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	369.425 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 ;
	(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]

gollark: In any case, would most lasers *not* just be blocked by the skull and not interact with brain tissue anyway?

gollark: This is probably more of an issue for neuroscientists than... people with lasers.

gollark: Oh, and magnetic thingies and lasers are very different.

gollark: <@542811977383280662> Talking in <#482370338324348932> is annoying so I'll say it here: the current state of brain interaction stuff seems to be at the level of just hamfistedly meddling with large regions of the brain, not anything targeted enough to make people "super intelligent".

gollark: As far as I'm aware the way that works is that you can profit off it being worse than *other people predicted*, not just bad.

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.