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Systematic (IUPAC) name
5-methyl-6-[(3,4,5-trimethoxyphenyl) aminomethyl] quinazoline-2,4-diamine
Clinical data
AHFS/ Consumer Drug Information
MedlinePlus a694019
Pharmacokinetic data
Bioavailability VD: 20-30 Liters
Metabolism Oxidative O-demethylation, followed by conjugation with glucuronide or sulfate
Biological half-life 11 to 12 hours
CAS Registry Number 52128-35-5 YesY
ATC code P01AX07
PubChem CID: 5583
DrugBank DB01157 YesY
ChemSpider 5381 YesY
KEGG D06238 YesY
Chemical data
Formula C19H23N5O3
Molecular mass 369.418 g/mol
 YesY (what is this?)  (verify)

Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor.[1]


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]


  1. ^ 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. 
  2. ^ 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. doi:10.1093/infdis/161.1.91. PMID 2136905. 
  3. ^ 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. 
  4. ^ Trimetrexate in relapsed T-cell lymphoma with skin involvement. J Clin Oncol. 2002 Jun 15;20(12):2876-80.

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