Toremifene
- Atc Codes:L02BA02
- CAS Codes:89778-27-8#89778-26-7
- PHARMGKB ID:89778-27-8#89778-26-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Fareston; Belgium: Fareston; Cyprus: Fareston; Czech Republic: Fareston; Estonia: Fareston; Finland: Fareston; France: Fareston; Germany: Fareston; Greece: Fareston; Hungary: Fareston; Ireland: Fareston; Italy: Fareston; Latvia: Fareston; Lithuania: Fareston; Luxembourg: Fareston; Malta: Fareston; Netherlands: Fareston; Poland: Fareston; Portugal: Fareston; Romania: Fareston; Slovakia: Fareston; Slovenia: Fareston; Spain: Fareston; Sweden: Fareston; UK: Fareston.
North America
Canada: Fareston; USA: Fareston.
Asia
Japan: Fareston.
Drug combinations
Chemistry
Toremifene Citrate: C~26~H~28~ClNO.C~6~H~8~O~7~. Mw: 598.08. (1) Ethanamine, 2-[4-(4-chloro-1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethyl-, (Z)-,2-hydroxy-1,2,3-propanetricarboxylate (1:1); (2) 2-[p-[(Z)-4-Chloro-1,2-diphenyl-1-butenyl]phenoxy]-N,N-dimethylethylamine citrate (1:1). CAS-89778-27-8; CAS-89778-26-7 (toremifene)(1988).
Pharmacologic Category
Antineoplastic Agents, Endocrine Therapy; Estrogen Receptor Antagonist. Hormones and Synthetic Substitute; Estrogen Agonist-Antagonists. (ATC-Code: L02BA02).
Mechanism of action
Nonsteroidal, triphenylethylene derivative with potent antiestrogenic properties (also has estrogenic effects). Competitively binds to estrogen receptors on tumors and other tissue targets, producing nuclear complex which decreases DNA synthesis and inhibits estrogen effects. Competes with estrogen for binding sites in breast and other tissues. Cytostatic rather than cytocidal.
Therapeutic use
Treatment of postmenopausal metastatic breast cancer with estrogen-receptor positive or estrogen-receptor unknown tumors (designated orphan drug by FDA for this use).
Pregnancy and lactiation implications
Animal studies demonstrated embryotoxicity and fetal adverse effects. There are no adequate, well-controlled studies in pregnant women. May cause fetal harm if administered during pregnancy. Excretion in breast milk unknown (not recommended in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to toremifene or any component of the formulation.
Warnings and precautions
Avoid use in thromboembolic disease. Tumor flare may occur during first weeks of treatment in breast cancer patients with bone metastases. Use caution with drugs which decrease renal calcium excretion (e.g. thiazide diuretics); may increase risk of hypercalcemia in patients receiving toremifene. Leukopenia and thrombocytopenia reported rarely. Use with caution in hepatic impairment. Endometrial hyperplasia reported. Endometrial cancer reported (role of toremifene in endometrial cancer development not established). Hypercalcemia may occur during first weeks of treatment in breast cancer patients with bone metastases.