Trimetrexate
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| Systematic (IUPAC) name | |
| 5-methyl-6-[(3,4,5-trimethoxyphenyl) aminomethyl] quinazoline-2,4-diamine | |
| Clinical data | |
| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a694019 |
| Pregnancy cat. | ? |
| Legal status | ? |
| Pharmacokinetic data | |
| Bioavailability | VD: 20-30 Liters |
| Metabolism | Oxidative O-demethylation, followed by conjugation with glucuronide or sulfate |
| Half-life | 11 to 12 hours |
| Identifiers | |
| CAS number | 52128-35-5  |
| ATC code | P01AX07 |
| PubChem | CID 5583 |
| DrugBank | APRD00268 |
| ChemSpider | 5381 |
| UNII | UPN4ITI8T4 |
| KEGG | D06238 |
| ChEMBL | CHEMBL119 |
| Chemical data | |
| Formula | C19H23N5O3 |
| Mol. mass | 369.418 g/mol |
| SMILES | eMolecules & PubChem |
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Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor.[1]
[edit] Uses
It has been used with leucovorin in treating pneumocystis pneumonia.[2]
It has been investigated for use in treating leiomyosarcoma.[3] It is a methotrexate (MTX) analog that is active against transport-deficient MTX-resistant tumor cells that overcome the acquired and natural resistance to methotrexate. Other uses include skin lymphoma. [4]
[edit] References
- ^ Wong BK, Woolf TF, Chang T, Whitfield LR (1990). "Metabolic disposition of trimetrexate, a nonclassical dihydrofolate reductase inhibitor, in rat and dog". Drug Metab. Dispos. 18 (6): 980–6. PMID 1981548. http://dmd.aspetjournals.org/cgi/pmidlookup?view=long&pmid=1981548.
- ^ Sattler FR, Allegra CJ, Verdegem TD, et al. (January 1990). "Trimetrexate-leucovorin dosage evaluation study for treatment of Pneumocystis carinii pneumonia". J. Infect. Dis. 161 (1): 91–6. PMID 2136905.
- ^ Smith HO, Blessing JA, Vaccarello L (January 2002). "Trimetrexate in the treatment of recurrent or advanced leiomyosarcoma of the uterus: a phase II study of the Gynecologic Oncology Group". Gynecol. Oncol. 84 (1): 140–4. doi:10.1006/gyno.2001.6482. PMID 11748990. http://linkinghub.elsevier.com/retrieve/pii/S0090825801964820.
- ^ Trimetrexate in relapsed T-cell lymphoma with skin involvement. J Clin Oncol. 2002 Jun 15;20(12):2876-80.
[edit] External links
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