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Trimetrexate
drug data and news
Trimetrexate 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 | Trimetrexate | ||
| Brand Names/Synonyms | CI 898; CI-898; HSDB 6545; JB 11; Jb-11; Neutrexin; TMQ; TMX; Trimetrexate; Trimetrexate [Usan:Ban:Inn]; Trimetrexato [Inn-Spanish]; Trimetrexatum [Inn-Latin]; [Usan:Ban:Inn] | ||
| Indication | For the treatment of moderate to severe Pneumocystis carinii pneumonia (PCP) in immunocompromised patients | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Trimetrexate is an antimetabolite which competitively inhibits the enzyme folic acid reductase. During DNA synthesis and cellular reproduction, folic acid is reduced to tetrahydrofolic acid by the enzyme folic acid reductase. By interfering with the reduction of folic acid, Trimetrexate interferes with tissue cell reproduction. Generally, the most sensitive cells to the antimetabolite effect of Trimetrexate are those cells which are most actively proliferating such as malignant cells, dermal epithelium, buccal and intestinal mucosa, bone marrow, fetal cells and cells of the urinary bladder. Because the proliferation of cells in malignant tissues is greater than in most normal tissues, Trimetrexate may impair the growth of the malignant tissues without causing irreversible damage to normal tissues. | ||
| Mechanism Of Action | Trimetrexate inhibits dihydrofolic acid reductase. Dihydrofolates must be reduced to tetrahydrofolates by this enzyme before they can be utilized as carriers of one-carbon groups in the synthesis of p.r.n. nucleotides and thymidylate. Therefore, Trimetrexate interferes with DNA synthesis, repair, and cellular replication. Actively proliferating tissues such as malignant cells, bone marrow, fetal cells, buccal and intestinal mucosa, and cells of the urinary bladder are in general more sensitive to this effect of Trimetrexate. When cellular proliferation in malignant tissues is greater than in most normal tissues, Trimetrexate may impair malignant growth without irreversible damage to normal tissues. | ||
| Trimetrexate News (When available) |
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| Dosage Forms | POWDER FOR SOLUTION | ||
| Drug_Category | Antimetabolites; Antifungals; Antiprotozoals; Antineoplastics; ATC:P01AX07 | ||
| Absorption | Not Available | ||
| Interactions |
Interactions for Trimetrexate: Since trimetrexate is metabolized by a P450 enzyme system, drugs that induce or inhibit this drug metabolizing enzyme system may elicit important drug-drug interactions that may alter trimetrexate plasma concentrations. Agents that might be coadministered with trimetrexate in AIDS patients for other indications that could elicit this activity include erythromycin, rifampin, rifabutin, ketoconazole, and fluconazole. In vitro perfusion of isolated rat liver has shown that cimetidine caused a significant reduction in trimetrexate metabolism and that acetaminophen altered the relative concentration of trimetrexate metabolites possibly by competing for sulfate metabolites. Based on an in vitro rat liver model, nitrogen substituted imidazole drugs (clotrimazole, ketoconazole, miconazole) were potent, non-competitive inhibitors of trimetrexate metabolism. Patients medicated with these drugs and trimetrexate should be carefully monitored. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 5-methyl-6-[(3,4,5-trimethoxyphenyl)aminomethyl]quinazoline-2,4-diamine | ||
| Chemical Formula | C19H23N5O3 | ||
| Molecular Weight | 369.418 g/mol | ||
| Smiles String | CC1=C(C=CC2=C1C(=NC(=N2)N)N)CNC3=CC(=C(C(=C3)OC)OC)OC | ||
| Melting Point | 215-217 °C | ||
| Water Solubility | 31.4 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 2.437 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic. Not fully characterized in humans; however, data suggest that the major metabolic pathway is oxidative O -demethylation, followed by conjugation to form either the glucuronide or sulfate metabolite | ||
| Half Life | 11 +/- 4 hours | ||
| Protein Binding [%] | 95-98% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Trimetrexate.html http://www.rxlist.com/cgi/generic2/trimetrexate.htm http://www.pharmgkb.org/views/index.jsp?objId= | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00268 | ||
| CAS Registry Number | 52128-35-5 | ||
| KEGG Compound ID | C11154 | ||
| PubChem ID | SID:181153 | ||
| PharmGKB ID | PA451790 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2065770 |
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