DGIdb - TRIMETREXATE Drug Record

TRIMETREXATE chembl:CHEMBL119 ApprovedAntineoplastic

Alternate Names:

TRIMETREXATE
CI-898
NEUTREXIN
TRIMETREXATE GLUCURONATE
TRIMETREXATUM
TRIMETREXATO
NEUTREXIN®
chemidplus:52128-35-5
pubchem.compound:5583
drugbank:01157
rxcui:42333
chembl:CHEMBL119

Drug Info:

Drug Class	antineoplastic agents
Year of Approval	1993
FDA Approval	1993
Drug Class	small molecule
Drug Indications	Antineoplastic Agents

(3 More Sources)

Publications:

Miyachi et al., 1999, Microsatellite instability and clonal heterogeneity of MDR1 messenger RNA expression in trimetrexate-resistant human leukemia MOLT-3 cells developed in thymidine., Int. J. Cancer
Polshakov et al., 1999, Structure and dynamics in solution of the complex of Lactobacillus casei dihydrofolate reductase with the new lipophilic antifolate drug trimetrexate., Protein Sci.
Warlick et al., 2002, In vivo selection of antifolate-resistant transgenic hematopoietic stem cells in a murine bone marrow transplant model., J. Pharmacol. Exp. Ther.
Bertino et al., 1999, Use of variants of dihydrofolate reductase in gene transfer to produce resistance to methotrexate and trimetrexate., Prog Exp Tumor Res
Graffner-Nordberg et al., 2001, Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii., J. Med. Chem.
Zhu et al., Severe folate restriction results in depletion of and alteration in the composition of the intracellular folate pool, moderate sensitization to methotrexate and trimetrexate, upregulation of endogenous DHFR activity, and overexpression of metallothionein II and folate receptor alpha that, upon folate repletion, confer drug resistance to CHL cells., J. Exp. Ther. Oncol.
Sweeney et al., 2003, Trimetrexate inhibits progression of the murine 32Dp210 model of chronic myeloid leukemia in animals expressing drug-resistant dihydrofolate reductase., Cancer Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Sowers R et al., 2011, Impairment of methotrexate transport is common in osteosarcoma tumor samples., Sarcoma

TRIMETREXATE DHFR

Interaction Score: 4.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction <i>In vitro</i> inhibition of wild-type human DHFR

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
10091649 11752096 10386066 11448221 12416030 12649191 11752352 21234348

Sources:
TdgClinicalTrial TEND GuideToPharmacology
TRIMETREXATE PDF

Interaction Score: 1.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TRIMETREXATE MEN1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRIMETREXATE KMT2A

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRIMETREXATE BLM

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRIMETREXATE ABCB1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10360822

Sources:
NCI
TRIMETREXATE MAPT

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRIMETREXATE VDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRIMETREXATE EHMT2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TEND: TRIMETREXATE
- Version: 01-August-2011
Alternate Names:

TRIMETREXATE Primary Drug Name

Drug Info:

Year of Approval 1993

Drug Class antineoplastic agents

Publications:
TdgClinicalTrial: TRIMETREXATE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Antineoplastic Agents

Drug Class small molecule

FDA Approval 1993

Publications:

NCI: TRIMETREXATE

Version: 14-September-2017

Alternate Names:

C1314 NCI drug code

Drug Info:

Publications:

Miyachi et al., 1999, Microsatellite instability and clonal heterogeneity of MDR1 messenger RNA expression in trimetrexate-resistant human leukemia MOLT-3 cells developed in thymidine., Int. J. Cancer

GuideToPharmacology: 223365948
- Version: 29-September-2020
Alternate Names:

TRIMETREXATE GuideToPharmacology Ligand Name

Drug Info:

Publications:
DTC: TRIMETREXATE
- Version: 02-September-2020
Alternate Names:

CHEMBL119 ChEMBL Drug ID

Drug Info:

Publications:
TTD: Trimetrexate
- Version: 2020.06.01
Alternate Names:

D0Y7TS TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL119
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Details of the Assay for Interaction	<i>In vitro</i> inhibition of wild-type human DHFR
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

TRIMETREXATE Drug Record

TRIMETREXATE chembl:CHEMBL119 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction <i>In vitro</i> inhibition of wild-type human DHFR Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 10091649 11752096 10386066 11448221 12416030 12649191 11752352 21234348

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10360822

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TEND: TRIMETREXATE

Alternate Names: TRIMETREXATE Primary Drug Name

Drug Info: Year of Approval 1993 Drug Class antineoplastic agents

Publications:

TdgClinicalTrial: TRIMETREXATE

Alternate Names:

Drug Info: Drug Indications Antineoplastic Agents Drug Class small molecule FDA Approval 1993

Publications:

NCI: TRIMETREXATE

Alternate Names: C1314 NCI drug code

Drug Info:

Publications: Miyachi et al., 1999, Microsatellite instability and clonal heterogeneity of MDR1 messenger RNA expression in trimetrexate-resistant human leukemia MOLT-3 cells developed in thymidine., Int. J. Cancer

GuideToPharmacology: 223365948

Alternate Names: TRIMETREXATE GuideToPharmacology Ligand Name

Drug Info:

Publications:

DTC: TRIMETREXATE

Alternate Names: CHEMBL119 ChEMBL Drug ID

Drug Info:

Publications:

TTD: Trimetrexate

Alternate Names: D0Y7TS TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL119

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction <i>In vitro</i> inhibition of wild-type human DHFR

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
10091649 11752096 10386066 11448221 12416030 12649191 11752352 21234348

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
10360822

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

TRIMETREXATE Primary Drug Name

Drug Info:

Year of Approval 1993

Drug Class antineoplastic agents

Drug Info:

Drug Indications Antineoplastic Agents

Drug Class small molecule

FDA Approval 1993

Alternate Names:

C1314 NCI drug code

Publications:

Miyachi et al., 1999, Microsatellite instability and clonal heterogeneity of MDR1 messenger RNA expression in trimetrexate-resistant human leukemia MOLT-3 cells developed in thymidine., Int. J. Cancer

Alternate Names:

TRIMETREXATE GuideToPharmacology Ligand Name

Alternate Names:

CHEMBL119 ChEMBL Drug ID

Alternate Names:

D0Y7TS TTD Drug ID