Trimetrexate

Trimetrexate
Clinical data
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
Elimination half-life	11 to 12 hours
Identifiers
	IUPAC name 5-methyl-6-[(3,4,5-trimethoxyphenyl) aminomethyl] quinazoline-2,4-diamine;
CAS Number	52128-35-5 ;
PubChem CID	5583;
IUPHAR/BPS	7613;
DrugBank	DB01157 ;
ChemSpider	5381 ;
UNII	UPN4ITI8T4;
KEGG	D06238 ;
ChEMBL	ChEMBL119 ;
CompTox Dashboard (EPA)	DTXSID3023714 ;
Chemical and physical data
Formula	C19H23N5O3
Molar mass	369.418 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES n3c1c(c(c(cc1)CNc2cc(OC)c(OC)c(OC)c2)C)c(nc3N)N;
	InChI InChI=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) ; Key:NOYPYLRCIDNJJB-UHFFFAOYSA-N ;
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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

MedlinePlus DrugInfo uspdi-202693
DDB 30480

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[pmid1981548-1] 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.

[pmid2136905-2] 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.

[pmid11748990-3] 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.