Generic Medicine Info
Indications and Dosage
Metastatic breast cancer in postmenopausal women with estrogen-receptor positive tumours
Adult: 60 mg once daily.
Hepatic Impairment
Dosage adjustments may be needed. Severe: Contraindicated.
May be taken with or without food.
Pre-existing endometrial hyperplasia, severe hepatic failure. History of severe thromboembolic disease. Pregnancy and lactation.
Special Precautions
Uncompensated heart failure, severe angina pectoris. Monitor for signs of hypercalcaemia for patients with bone metastases. Perform gynaecological examinations before therapy and at least once a year. Closely monitor patients at risk of endometrial cancer. Monitor CBC, serum calcium concentration and LFT periodically.
Adverse Reactions
Hot flushes, sweating, nausea, leucorrhoea, dizziness, vaginal bleeding or discharge, fatigue, headache, skin discolouration, increased weight, insomnia, constipation, dyspnoea, vomiting, vertigo, pruritus, abnormal vision, asthenia, thromboembolic events, depression, jaundice, pulmonary embolism, thrombophlebitis, loss of appetite, endometrial changes.
Symptoms: Anti-estrogenic effects e.g. hot flashes; estrogenic effects e.g. vaginal bleeding; or nervous system disorders e.g. vertigo, dizziness, ataxia and nausea. Management: Treatment is symptomatic and there is no specific antidote.
Drug Interactions
Decreased serum concentrations of toremifene with concomitant use of known CYP3A4 inducers (e.g. carbamazepine, phenobarbital, phenytoin, rifampicin). Increased serum concentrations of toremifene with erythromycin, troleandomycin, ketoconazole. Increased risk of bleeding with coumarins. Increased risk of hypercalcaemia with drugs which decrease renal calcium excretion e.g. thiazide diuretics.
Description: Toremifene, a non-steroidal triphenylethylene derivative, competitively binds to estrogen receptors on tumours and other tissue targets. It may exert estrogenic, anti-estrogenic, or both activities. In breast cancer it is believed to exert anti-estrogenic effects, by competing with estrogen for binding sites in the cancer, hence blocking the growth-stimulating effects of estrogen in the tumour.
Absorption: Well absorbed from GI tract. Peak plasma concentrations within 3 hr.
Distribution: Protein-binding: Extensive, mainly to albumin.
Metabolism: Metabolised mainly by the cytochrome P450 isoenzyme CYP3A4 to less active metabolites.
Excretion: Excreted mainly in faeces and in urine (10%) as metabolites. Undergoes enterohepatic circulation.
Store at 15-30°C (59-86°F).
Disclaimer: This information is independently developed by MIMS based on Toremifene from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS 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 © 2021 MIMS. All rights reserved. Powered by
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