- Trimetrexate
-
Trimetrexate 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 (what is this?) (verify)
Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor.[1]
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]
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.
External links
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