| Verifiedrevid | 470615984 |
|---|---|
| Iupac name | 5-methyl-6-[(3,4,5-trimethoxyphenyl) aminomethyl] quinazoline-2,4-diamine |
| Width | 250 |
| Medlineplus | a694019 |
| Bioavailability | VD: 20-30 Liters |
| Metabolism | Oxidative O-demethylation, followed by conjugation with glucuronide or sulfate |
| Elimination half-life | 11 to 12 hours |
| Iuphar ligand | 7613 |
| Cas number | 52128-35-5 |
| Atc prefix | P01 |
| Atc suffix | AX07 |
| Pubchem | 5583 |
| Drugbank | DB01157 |
| Chemspiderid | 5381 |
| Unii | UPN4ITI8T4 |
| Kegg | D06238 |
| Chembl | 119 |
| C | 19 |
| H | 23 |
| N | 5 |
| O | 3 |
| Smiles | n3c1c(c(c(cc1)CNc2cc(OC)c(OC)c(OC)c2)C)c(nc3N)N |
| Stdinchi | 1S/C19H23N5O3/c1-10-11(5-6-13-16(10)18(20)24-19(21)23-13)9-22-12-7-14(25-2)17(27-4)15(8-12)26-3/h5-8,22H,9H2,1-4H3,(H4,20,21,23,24) |
| Stdinchikey | NOYPYLRCIDNJJB-UHFFFAOYSA-N |
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. doi:10.1016/S0090-9556(25)08702-1. PMID 1981548
- ^ Sattler FR, Allegra CJ, Verdegem TD, etal (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
- ^ 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
- ^ Trimetrexate in relapsed T-cell lymphoma with skin involvement. J Clin Oncol. 2002 Jun 15;20(12):2876-80.