Systemic Therapy Program

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Document Type

Drug Monographs
Treatment Regimens

Scientific Name:
EXEMESTANE
Brand Name(s):
Aromasin®

Drug Monograph

Pharmacology

Mechanism of Action

Exemestane is an irreversible, steroidal aromatase inhibitor. No detectable effect on synthesis of adrenal corticosteroids or aldosterone. It inhibits the activity of aromatase, the principal enzyme responsible for the conversion of androstenedione to estrone, and testosterone to estradiol. Structurally related to androstenedione, one of the usual aromatase substrates, exemestane inactivates the enzyme by irreversibly binding to the active site on aromatase.

Pharmacokinetics

Oral Absorption:
rapidly and moderately well (about 42%), reaching peak concentrations in ~1 hour; taking after a high fat meal increases the absorption ~ 40%.
Distribution:
extensive; excretion in breast-milk unknown
cross blood brain barrier? No information
Vd:  no information
PPB ~90%, primarily to albumin and a1-acid glycoprotein
Metabolism:
hepatic, oxidation by CTP 450 3A4 followed by reduction; metabolites have little, or no, activity
Excretion:
hepatic: 36% to 48% renal: 39% to 45% urine: <1% unchanged
t½  24 hours 
Cl: no information

Side Effects

EARLY ONSET  (days to weeks)
   hot flushes (13-21%)
   nausea (9%), increased appetite (3%)
   fatigue (8-16%)
   arthralgia (15%), headache (13%)
   insomnia (12%), anxiety (10%), depression (6%), dizziness (9%)
   increased sweating (hyperhidrosis 4-12%), alopecia (15%)
* cardiac ischemic events (myocardial infarction, angina, myocardial ischemia- Rare-1.6%)
* cardiac failure (Rare- 0.4%)
   dyspnea (10%)
   hypertension (10%)
DELAYED/LATE ONSET (weeks to years)
   osteoporosis (5%), bone fracture (4%)

Therapeutics

Approved Indications

Breast cancer

Routes

Oral

Dosing

Oral:
• 25 mg PO once daily.
• Administer with food, after breakfast.

Pediatric: Safety & effectiveness not established

Contraindications

• Hypersensitivity to exemestane or any component; pregnancy; premenopausal women.

Monitoring

Clinical Monitoring

NO RECOMMENDED TOXICITY RATINGS.

Significant Interactions

Estrogen-containing drugs • CYP 3A4 substrate drugs

Product Information

Commercial Product Description

Small, light grey tablets.

Handling Risk Level

Pregnancy DKNOWN HAZARDOUS DRUG
FDA Pregnancy Risk Factor D

  • This drug must be handled using precuations outlined in CCNS Policies for Occupational Safety and Administering Cancer Chemotherapy

Note

HANDLING RISK LEVEL:

HAZARD RISK LEVEL 2
FDA Pregnancy Risk Factor D
• This drug must be handled using precautions outlined in CCNS Policies for Preparing Cancer Chemotherapy and Administering Cancer Chemotherapy and the CCNS Standard for Oral Systemic Therapy for Cancer
• Go to "Additional Information" tab (above) for links to CCNS Policies

SERIOUS WARNINGS:

Not recommended for use in pre-menopausal women as safety and efficacy have not been established in these patients.

Potential risk/benefit should be carefully assessed in patients with osteoporosis or risk factors for osteoporosis.

Availability & Funding

Administrative Information (Nova Scotia)

• CCNS Provincial Formulary Status- Community Level • Take Home Prescription- As per Guidelines • Go to "Additional Information" tab (above) for links to the Provincial Formulary of Cancer Drugs • Pharmacare Formulary Status- Non-Formulary



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