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At a glance

Exemestane is an aromatase inhibitor used for the treatment of breast cancer in postmenopausal women.

Indications
  • Early Breast Cancer: Adjuvant treatment of postmenopausal ER-positive early breast cancer after 2-3 years of tamoxifen.
  • Advanced Breast Cancer: Treatment of advanced breast cancer in postmenopausal women who have progressed following tamoxifen therapy.
Pharmacology

Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme, causing its inactivation. Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women.

Dosage

Adult Dose (Oral):

  • Advanced or Locally Advanced Breast Cancer: 25 mg once daily (with food).
  • With strong CYP3A4 inducers: 50 mg once daily.
Side effects

Common Side Effects:

  • Insomnia (difficulty in sleeping)
  • Headache
  • Nausea
  • Increased sweating
  • Musculoskeletal pain
  • Fatigue
  • Hot flushes
Use in pregnancy

Use in Pregnancy: Based on animal studies, can cause fetal harm; highly unsafe during pregnancy.

Pregnancy Category: D — always consult a doctor before taking during pregnancy.

Precautions & warnings

Precautions:

  • Exemestane may decrease alertness, affect vision or make you feel sleepy and dizzy; do not drive if these symptoms occur.
  • Used for treatment of hormone dependent breast cancer in postmenopausal women.
  • Take at the same time every day, preferably after food.
  • May cause dizziness and sleepiness; do not drive or do anything requiring concentration until you know how it affects you.
  • Your doctor may regularly check Vitamin D level and bone mineral density and suggest supplements.
  • Reductions in bone mineral density over time are seen; perform routine assessment of 25-hydroxy vitamin D levels.
Overdose effects

Overdose: Limited information on overdose; symptomatic treatment.

Storage conditions

Storage: Keep below 30 degree C, away from light and moisture. Keep out of reach of children.

Exemestane — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.