Important Safety Information
Exemestane is FDA-approved for adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer and for advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy. Exemestane is contraindicated in patients with a known hypersensitivity to the drug or to any of the excipients.
Exemestane can cause fetal harm when administered to a pregnant woman. Females of reproductive potential should use effective contraception during treatment and for one month after the last dose.
Important
Non-Medical Use
Exemestane has no approved indication for bodybuilding or performance enhancement. Non-medical use falls outside approved indications and carries health risks including bone mineral density loss, arthralgia, dyslipidemia, and cardiovascular risk. Product strength and laboratory verification do not establish safety for non-medical use.
Potential Adverse Effects
Bone effects: Reductions in bone mineral density over time are seen with exemestane use. In clinical trials, mean BMD decreased by 3.1% in the lumbar spine and 4.2% in the femoral neck at 24 months. Bone mineral density monitoring is recommended.
Cardiovascular effects: Incidences of cardiac ischemic events (myocardial infarction, angina, and myocardial ischemia) were exemestane 1.6%, tamoxifen 0.6%.
Cholesterol: Plasma HDL cholesterol was decreased 6–9% in exemestane-treated patients. Increased serum cholesterol has been reported.
Common adverse reactions: Hot flushes (21%), fatigue (16%), arthralgia (15%), headache (13%), insomnia (12%), and increased sweating (12%).
Androgenic effects: Due to its steroidal profile, androgenic side effects such as weight gain, acne, and hypertrichosis have been reported, which may lead to tolerance problems, especially with prolonged treatment.
Conditions Requiring Medical Evaluation
Exemestane should be used with caution in patients with pre-existing ischemic heart disease due to increased incidence of ischemic cardiovascular events. Bone mineral density monitoring is recommended. Routine assessment of 25-hydroxy vitamin D levels prior to the start of aromatase inhibitor treatment should be performed.
Monitoring During Therapy
Medically supervised exemestane therapy involves monitoring for adverse effects including bone mineral density changes, cholesterol levels, and cardiovascular events. For patients receiving exemestane with a strong CYP3A4 inducer, the recommended dose is 50 mg once daily after a meal. No dosage adjustment is necessary for patients with renal impairment or for elderly patients. The AUC of exemestane is approximately 3 times higher in subjects with moderate or severe hepatic or renal impairment.
Product Care
Storage & Handling
Store in a cool, dry place away from direct light and moisture. Keep the product in its original packaging and out of the reach of children.
Further Safety Information