Trimetrexate
Clinical data | |
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AHFS/Drugs.com | Consumer Drug Information |
MedlinePlus | a694019 |
ATC code | P01AX07 (WHO) |
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 |
Identifiers | |
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CAS Number | 52128-35-5 |
PubChem (CID) | 5583 |
IUPHAR/BPS | 7613 |
DrugBank | DB01157 |
ChemSpider | 5381 |
UNII | UPN4ITI8T4 |
KEGG | D06238 |
ChEMBL | CHEMBL119 |
Chemical and physical data | |
Formula | C19H23N5O3 |
Molar mass | 369.418 g/mol |
3D model (Jmol) | Interactive image |
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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.
- ↑ 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.
- ↑ 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.
External links
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