Supo aromasin 25mg – exemestane
Mechanism of action
Exemestane is an irreversible steroidal aromatase inhibitor. It binds covalently to the aromatase enzyme (CYP19A1), permanently deactivating it and preventing the conversion of androgens (testosterone and androstenedione) into estrogens (estradiol and estrone). This leads to a marked reduction in circulating estrogen levels, which is useful in conditions driven by estrogen excess.
Indications
Males: Used off‑label for estrogen control in men undergoing anabolic‑androgenic steroid (AAS) cycles, to prevent gynecomastia and maintain a favorable testosterone‑to‑estrogen ratio. Also employed in the treatment of estrogen‑dependent breast cancer in men (rare).Females: FDA‑approved for the treatment of hormone‑receptor‑positive breast cancer in post‑menopausal women, both as adjuvant therapy and for metastatic disease.
Contraindications
- Known hypersensitivity to exemestane or any of its excipients.
- Pregnant or breastfeeding women (exemestane can cause fetal harm and is excreted in milk).
- Severe hepatic impairment (exemestane is metabolized in the liver).
Side effects
Common: hot flashes, headache, fatigue, arthralgia, nausea, and mild elevations in liver enzymes.Less common but serious: severe hepatic dysfunction, thromboembolic events, and bone mineral density loss with long‑term use.
Drug interactions
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase exemestane plasma levels.
- CYP3A4 inducers (e.g., rifampin, carbamazepine) may reduce its efficacy.
- Concurrent use with other aromatase inhibitors provides no additional benefit and increases toxicity risk.
Dosage
Standard oral dose for breast cancer: 25 mg once daily, taken with or without food. For off‑label estrogen control in men, the same 25 mg daily dose is commonly used, though some protocols split the dose (e.g., 12.5 mg twice daily) to reduce gastrointestinal upset.
Storage
Store at controlled room temperature (15‑30 °C). Protect from moisture and direct sunlight. Keep out of reach of children.
Regulatory compliance statements
Exemestane is approved by major regulatory agencies (FDA, EMA) for breast cancer treatment and is manufactured under Good Manufacturing Practices (GMP).
Safety information
Overdose instructions: Seek immediate medical attention; symptomatic treatment may include activated charcoal and supportive care.Adverse reactions: Report any severe or unexpected reactions to a healthcare professional promptly.