Class: Aromatase inhibitor
- 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.
Special PopulationsRenal Function Impairment
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.
Indications and Usage
Advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy.
Prevention of prostate cancer.
Known hypersensitivity to any component of the product; women who are or may become pregnant.
Dosage and AdministrationBreast Cancer
PO 25 mg once daily after a meal.Concomitant therapy
In patients taking a potent CYP3A4 inducer (eg, phenytoin, rifampin), increase exemestane to 50 mg once daily after a meal.
Store at controlled room temperature.
Drug InteractionsAgents that inhibit or induce CYP3A4 (eg, rifampin, phenobarbital, erythromycin, ketoconazole, and others)
A possible decrease of exemestane by agents which inhibit or induce CYP3A4 (eg, rifampin, phenobarbital, erythromycin, ketoconazole).
Laboratory Test Interactions
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 X . Contraindicated in women who are or may become pregnant.
Safety and efficacy not established in patients younger than 18 y.
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.
- Androgenic effects have been reported with exemestane. Inform patients that hypertrichosis, hair loss, acne, or hoarseness may occur.
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