Exemestane


Full Generic Medicine Info
Dosage/Direction for Use

Oral
Adjuvant therapy for postmenopausal women with hormone receptor positive early breast cancer
Adult: Following 2-3 yr initial adjuvant tamoxifen treatment, 25 mg once daily for a total of 5 yr of combined sequential adjuvant hormonal therapy; or earlier if tumour relapse occurs.

Oral
Advanced or locally advanced breast cancer
Adult: 25 mg once daily continued until evident tumour progression.

Special Populations: Patients on strong CYP3A4 enzyme inducers: 50 mg once daily.
Administration
Should be taken with food.
Contraindications
Premenopausal women. Pregnancy and lactation.
Special Precautions
Patient w/ uncontrolled HTN, osteoporosis and its potential causes (e.g. vit D deficiency, hyperthyroidism, hyperparathyroidism). Hepatic and renal impairment. Patient Counselling This drug may cause drowsiness, asthenia, and dizziness, if affected, do not drive or operate machinery. Monitoring Parameters Monitor 25-hydroxy vit D level and BMD prior to therapy; and LFT. Assess for new or unusual bone pain or swelling of face, lips, or throat.
Adverse Reactions
Significant: Decrease in BMD. Nervous: Headache, dizziness, depression, insomnia, anxiety, neuropathy, paraesthesia. CV: HTN. GI: Diarrhoea, nausea, abdominal pain, anorexia, constipation, vomiting. Resp: Dyspnoea. Musculoskeletal: Arthralgia, myalgia, carpal tunnel syndrome, osteoarthritis, osteoporosis. Ophthalmologic: Visual disturbances. Dermatologic: Hot flushes, alopecia, increased sweating, dermatitis, peripheral eodema, rash. Others: Fatigue.
Drug Interactions
Decreased plasma levels of exemestane when used w/ strong CYP3A4 enzyme inducers (e.g. phenytoin, carbamazepine, rifampicin). Antagonised effect w/ oestrogens.
Food Interaction
Increased bioavailability w/ food. Decreased therapeutic effect w/ St John's wort.
Action
Exemestane is an irreversible, selective aromatase inhibitor which acts as a false substrate for the enzyme and forms an intermediate that binds to its active site. This leads to inactivation or suicide inhibition, thus preventing the conversion of androgens to oestrogens in peripheral tissues. It lowers circulating oestrogens in postmenopausal women w/ breast cancers where growth is oestrogen-dependent.
Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: 1.2 hr.
Distribution: Extensively distributed into tissues; crosses the placenta. Plasma protein binding: 90%, primarily to albumin and α1-acid glycoprotein.
Metabolism: Metabolised via oxidation by CYP3A4 enzyme and via reduction by aldoketoreductase into inactive metabolites.
Excretion: Via urine (<1% as unchanged drug; 39-45% as metabolites); faeces (36-48%). Elimination half-life: Approx 24 hr.
Storage
Oral: Store between 20-25°C.
CIMS Class
Hormonal Chemotherapy
ATC Classification
L02BG06 - exemestane ; Belongs to the class of enzyme inhibitors. Used in endocrine therapy.
Disclaimer: This information is independently developed by CIMS based on exemestane from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 CIMS. All rights reserved. Powered by CIMSAsia.com
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