Aromasin (exemestane) dosing, indications, interactions, adverse effects, and more

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Sections exemestane
Dosing & Uses
Interactions
Adverse Effects
Warnings
Pregnancy
Pharmacology
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

25mg

Postmenopausal ER-Positive Breast Cancer

25 mg PO qDay; continue until tumor progression

Breast Cancer Adjuvant Treatment

Switch to exemestane after 2-3 years of tamoxifen treatment

25 mg PO qDay; continue until tumor progression

Take after meals

Breast Cancer Prevention (Off-label)

2013 ASCO guidelines suggest exemestane as an alternative to tamoxifen or raloxifene to prevent invasive breast cancer in high risk women

25 mg PO qDay for 5 years

Dosage Modifications

Coadministration with potent CYP3A4 inducers: 50 mg PO qDay

Dosing Considerations

High risk of breast cancer is defined as at least 1 breast biopsy showing lobular carcinoma in situ (LCIS) or atypical hyperplasia, 1 or more first-degree relatives with breast cancer, or a 5-year predicted risk of breast cancer >1.66% (based on the modified Gail model)

Safety and efficacy not established

Interaction Checker

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Contraindicated

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>10%

Fatigue (22%)

Nausea (18%)

Hot flashes (13%)

Depression (13%)

Pain (13%)

Insomnia (11%)

1-10%

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%)

<1%

Cardiac failure

Uterine polyps

Endometrial hyperplasia

Gastric ulcer

Frequency not defined

Hepatitis

Visual disturbances

Postmarketing Reports

Immune system disorders: Hypersensitivity

Hepatobiliary disorders: Hepatitis including cholestatic hepatitis

Nervous system disorder: Paresthesia

Skin and subcutaneous tissue disorders: Acute generalized exanthematous pustulosis, urticaria, pruritus

Contraindications

Hypersensitivity

Cautions

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 & 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

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Aromatase inhibitor - blocks conversion of androgens to estrogens by binding to the heme group of aromatase enzyme, which in turn inhibits its activity

Pharmacokinetics

Half-Life: 24 hr

Protein Bound: 90%

Peak time: 1.2 (women with breast cancer)

Metabolism: via CYP3A4 (extensive)

Excretion: Urine (39-45%); feces (35-48%)

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Patient Handout

Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

View explanations for tiers and restrictions

Tier	Description
1	This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2	This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3	This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4	This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5	This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6	This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC	NOT COVERED – Drugs that are not covered by the plan.

Code	Definition
PA	Prior Authorization Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL	Quantity Limits Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST	Step Therapy Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR	Other Restrictions Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.

Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.

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Sections exemestane
Dosing & Uses
Interactions
Adverse Effects
Warnings
Pregnancy
Pharmacology
Images
Patient Handout
Formulary

exemestane (Rx)