Exemestane

Exemestane is an aromatase inhibitor. It is used in the treatment of breast cancer in women who have gone through menopause. It works by adjusting the level of estrogen and helps in slowing down the growth of cancer cells. Exemestane is also used in combination with medication in early cancer to prevent the risk of coming back.

Exemestane is an aromatase inhibitor. It works by lowering the amount of estrogen (natural female hormone) produced in the body. This can lower or stop the growth of some breast cancer cells that need estrogen to grow.

• 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.

Aromatase inhibitor

Aromatase Inhibitor (Steroidal)

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.

Exemestane irreversibly inactivates the aromatase enzyme, reducing estrogen production, which slows the growth of estrogen-dependent breast cancer cells.

Adult Dose (Oral):

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

Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Exemestane is to be taken with food.

If you miss a dose of Exemestane, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.

Common Side Effects:

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

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.

Contraindications:

• Hypersensitivity
• Premenopausal women
• Pregnancy and lactation

Drug Interactions:

• CYP3A4 enzyme inducers (rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's Wort): May reduce plasma levels of exemestane.
• Estrogen-containing drugs, St. John's wort, black cohosh, dong quai: Avoid.

Food Interactions: It is not known whether it is safe to consume alcohol with Exemestane. Consult your doctor.

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

Use in Lactation: Unsafe during breastfeeding; data suggests drug may cause toxicity to the baby.

Pediatric Use: Not indicated for children.

Geriatric Use: No specific dosage adjustment is necessary for elderly patients.

Renal Impairment: Probably safe in patients with kidney disease; dose adjustment may not be needed.

Hepatic Impairment: Probably safe in patients with liver disease; dose adjustment may not be needed.

Overdose: Limited information on overdose; symptomatic treatment.

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

Exemestane