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Tamoxifen
drug data and news
Tamoxifen 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 | Tamoxifen | ||
| Brand Names/Synonyms | ,Citrate; Apo-Tamox; CCRIS 3275; CTX; Citofen; Crisafeno; Diemon; Gen-Tamoxifen; HSDB 6782; Istubol; Kessar; Noltam; Nolvadex; Nolvadex-D; Nourytam; Novo-Tamoxifen; Oncomox; Pms-Tamoxifen; Retaxim; TRANS FORM OF TAMOXIFEN; Tamizam; Tamofen; Tamone; Tamoxasta; Tamoxen; Tamoxifen; Tamoxifen Citrate; Tamoxifen Drug Standard Solution; Tamoxifen and Its Salts; Tamoxifene [Inn-French]; Tamoxifeno [Inn-Spanish]; Tamoxifenum [Inn-Latin]; Trans-Tamoxifen; Valodex; Zemide | ||
| Indication | for the treatment of breast cancer | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Tamoxifen belongs to a class of drugs called selective estrogen receptor modulators (SERMs), which have both estrogenic and antiestrogenic effects. Tamoxifen has the same nucleus as diethylstilbestrol but possesses an additional side chain (trans isomer) which accounts for its antiestrogenic activity. Tamoxifen, chemically related to clomiphene., is used to in the therapy of metastatic breast cancer. | ||
| Mechanism Of Action | Tamoxifen binds to estrogen receptors (ER), inducing a conformational change in the receptor. This results in a blockage or change in the expression of estrogen dependent genes. The prolonged binding of tamoxifen to the nuclear chromatin of these results in reduced DNA polymerase activity, impaired thymidine utilization, blockade of estradiol uptake, and decreased estrogen response. It is likely that tamoxifen interacts with other coactivators or corepressors in the tissue and binds with different estrogen receptors, ER-alpha or ER-beta, producing both estrogenic and antiestrogenic effects. | ||
| Tamoxifen News (When available) |
Pak1 expression increases tamoxifen resistance in breast cancer ... 16 May 2006 EntreMed hoping for success with Panzem/Avastin combo 16 May 2006 New York Times Reporter Examines Recent Study Comparing Raloxifene ... May 10, 2006 Tamoxifen Use Associated With Smaller Optic Cup Size: Presented at ... May 5, 2006 New Breast Cancer Drug Safer Than Tamoxifen Apr 17, 2006 Raloxifene Reduces Breast Cancer Risk As Well As Tamoxifen Apr 17, 2006 Cousin of tamoxifen prevents breast cancer Apr 18, 2006 Lilly`s Evista beats tamoxifen Apr 17, 2006 Evista as good as tamoxifen for breast cancer: study Apr 17, 2006 Drug equals tamoxifen in preventing breast cancer: Study Apr 17, 2006 Drug equals tamoxifen in preventing breast cancer: Study Apr 17, 2006 Osteoporosis drug as effective as tamoxifen: study Apr 17, 2006 STAR Study: Raloxifene is as effective as Tamoxifen in reducing ... Apr 20, 2006 Study of Tamoxifen and Raloxifene (STAR) Results: Osteoporosis ... Apr 17, 2006 Osteoporosis drug Raloxifene shown to be as effective as Tamoxifen ... Apr 17, 2006 Raloxifene trumps tamoxifen in safety trials for breast cancer Apr 18, 2006 Raloxifene as Good as Tamoxifen to Prevent Breast Cancer Apr 17, 2006 Raloxifene or tamoxifen: Which is the right drug for you? Apr 19, 2006 Osteoporosis drug equals tamoxifen in preventing breast cancer Apr 17, 2006 Raloxifene as effective as Tamoxifen in preventing invasive breast ... Apr 18, 2006 Study shows osteoporosis drug as good as Tamoxifen Apr 18, 2006 Osteoporosis Drug As Effective as Tamoxifen in Reducing Breast ... Apr 17, 2006 Evista may be a better option than Tamoxifen for reducing breast ... Apr 17, 2006 Drug has fewer side effects, is as effective as Tamoxifen, study ... Apr 17, 2006 Raloxifene Better Than Tamoxifen For Breast Cancer Apr 18, 2006 Comment: Should Women Switch From Tamoxifen to Raloxifene (Evista) ... Apr 18, 2006 Evista Equivalent to Tamoxifen for Breast Cancer Patients Apr 18, 2006 Eli Lilly Releases Statement On Results Of Study Of Tamoxifen And ... Apr 17, 2006 New Breast Cancer Drug, Safer Than Tamoxifen Apr 17, 2006 Pre-Operative Arimidex® Provides Greater Responses than Tamoxifen ... May 3, 2006 Pre-Operative Arimidex® Provides Greater Responses than Tamoxifen ... May 4, 2006 Tamoxifen vs. Raloxifene Apr 19, 2006 Osteoporosis Drug As Effective As Tamoxifen In Preventing Invasive ... Apr 20, 2006 Bone Thinning Drug Raloxifene As Effective As Tamoxifen In ... Apr 20, 2006 Osteoporosis drug raloxifene shown to be as effective as tamoxifen ... Apr 18, 2006 Evista® as Effective as Tamoxifen in Preventing Breast Cancer ... Apr 18, 2006 Raloxifene Shows Advantages Over Tamoxifen in Breast Cancer ... Apr 18, 2006 Lilly's Evista rivals tamoxifen in breast cancer Apr 18, 2006 Study: Evista safer than tamoxifen in preventing breast cancer Apr 18, 2006 Sorting Out Pills to Reduce Breast Cancer Risk May 10, 2006 Women needlessly having breast cancer surgery: doctor May 15, 2006 Lilly Calls Tamoxifen/Raloxifene Study Important Milestone Apr 17, 2006 Evista as good as tamoxifen for breast cancer: study Apr 18, 2006 Evista is as effective as Tamoxifen for Breast Cancer Apr 18, 2006 Evista as good as tamoxifen for breast cancer: study Apr 17, 2006 New drug safer than tamoxifen? Apr 18, 2006 Safer alternative for breast cancer drug tamoxifen Apr 17, 2006 Is new breast cancer pill better? May 11, 2006 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Antineoplastic Agents; ATC:L02BA01 | ||
| Absorption | Not Available | ||
| Interactions |
-->Interactions for Tamoxifen: When NOLVADEX is used in combination with coumarin-type anticoagulants, a significant increase in anticoagulant effect may occur. Where such coadministration exists, careful monitoring of the patientís prothrombin time is recommended. In the NSABP P-1 trial, women who required coumarin-type anticoagulants for any reason were ineligible for participation in the trial. There is an increased risk of thromboembolic events occurring when cytotoxic agents are used in combination with NOLVADEX. Tamoxifen reduced letrozole plasma concentrations by 37%. The effect of tamoxifen on metabolism and excretion of other antineoplastic drugs, such as cyclophosphamide and other drugs that require mixed function oxidases for activation, is not known. Tamoxifen and N-desmethyl tamoxifen plasma concentrations have been shown to be reduced when coadministered with rifampin or aminoglutethimide. Induction of CYP3A4-mediated metabolism is considered to be the mechanism by which these reductions occur; other CYP3A4 inducing agents have not been studied to confirm this effect. One patient receiving NOLVADEX with concomitant phenobarbital exhibited a steady state serum level of tamoxifen lower than that observed for other patients (ie, 26 ng/mL vs. mean value of 122 ng/mL). However, the clinical significance of this finding is not known. Rifampin induced the metabolism of tamoxifen and significantly reduced the plasma concentrations of tamoxifen in 10 patients. Aminoglutethimide reduces tamoxifen and N desmethyl tamoxifen plasma concentrations. Medroxyprogesterone reduces plasma concentrations of N-desmethyl, but not tamoxifen. Concomitant bromocriptine therapy has been shown to elevate serum tamoxifen and N-desmethyl tamoxifen. Drug/Laboratory Testing Interactions: During postmarketing surveillance, T4 elevations were reported for a few postmenopausal patients which may be explained by increases in thyroid-binding globulin. These elevations were not accompanied by clinical hyperthyroidism. Variations in the karyopyknotic index on vaginal smears and various degrees of estrogen effect on Pap smears have been infrequently seen in postmenopausal patients given NOLVADEX. In the postmarketing experience with NOLVADEX, infrequent cases of hyperlipidemias have been reported. Periodic monitoring of plasma triglycerides and cholesterol may be indicated in patients with pre-existing hyperlipidemias . | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | [5-(2-amino-6-oxo-3,9-dihydropurin-9-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl]methoxy-[(3,4-dihydroxy-6-methyl-5-oxo-tetrahydropyran-2-yl)oxy-hydroxy-phosphoryl]oxy-phosphinicacid | ||
| Chemical Formula | C16H23N5O15P2 | ||
| Molecular Weight | 587.326 g/mol | ||
| Smiles String | CC1C(=O)C(C(C(O1)OP(=O)(O)OP(=O)(O)OCC2C(C(C(O2)N3C=NC4=C3NC(=NC4=O)N)O)O)O)O | ||
| Melting Point | 97 °C | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | 6.3 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Not Available | ||
| Half Life | 5-7 days | ||
| Protein Binding [%] | Not Available | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Tamoxifen.html http://www.rxlist.com/cgi/generic/tamox.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00123 | ||
| CAS Registry Number | 10540-29-1 | ||
| KEGG Compound ID | C07108 | ||
| PubChem ID | SID:4444 | ||
| PharmGKB ID | PA451581 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2237460 |
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