
- Favorable long-term safety profile compared to earlier generation inhibitors
- Oral administration allows for convenient once-daily dosing
- May preserve bone density better than non-steroidal inhibitors in some patient profiles
Common use
Aromasin is primarily indicated for the adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer who have received 2–3 years of tamoxifen and are switched to complete a total of 5 years of adjuvant hormonal therapy. It is also approved for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy. Off-label uses may include estrogen suppression in other clinical scenarios under specialist supervision.
Dosage and direction
The recommended dosage is one 25 mg tablet taken orally once daily after a meal. Administration with food enhances absorption and reduces gastrointestinal discomfort. Treatment should continue for the duration prescribed by the oncology team, typically until disease progression or completion of adjuvant therapy. Dosage adjustment is not required for elderly patients but should be carefully considered in those with hepatic impairment. Tablets should be swallowed whole and not crushed or divided.
Precautions
Patients should undergo comprehensive baseline assessment including bone mineral density testing due to the potential for accelerated bone loss. Regular monitoring of lipid profiles is recommended. Caution is advised in patients with pre-existing hepatic or renal impairment. Patients should be advised about potential dizziness and cautioned against driving or operating machinery until they know how Aromasin affects them. Vitamin D and calcium supplementation is often recommended prophylactically.
Contraindications
Aromasin is contraindicated in premenopausal women, pregnant or breastfeeding women, and patients with known hypersensitivity to exemestane or any component of the formulation. It must not be used in patients with severe hepatic impairment (Child-Pugh Class C) or in combination with estrogen-containing therapies. Concomitant use with other aromatase inhibitors or estrogen receptor blockers is not recommended.
Possible side effects
Most common adverse reactions (≥10%) include:
- Hot flashes (≈25%)
- Fatigue (≈16%)
- Arthralgia (≈15%)
- Headache (≈13%)
- Insomnia (≈12%)
- Increased sweating (≈11%)
Less common but serious side effects may include:
- Osteoporosis and fractures
- Cardiovascular events
- Elevated cholesterol levels
- Depression and mood changes
- Hepatitis and liver enzyme elevations
- Visual disturbances
Drug interaction
Strong CYP3A4 inducers (rifampicin, carbamazepine, St. John’s wort) may significantly decrease exemestane concentrations. Concomitant use with estrogen-containing therapies may diminish its therapeutic effect. Caution is advised with other medications that affect bone metabolism (corticosteroids, thyroid replacements). Monitor patients taking warfarin due to potential INR changes.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next dose. In that case, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed tablet. Maintain consistent daily timing for optimal therapeutic effect.
Overdose
There is limited experience with acute overdose. Single doses up to 800 mg have been tolerated with no severe effects. Management should be symptomatic and supportive. Gastric lavage may be considered if ingestion occurred within 2 hours. Monitor vital signs and provide appropriate symptomatic treatment. Dialysis is unlikely to be effective due to high protein binding.
Storage
Store at room temperature (20–25°C or 68–77°F) in the original container. Protect from light and moisture. Keep tightly closed and out of reach of children. Do not use after the expiration date printed on the packaging. Do not transfer tablets to other containers as this may affect stability.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient characteristics. Always follow the prescribing information provided with the medication and consult with your oncology team regarding any questions or concerns about therapy.
Reviews
Clinical trials demonstrate Aromasin’s significant efficacy in breast cancer treatment. The TEAM trial showed superior disease-free survival compared to tamoxifen, while the IES study demonstrated a 32% reduction in recurrence risk when switching to exemestane after 2–3 years of tamoxifen. Real-world evidence supports maintained efficacy with generally manageable side effect profiles, though individual experiences with arthralgia and vasomotor symptoms vary. Ongoing research continues to refine its role in combination therapies and extended adjuvant treatment.