词条 | Trimetrexate |
释义 |
| verifiedrevid = 470615984 | IUPAC_name = 5-methyl-6-[(3,4,5-trimethoxyphenyl) aminomethyl] quinazoline-2,4-diamine | image = Trimetrexate.svg | width = 250 | tradename = | Drugs.com = {{drugs.com|CDI|trimetrexate}} | MedlinePlus = a694019 | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = VD: 20-30 Liters | protein_bound = | metabolism = Oxidative O-demethylation, followed by conjugation with glucuronide or sulfate | elimination_half-life = 11 to 12 hours | IUPHAR_ligand = 7613 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 52128-35-5 | ATC_prefix = P01 | ATC_suffix = AX07 | ATC_supplemental = | PubChem = 5583 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB01157 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 5381 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = UPN4ITI8T4 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D06238 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 119 | C=19 | H=23 | N=5 | O=3 | molecular_weight = 369.418 g/mol | smiles = n3c1c(c(c(cc1)CNc2cc(OC)c(OC)c(OC)c2)C)c(nc3N)N | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | 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_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = NOYPYLRCIDNJJB-UHFFFAOYSA-N }}Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor.[1] UsesIt 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] References1. ^{{cite journal |vauthors =Wong BK, Woolf TF, Chang T, Whitfield LR |title=Metabolic disposition of trimetrexate, a nonclassical dihydrofolate reductase inhibitor, in rat and dog |journal=Drug Metab. Dispos. |volume=18 |issue=6 |pages=980–6 |year=1990 |pmid=1981548 |doi= |url=http://dmd.aspetjournals.org/cgi/pmidlookup?view=long&pmid=1981548}} 2. ^{{cite journal |vauthors=Sattler FR, Allegra CJ, Verdegem TD, etal |title=Trimetrexate-leucovorin dosage evaluation study for treatment of Pneumocystis carinii pneumonia |journal=J. Infect. Dis. |volume=161 |issue=1 |pages=91–6 |date=January 1990 |pmid=2136905 |doi= 10.1093/infdis/161.1.91|url=}} 3. ^{{cite journal |vauthors =Smith HO, Blessing JA, Vaccarello L |title=Trimetrexate in the treatment of recurrent or advanced leiomyosarcoma of the uterus: a phase II study of the Gynecologic Oncology Group |journal=Gynecol. Oncol. |volume=84 |issue=1 |pages=140–4 |date=January 2002 |pmid=11748990 |doi=10.1006/gyno.2001.6482 |url=http://linkinghub.elsevier.com/retrieve/pii/S0090825801964820}} 4. ^Trimetrexate in relapsed T-cell lymphoma with skin involvement. J Clin Oncol. 2002 Jun 15;20(12):2876-80. External links
9 : Antifungals|Mammalian dihydrofolate reductase inhibitors|Protozoal dihydrofolate reductase inhibitors|Fungal dihydrofolate reductase inhibitors|Quinazolines|Antiprotozoal agents|Aromatic amines|Phenol ethers|Anilines |
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