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Trade Names:
Aromasin
- Tablets for oral use 25 mg

Mechanism of Action

Pharmacology

An irreversible, steroidal aromatase inactivator. It lowers circulating estrogen concentrations in postmenopausal women. Exemestane is 90% bound to plasma proteins. Exemestane is extensively metabolized.

Pharmacokinetics

Absorption

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%.

Distribution

90% protein bound.

Metabolism

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.

Elimination

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 Populations

AUC is about 3 times higher in those with moderate or severe renal insufficiency. No dosage adjustment necessary.

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.

Unlabeled Uses

Prevention of prostate cancer.

Contraindications

Standard considerations.

Dosage and Administration

PO 25 mg once daily.

Storage/Stability

Store at controlled room temperature.

Drug Interactions

A possible decrease of exemestane by agents which inhibit or induce CYP-450 3A4 (eg, rifampin, phenobarbital, erythromycin, ketoconazole).

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Chest pain; hypertension; peripheral edema.

CNS

Fatigue; depression; insomnia; anxiety; headache; dizziness.

Dermatologic

Rash; increased sweating; androgenic effects reported including hypertrichosis, hair loss, and acne.

Endocrine

Hot flushes; weight gain.

GI

Low potential for nausea and vomiting; abdominal pain; anorexia; constipation; diarrhea; and increased appetite.

Hematologic

Lymphopenia.

Musculoskeletal

Musculoskeletal pain; arthralgia.

Respiratory

Dyspnea; coughing.

Miscellaneous

Flu-like symptoms with fever; hoarseness.

Precautions

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy not established in patients younger than 18 yr of age.

Endocrine effects

Increases in testosterone and androstenedione levels observed.

Premenopausal women

Do not administer exemestane tablets to premenopausal women.

Lymphocytopenia

Approximately 20% of patients receiving exemestane in clinical studies experienced common toxicity criteria. Grade 3 or 4 lymphocytopenia.

Patient Information

• Androgenic effects have been reported with exemestane. Inform patients that hypertrichosis, hair loss, acne, or hoarseness may occur.