Trade Names:Aromasin- Tablets for oral use 25 mg
An irreversible, steroidal aromatase inactivator. It lowers circulating estrogen concentrations in postmenopausal women. Exemestane is 90% bound to plasma proteins. Exemestane is extensively metabolized.
Rapidly absorbed. At least 42% if the dose is absorbed. T max is 1.2 h (women with breast cancer) and 2.9 h (healthy women). When taken after a high-fat breakfast, the plasma levels increased approximately 40%.
90% protein bound.
Extensively metabolized. CYP3A4 is the principal isoenzyme involved in the oxidation of exemestane. The metabolites are inactive or inhibit aromatase with decreased potency compared to exemestane.
The t 1/2 is 24 h. Approximately 42% is excreted in the urine and approximately 42% is excreted in the feces. Less than 1% is excreted unchanged in the urine.
AUC is about 3 times higher in those with moderate or severe renal insufficiency. No dosage adjustment necessary.Hepatic Function Impairment
AUC increased approximately 3 times in those with moderate or sever hepatic insufficiency. No dosage adjustment necessary.
Advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy.
Prevention of prostate cancer.
PO 25 mg once daily.
Store at controlled room temperature.
A possible decrease of exemestane by agents which inhibit or induce CYP-450 3A4 (eg, rifampin, phenobarbital, erythromycin, ketoconazole).
None well documented.
Chest pain; hypertension; peripheral edema.
Fatigue; depression; insomnia; anxiety; headache; dizziness.
Rash; increased sweating; androgenic effects reported including hypertrichosis, hair loss, and acne.
Hot flushes; weight gain.
Low potential for nausea and vomiting; abdominal pain; anorexia; constipation; diarrhea; and increased appetite.
Musculoskeletal pain; arthralgia.
Flu-like symptoms with fever; hoarseness.
Category D .
Safety and efficacy not established in patients younger than 18 yr of age.
Increases in testosterone and androstenedione levels observed.
Do not administer exemestane tablets to premenopausal women.
Approximately 20% of patients receiving exemestane in clinical studies experienced common toxicity criteria. Grade 3 or 4 lymphocytopenia.
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