トリメトレキサート
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/10/03 05:56:54」(JST)
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Trimetrexate
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| Clinical data |
| AHFS/Drugs.com |
Consumer Drug Information |
| MedlinePlus |
a694019 |
| ATC code |
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| 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 |
IUPAC name
- 5-methyl-6-[(3,4,5-trimethoxyphenyl) aminomethyl] quinazoline-2,4-diamine
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| CAS Number |
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| PubChem CID |
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| IUPHAR/BPS |
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| DrugBank |
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| ChemSpider |
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| UNII |
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| KEGG |
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| ChEMBL |
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| Chemical and physical data |
| Formula |
C19H23N5O3 |
| Molar mass |
369.418 g/mol |
| 3D model (JSmol) |
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SMILES
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n3c1c(c(c(cc1)CNc2cc(OC)c(OC)c(OC)c2)C)c(nc3N)N
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InChI
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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) Y
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Key:NOYPYLRCIDNJJB-UHFFFAOYSA-N Y
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| (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]
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. PMID 2136905. doi:10.1093/infdis/161.1.91.
- ^ 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. PMID 11748990. doi:10.1006/gyno.2001.6482.
- ^ 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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Antiparasitics – antiprotozoal agents – Chromalveolate antiparasitics (P01)
|
Alveo-
late |
Apicom-
plexa |
Conoidasida/
(Coccidiostats) |
| Cryptosporidiosis |
- thiazolides (nitazoxanide)
|
| Isosporiasis |
- trimethoprim/sulfamethoxazole#
|
| Toxoplasmosis |
- pyrimethamine
- sulfadiazine
|
|
| Aconoidasida |
| Malaria |
Individual
agents |
Hemozoin
inhibitors |
| Aminoquinolines |
- (4-): amodiaquine#
- chloroquine#
- hydroxychloroquine#
- (8-): primaquine#
- pamaquine‡
- tafenoquine†
|
| 4-Methanolquinolines |
- mefloquine#
- quinine#
- quinidine
|
| Other |
|
|
| Antifolates |
| DHFR inhibitors |
- biguanides
- chlorproguanil
- proguanil#
|
| Sulfonamides |
|
| Co-formulation |
- sulfadoxine/pyrimethamine (SP)#
|
|
Sesquiterpene
lactones |
- artemether#
- artemisinin
- artemotil
- artesunate#
- dihydroartemisinin
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| Other |
- atovaquone (+ proguanil)
- tetracycline
- doxycycline#
- clindamycin
- mepacrine
- pyronaridine
- piperaquine
|
|
Combi-
nations |
| Fixed-dose (co-formulated) ACTs |
- artemether/lumefantrine#
- arterolane/piperaquine
- artesunate/amodiaquine (ASAQ)
- artesunate/mefloquine (ASMQ)
- artesunate/pyronaridine
- dihydroartemisinin/piperaquine
|
Other combinations
(not co-formulated) |
- artesunate/mefloquine
- artesunate/SP
- quinine/clindamycin
- quinine/doxycycline
- quinine/tetracycline
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|
|
| Babesiosis |
|
|
|
Cilio-
phora |
- Balantidiasis: tetracycline
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|
Hetero-
kont |
- Blastocystosis: metronidazole
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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UpToDate Contents
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English Journal
- Lipophilic antifolate trimetrexate is a potent inhibitor of Trypanosoma cruzi: prospect for chemotherapy of Chagas' disease.
- Senkovich O1, Bhatia V, Garg N, Chattopadhyay D.
- Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2005 Aug;49(8):3234-8.
- PMID 16048931
- Transient in vivo selection of transduced peripheral blood cells using antifolate drug selection in rhesus macaques that received transplants with hematopoietic stem cells expressing dihydrofolate reductase vectors.
- Persons DA1, Allay JA, Bonifacino A, Lu T, Agricola B, Metzger ME, Donahue RE, Dunbar CE, Sorrentino BP.
- Blood.Blood.2004 Feb 1;103(3):796-803. Epub 2003 Aug 14.
- PMID 12920024
- Does leucovorin alter the intratumoral pharmacokinetics of 5-fluorouracil (5-FU)? A Southwest Oncology Group study.
- Presant CA1, Jacobson J, Wolf W, Waluch V, Weitz IC, Macdonald JS; Southwest Oncology Group.
- Investigational new drugs.Invest New Drugs.2002 Nov;20(4):369-76.
- PMID 12448653
Related Links
- Neutrexin official prescribing information for healthcare professionals. Includes: indications, dosage, adverse reactions, pharmacology and more. ... Indications and Usage for Neutrexin Neutrexin (trimetrexate glucuronate for injection ...
- Easy to read patient leaflet for Neutrexin. Includes indications, proper use, special instructions, precautions, and possible side effects. ... How to use Neutrexin: Use Neutrexin as directed by your doctor. Check the label on the ...
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