Classes
DEA Class; Rx
Common Brand Names; Aromasin
- Antineoplastics, Aromatase Inhibitor
Description
Oral, irreversible, steroidal aromatase inhibitor for early breast cancer (estrogen-receptor positive after 2 to 3 years of tamoxifen therapy) or advanced breast cancer
Lacks cross-resistance with other aromatase inhibitors or tamoxifen; more complete estrogen blockade than anastrazole or letrozole
Similar response rate to megestrol but causes less weight gain and prolongs survival
Indications
Breast Cancer
Advanced disease
- Indicated for treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy
Adjuvant treatment
- Indicated for adjuvant treatment of postmenopausal women with ER+ early breast cancer who have received 2-3 years of tamoxifen treatment and are switched to exemestane
Contraindications
Hypersensitivity
Adverse Effects
- Fatigue (22%)
- Nausea (18%)
- Hot flashes (13%)
- Depression (13%)
- Pain (13%)
- Insomnia (11%)
- Anxiety (10%)
- Dyspnea (10%)
- Dizziness (8%)
- Headache (8%)
- Edema (7%)
- Vomiting (7%)
- Flu-like syndrome (6%)
- Abdominal pain (6%)
- Anorexia (6%)
- Cough (6%)
- Hypertension (5%)
- Constipation (5%)
- Diarrhea (4%)
Warnings
Therapy should not be coadministered with estrogen-containing agents as these could interfere with pharmacological action
Routine assessment of 25-hydroxy vitamin D levels prior to the start of aromatase inhibitor treatment should be performed, due to the high prevalence of vitamin D deficiency in women with early breast cancer; women with vitamin D deficiency should receive supplementation with vitamin D
Reductions in bone mineral density (BMD) seen with therapy over time; during adjuvant treatment with exemestane, women with osteoporosis or at risk of osteoporosis should have their bone mineral density formally assessed by bone densitometry at the commencement of treatment; monitor patients for bone mineral density loss and treat as appropriate
Not indicated for breast cancer in premenopausal women
Advise females of reproductive potential to use effective contraception during treatment and for 1 month after final dose
Based on findings in animals, male and female fertility may be impaired by treatment
Pregnancy and Lactation
Pregnancy Category: X
Lactation: Excretion in milk unknown; because of potential for serious adverse reactions in breast-fed infants, advise women not to breastfeed during treatment and for 1 month after final dose
Maximum Dosage
25 mg/day PO; if a potent CYP3A4 inducer is co-prescribed the maximum is 50 mg/day PO. Higher doses are tolerated but do not result in clinically significant increases in estrogen suppression.
25 mg/day PO; if a potent CYP3A4 inducer is co-prescribed the maximum is 50 mg/day PO. Higher doses are tolerated but do not result in clinically significant increases in estrogen suppression.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Exemestane
tablet
- 25mg
