Tamoxifen
- Atc Codes:L02BA01
- CAS Codes:54965-24-1#10540-29-1
- PHARMGKB ID:54965-24-1#10540-29-1
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Ebefen, Nolvadex, Tamoxifen; Belgium: Doctamoxifene, Nolvadex, Tamizam, Tamoplex, Tamoxifen, Tamoxifene; Bulgaria: Nolvadex, Tamoxifen; Cyprus: Nolvadex, Novofen, Soltamox, Tamifen, Tamoxifen, Zymoplex; Czech Republic: Nolvadex, Tamoplex, Tamoxifen; Denmark: Tamoxifen; Estonia: Nolvadex, Tamoxifen; Finland: Tadex, Tamexin, Tamofen; France: Nolvadex, Tamoxifene; Germany: Jenoxifen, Kessar, Mandofen, Nolvadex, Nourytam, Novaldex, Soltamox, Tamofen, Tamokadin, Tamox, Tamoxifen, Tamoxistad, Zemide; Greece: Adifen, Kessar, Nolvadex, Puretam, Soltamox, Tamoplex, Tamoxifen, Taxifen, Zymoplex; Hungary: Tamoxifen, Zitazonium; Ireland: Moxelle, Nolvadex, Soltamox, Tamox, Tamoxifen; Italy: Kessar, Nolvadex, Nomafen, Tamoxene, Tamoxifene; Latvia: Tamoxifen; Lithuania: Tamoxifen; Luxembourg: Nolvadex, Tamizam, Tamoxifen; Malta: Nolvadex, Tamofen, Tamoxifen; Netherlands: Nolvadex, Soltamox, Tamoxifen; Poland: Nolvadex, Tamofen, Tamoxifen; Portugal: Mastofen, Nolvadex, Tamoxan; Romania: Tamoneprin, Tamoxifen; Slovakia: Tamoxifen; Slovenia: Nolvadex; Spain: Nolvadex, Tamoxifeno; Sweden: Nolvadex, Tamoxifen; UK: Nolvadex, Tamoxifen.
North America
Canada: Nolvadex, Tamofen, Tamox, Tamoxifen; USA: Tamoxifen.
Latin America
Argentina: Crisafeno, Ginarsan, Nolvadex, Tamoxifeno, Tamoxis; Brazil: Bioxifeno, Festone, Kessar, Nolvadex, Tamoxin, Taxofen-Tamoxifeno, Tecnotax; Mexico: Bagotam, Bilem, Cryoxifeno, Fenobest, Luzamoxin, Nolvadex, Ralsifen, Tamoxifen, Taxus.
Asia
Japan: Adopan, Emalook, Nolvadex, Norxifen, Panleef, Phenolurn, Respol, Soshigen, Tasuomin.
Drug combinations
Tamoxifen and Epirubicin
Tamoxifen, Carmustine, Cisplatin, and Dacarbazine
Chemistry
Tamoxifen Citrate: C~26~H~29~NO C~6~H~8~O~7~. Mw: 563.64. (1) Ethanamine, 2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethyl, (Z)-,2-hydroxy-1,2,3-propanetricarboxylate (1:1); (2)(Z)-2-[p-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine citrate (1:1). CAS-54965-24-1; CAS-10540-29-1 (tamoxifen)(1976).
Pharmacologic Category
Antineoplastic Agents; Endocrine Therapy; Estrogen Receptor Antagonist. Hormones and Synthetic Substitutes; Estrogen Agonist-Antagonists. (ATC-Code: L02BA01).
Mechanism of action
Competitively binds to estrogen receptors on tumors and other tissue targets, producing nuclear complex which decreases DNA synthesis and inhibits estrogen effects.
Therapeutic use
Treatment of metastatic (female and male) breast cancer. Adjuvant treatment of breast cancer. Reduction of risk of invasive breast cancer in women with ductal carcinoma in situ. Reduction of incidence of breast cancer in women at high risk.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies in pregnant women. Reports exist of vaginal bleeding, birth defects and fetal loss in pregnant women. Tamoxifen may induce ovulation. Excretion in breast milk unknown (use not recommended in nursing women).
Unlabeled use
Treatment of mastalgia, gynecomastia, melanoma and desmoid tumors. Induction of ovulation. Treatment of precocious puberty in females, secondary to McCune-Albright syndrome.
Contraindications
Hypersensitivity to tamoxifen or any component of the formulation. Concurrent warfarin therapy or history of deep vein thrombosis or pulmonary embolism (when tamoxifen is used for cancer risk reduction).
Warnings and precautions
Thrombocytopenia and/or leukopenia may occur. Neutropenia and pancytopenia reported rarely. Endometrial hyperplasia, polyps, endometriosis, uterine fibroids, and ovarian cysts occurred. May increase risk of uterine or endometrial cancer. Amenorrhea, menstrual irregularities reported with tamoxifen use. Liver abnormalities such as cholestasis, fatty liver, hepatitis, and hepatic necrosis occurred. Hepatocellular carcinomas reported in some studies (relationship to treatment unclear). Decreased visual acuity, retinal vein thrombosis, retinopathy, corneal changes, color perception changes and increased incidence of cataracts reported. Serious and life-threatening events (including stroke, pulmonary emboli, and uterine malignancy) occurred during use for cancer risk reduction (these events are rare). In patients already diagnosed with breast cancer, benefits of tamoxifen use are greater than risks. Increased incidence of thromboembolic events, including DVT and pulmonary embolism, associated with use for breast cancer. Risk increased with concomitant chemotherapy. Use with caution in history of thromboembolic events. Tamoxifen use may be associated with changes in bone mineral density and effects may be dependent upon menstrual status. In postmenopausal women, tamoxifen use associated with protective effect on bone mineral density. In premenopausal women, decline in bone mineral density observed in women who continued to menstruate (may be associated with increased risk of fractures). Use with caution in hyperlipidemias (infrequent postmarketing cases of hyperlipemias reported). Local disease flare and increased bone and tumor pain may occur. May be associated with (good) tumor response. In bone metastasis, hypercalcemia occurred usually within a few weeks of therapy initiation.