Exemstane

Indications
 Oral
Advanced or locally advanced breast cancer
Adult: In women who are no longer responsive to anti-oestrogen therapy: 25 mg once daily.
Contraindications
 Hypersensitivity. Premenopausal women. Pregnancy and lactation.
Warnings / Precautions
 Hepatic and renal impairment. Monitor bone mineral density at regular intervals especially in patients at risk of osteoporosis.
Adverse Reactions
 Hot flushes; nausea; fatigue; increased sweating; dizziness; headache; insomnia; skin rash; abdominal pain; anorexia, vomiting (less frequently), dyspepsia, depression, alopoecia, peripheral oedema, constipation, dyspepsia. Rarely thrombocytopaenia, leucopaenia.
Drug Interactions
 May result in reduced plasma levels of exemestane when used with CYP3A4 enzyme inducers. Oestrogen-containing drugs; St. John's wort, black cohosh, dong quai.
See Below for More exemestane Drug Interactions
Mechanism of Actions
 Exemestane is an irreversible selective aromatase inhibitor which acts as a false substrate for the aromatase enzyme, forming an intermediate that binds irreversibly to the active site causing its inactivation. It also lowers circulating oestrogens in estrogen-dependent breast carcinoma.
Absorption: Rapidly absorbed.
Distribution: Widely distributed and extensively bound to plasma proteins.
Metabolism: Metabolised via oxidation by CYP3A4, and via reduction by aldoketoreductase
Excretion: Metabolites are excreted in urine and faeces, less than 1% excreted unchanged in the urine.
Administration
 Should be taken with food. (Take after a meal.)
ATC Classification
 L02BG06 - exemestane ; Belongs to the class of enzyme inhibitors. Used in endocrine therapy.
Available As
  • Exemstane 25 mg

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