Oral Adjuvant therapy for postmenopausal women with hormone receptor positive early breast cancer
Adult: In estrogen receptor-positive patients who have received 2-3 years of initial adjuvant tamoxifen therapy: 25 mg once daily, continue until completion of 5 years of combined sequential adjuvant hormonal therapy (tamoxifen followed by exemestane) or earlier if tumour relapse occurs.
Oral Advanced breast cancer in postmenopausal women
Adult: In patients with natural or artificially induced postmenopausal status whose disease has progressed after anti-estrogen treatment: 25 mg once daily, continue until tumour progression is evident.
What are the brands available for Exemestane in Malaysia?
Patient with osteoporosis or who are at increased risk of osteoporosis. Patients taking strong CYP3A4 inducers (e.g. rifampicin, phenytoin). Renal and hepatic impairment.
Adverse Reactions
Significant: Reduction in BMD and increased fracture rate. Rarely, increased AST, ALT, alkaline phosphatase, and GGT >5 times ULN (particularly in patients with advanced breast cancer). Blood and lymphatic system disorders: Lymphocytopenia. Eye disorders: Visual disturbances. Gastrointestinal disorders: Nausea, abdominal pain, vomiting, constipation, dyspepsia, diarrhoea. General disorders and administration site conditions: Fatigue, pain, peripheral oedema, asthenia. Metabolism and nutrition disorders: Anorexia. Musculoskeletal and connective tissue disorders: Arthralgia, musculoskeletal pain. Nervous system disorders: Headache, dizziness, carpal tunnel syndrome, paraesthesia, somnolence. Psychiatric disorders: Insomnia, depression. Skin and subcutaneous tissue disorders: Hyperhidrosis, alopecia, rash, urticaria, pruritus. Vascular disorders: Hot flushes, hypertension.
PO: Z (May disrupt oestrogen metabolism and result in abortion. Generally contraindicated during pregnancy.)
Patient Counseling Information
Women of childbearing potential should use effective contraception during and 1 month after treatment.
Monitoring Parameters
Evaluate pregnancy status within 7 days before starting therapy. Confirm postmenopausal status through LH, FSH, or estradiol level assessments as clinically indicated. Monitor 25-hydroxy vitamin D levels and BMD (particularly in patients with or at risk for osteoporosis) at baseline; blood pressure. Assess for new or unusual bone pain.
Drug Interactions
Reduced therapeutic effect with estrogen-containing drugs. May decrease plasma concentration with CYP3A4 inducers (e.g. rifampicin, phenytoin, carbamazepine, phenobarbital).
Food Interaction
Increased bioavailability with food. May decrease the serum concentration with St. John's wort.
Action
Description: Mechanism of Action: Exemestane is an irreversible, selective steroidal aromatase inhibitor. It acts as a false substrate and is converted by aromatase into reactive alkylating intermediates that irreversibly bind to the active site of the enzyme, leading to its inactivation, a mechanism known as "suicide inhibition". Consequently, it blocks the conversion of androgen to estrogen in peripheral tissues, thereby significantly reducing circulating estrogen levels in postmenopausal breast cancers, inhibiting tumour growth, and delaying disease progression. Pharmacokinetics: Absorption: Rapidly and moderately absorbed from the gastrointestinal tract. Increased bioavailability with food. Distribution: Extensively distributed into the tissues. Plasma protein binding: 90%, mainly to albumin and α1-acid glycoprotein. Metabolism: Extensively metabolised in the liver via oxidation of methylene group by CYP3A4 isoenzyme and via reduction of 17-keto group by aldoketoreductase into inactive metabolites. Excretion: Via urine (<1% as unchanged drug, 39-45% as metabolites); faeces (36-48%). Elimination half-life: Approx 24 hours.
Chemical Structure
Exemestane Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 60198, Exemestane. https://pubchem.ncbi.nlm.nih.gov/compound/Exemestane. Accessed Mar. 27, 2025.
Storage
Store between 15-30°C. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
L02BG06 - exemestane ; Belongs to the class of enzyme inhibitors. Used in treatment of neoplastic diseases.
References
Aromasin Tablet (Pharmacia & Upjohn Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/03/2025.Brayfield A, Cadart C (eds). Exemestane. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/03/2025.Exemestane 25 mg Film-coated Tablets (Rudipharm Limited). MHRA. https://products.mhra.gov.uk. Accessed 06/03/2025.Exemestane. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/03/2025.Exemestane. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/03/2025.Exetas 25 mg Tablet (Accord Healthcare Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 06/03/2025.Joint Formulary Committee. Exemestane. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/03/2025.Pfizer New Zealand Ltd. Exemestane Pfizer 25 mg Coated Tablets data sheet 16 October 2024. Medsafe. http://www.medsafe.govt.nz. Accessed 06/03/2025.
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