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Toremifene
drug data and news
Toremifene drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Toremifene | ||
| Brand Names/Synonyms | Acapodene; Fareston; Farestone; Toremifene; Toremifene Base; Toremifeno [Spanish]; Toremifenum [Latin]; Z-Toremifene | ||
| Indication | For the treatment of metastatic breast cancer in postmenopausal women with estrogen receptor-positive or receptor-unknown tumors | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Toremifene is an antineoplastic hormonal agent primarily used in the treatment of advanced breast cancer. Toremifene is a nonsteroidal agent that has demonstrated potent antiestrogenic properties in animal test systems. The antiestrogenic effects may be related to its ability to compete with estrogen for binding sites in target tissues such as breast. Toremifene inhibits the induction of rat mammary carcinoma induced by dimethylbenzanthracene (DMBA) and causes the regression of already established DMBA-induced tumors. In this rat model, Toremifene appears to exert its antitumor effects by binding the estrogen receptors. In cytosols derived from human breast adenocarcinomas, Toremifene competes with estradiol for estrogen receptor protein. | ||
| Mechanism Of Action | Toremifene is a nonsteroidal triphenylethylene derivative. Toremifene binds to estrogen receptors and may exert estrogenic, antiestrogenic, or both activities, depending upon the duration of treatment, animal species, gender, target organ, or endpoint selected. The antitumor effect of toremifene in breast cancer is believed to be mainly due to its antiestrogenic effects, ie, its ability to compete with estrogen for binding sites in the cancer, blocking the growth-stimulating effects of estrogen in the tumor. | ||
| Toremifene News (When available) |
Cordova High-Rise Sells for $19.3 Million May 15, 2006 GTx, Inc. Attains Enrollment Goal for Phase III PIN Clinical Trial May 3, 2006 GTX, Inc. Reports First Quarter 2006 Financial Results Apr 27, 2006 GTx, Inc. Announces Initiation of Phase IIIb Extension Trial of ... Apr 21, 2006 Orion Oyj: Orion group interim report 1-3/2006 May 8, 2006 GTx Q1 Loss Per Share Narrows, To File NDA During 2008 - Quick ... Apr 27, 2006 | ||
| Dosage Forms | Tablet | ||
| Drug_Category | Antineoplastic Agents; Selective Estrogen Receptor Modulators; ATC:L02BA02 | ||
| Absorption | Well absorbed | ||
| Interactions |
Interactions for Toremifene: Drugs that decrease renal calcium excretion, eg, thiazide diuretics, may increase the risk of hypercalcemia in patients receiving FARESTON. There is a known interaction between antiestrogenic compounds of the triphenylethylene derivative class and coumarin-type anticoagulants (eg, warfarin), leading to an increased prothrombin time. When concomitant use of anticoagulants with FARESTON is necessary, careful monitoring of the prothrombin time is recommended. Cytochrome P450 3A4 enzyme inducers, such as phenobarbital, phenytoin, and carbamazepine increase the rate of toremifene metabolism, lowering the steady-state concentration in serum. Metabolism of toremifene may be inhibited by drugs known to inhibit the CYP3A4-6 enzymes. Examples of such drugs are ketoconazole and similar antimycotics as well as erythromycin and similar macrolides. This interaction has not been studied and its clinical relevance is uncertain. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 2-[4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy]-N,N-dimethyl-ethanamine | ||
| Chemical Formula | C26H28ClNO | ||
| Molecular Weight | 405.959 g/mol | ||
| Smiles String | CN(C)CCOC1=CC=C(C=C1)C(=C(CCCl)C2=CC=CC=C2)C3=CC=CC=C3 | ||
| Melting Point | 108-110 °C | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | 6.725 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Mainly by CYP3A4 | ||
| Half Life | 5 days | ||
| Protein Binding [%] | more than 99.5% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Toremifene.html http://www.rxlist.com/cgi/generic2/toremifene.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00391 | ||
| CAS Registry Number | 89778-26-7 | ||
| KEGG Compound ID | C08166 | ||
| PubChem ID | SID:193362 | ||
| PharmGKB ID | PA451731 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
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