DGIdb - RALTITREXED Drug Record

RALTITREXED chembl:CHEMBL225071 ApprovedAntineoplasticImmunotherapy

Alternate Names:

TOMUDEX
RALTITREXED
ZD-1694
ZD-16
TOMUDEX®
ZD1694
ICI-D-1694
drugbank:00293
chemidplus:112887-68-0
chembl:CHEMBL225071
pubchem.compound:104758
rxcui:196239

Drug Info:

Year of Approval	not approved by the fda
Drug Class	antineoplastic agents
FDA Approval	not approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent

(6 More Sources)

Publications:

Blair et al., 2004, Population pharmacokinetics of raltitrexed in patients with advanced solid tumours., Br J Clin Pharmacol
Cao et al., 1999, Antitumor activity of ZD1694 (tomudex) against human head and neck cancer in nude mouse models: role of dosing schedule and plasma thymidine., Clin. Cancer Res.
Orlandi et al., 1999, Involvement of bcl-2 and p21waf1 proteins in response of human breast cancer cell clones to Tomudex., Br. J. Cancer
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Chen et al., 1999, Cellular pharmacology of MTA: a correlation of MTA-induced cellular toxicity and in vitro enzyme inhibition with its effect on intracellular folate and nucleoside triphosphate pools in CCRF-CEM cells., Semin. Oncol.
Ferguson et al., 1999, Antisense down-regulation of thymidylate synthase to suppress growth and enhance cytotoxicity of 5-FUdR, 5-FU and Tomudex in HeLa cells., Br. J. Pharmacol.
Yang et al., 2008, DNA damage and homologous recombination signaling induced by thymidylate deprivation., Biochem. Pharmacol.
Grem et al., 1999, A Phase I study of raltitrexed, an antifolate thymidylate synthase inhibitor, in adult patients with advanced solid tumors., Clin. Cancer Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Yin et al., 1999, Cyclin E-cdk2 activation is associated with cell cycle arrest and inhibition of DNA replication induced by the thymidylate synthase inhibitor Tomudex., Exp. Cell Res.
Salgado J et al., 2007, Polymorphisms in the thymidylate synthase and dihydropyrimidine dehydrogenase genes predict response and toxicity to capecitabine-raltitrexed in colorectal cancer., Oncol Rep
Massacesi et al., 2006, Uridine diphosphate glucuronosyl transferase 1A1 promoter polymorphism predicts the risk of gastrointestinal toxicity and fatigue induced by irinotecan-based chemotherapy., Cancer
Rustum, 2004, Thymidylate synthase: a critical target in cancer therapy?, Front. Biosci.
Wang L et al., 2011, Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase., J Med Chem
Whetstine JR et al., 2001, Single nucleotide polymorphisms in the human reduced folate carrier: characterization of a high-frequency G/A variant at position 80 and transport properties of the His(27) and Arg(27) carriers., Clin Cancer Res
Peters et al., 2000, Molecular downstream events and induction of thymidylate synthase in mutant and wild-type p53 colon cancer cell lines after treatment with 5-fluorouracil and the thymidylate synthase inhibitor raltitrexed., Eur. J. Cancer
Takemura et al., 1996, Biological activity and intracellular metabolism of ZD1694 in human leukemia cell lines with different resistance mechanisms to antifolate drugs., Jpn. J. Cancer Res.
Li et al., 1995, Antitumor activity of antifolate inhibitors of thymidylate and purine synthesis in human soft tissue sarcoma cell lines with intrinsic resistance to methotrexate., Clin. Cancer Res.

RALTITREXED TYMS

Interaction Score: 3.94

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name raltitrexed, ZD-1694,Tomudex

Specific Action of the Ligand Inhibition

PMIDs:
10430100 10496350 10592235 10598555 10482907 18773878 10499608 11752352 10047461 17203168 16456808 15353299

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB
RALTITREXED SLC19A1

Interaction Score: 3.31

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21879757 11705857

Sources:
DTC PharmGKB
RALTITREXED DHFR

Interaction Score: 1.71

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8698629 9816025

Sources:
NCI
RALTITREXED CDKN1B

Interaction Score: 1.52

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10047461

Sources:
NCI
RALTITREXED ALB

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15025739

Sources:
NCI
RALTITREXED BCL2

Interaction Score: 0.41

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10785598

Sources:
NCI
RALTITREXED CDK2

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10047461

Sources:
NCI

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

RALTITREXED Primary Drug Name

Drug Info:

Drug Class antineoplastic agents

Year of Approval not approved by the fda

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

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval not approved

Publications:

NCI: ZD1694

Version: 14-September-2017

Alternate Names:

C1804 NCI drug code

Drug Info:

Publications:

Peters et al., 2000, Molecular downstream events and induction of thymidylate synthase in mutant and wild-type p53 colon cancer cell lines after treatment with 5-fluorouracil and the thymidylate synthase inhibitor raltitrexed., Eur. J. Cancer

Takemura et al., 1996, Biological activity and intracellular metabolism of ZD1694 in human leukemia cell lines with different resistance mechanisms to antifolate drugs., Jpn. J. Cancer Res.

NCI: TOMUDEX

Version: 14-September-2017

Alternate Names:

C1804 NCI drug code

Drug Info:

Publications:

Li et al., 1995, Antitumor activity of antifolate inhibitors of thymidylate and purine synthesis in human soft tissue sarcoma cell lines with intrinsic resistance to methotrexate., Clin. Cancer Res.

Yin et al., 1999, Cyclin E-cdk2 activation is associated with cell cycle arrest and inhibition of DNA replication induced by the thymidylate synthase inhibitor Tomudex., Exp. Cell Res.

NCI: RALTITREXED
- Version: 14-September-2017
Alternate Names:

C1804 NCI drug code

Drug Info:

Publications:

Blair et al., 2004, Population pharmacokinetics of raltitrexed in patients with advanced solid tumours., Br J Clin Pharmacol

DTC: RALTITREXED

Version: 02-September-2020

Alternate Names:

CHEMBL225071 ChEMBL Drug ID

Drug Info:

Publications:

Wang L et al., 2011, Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase., J Med Chem

PharmGKB: raltitrexed

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Whetstine JR et al., 2001, Single nucleotide polymorphisms in the human reduced folate carrier: characterization of a high-frequency G/A variant at position 80 and transport properties of the His(27) and Arg(27) carriers., Clin Cancer Res

Salgado J et al., 2007, Polymorphisms in the thymidylate synthase and dihydropyrimidine dehydrogenase genes predict response and toxicity to capecitabine-raltitrexed in colorectal cancer., Oncol Rep

Rustum, 2004, Thymidylate synthase: a critical target in cancer therapy?, Front. Biosci.

TTD: Raltitrexed
- Version: 2020.06.01
Alternate Names:

D01KKQ TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103975
- Version: 29-September-2020
Alternate Names:

RALTITREXED GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL225071
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	raltitrexed, ZD-1694,Tomudex
Specific Action of the Ligand	Inhibition

RALTITREXED Drug Record

RALTITREXED chembl:CHEMBL225071 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

RALTITREXED TYMS

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name raltitrexed, ZD-1694,Tomudex Specific Action of the Ligand Inhibition

PMIDs: 10430100 10496350 10592235 10598555 10482907 18773878 10499608 11752352 10047461 17203168 16456808 15353299

Sources: TdgClinicalTrial TEND GuideToPharmacology PharmGKB

RALTITREXED SLC19A1

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21879757 11705857

Sources: DTC PharmGKB

RALTITREXED DHFR

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8698629 9816025

Sources: NCI

RALTITREXED CDKN1B

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10047461

Sources: NCI

RALTITREXED ALB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15025739

Sources: NCI

RALTITREXED BCL2

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10785598

Sources: NCI

RALTITREXED CDK2

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10047461

Sources: NCI

TEND: RALTITREXED

Alternate Names: RALTITREXED Primary Drug Name

Drug Info: Drug Class antineoplastic agents Year of Approval not approved by the fda

Publications:

TdgClinicalTrial: RALTITREXED

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class Small Molecule FDA Approval not approved

Publications:

NCI: ZD1694

Alternate Names: C1804 NCI drug code

Drug Info:

NCI: TOMUDEX

Alternate Names: C1804 NCI drug code

Drug Info:

NCI: RALTITREXED

Alternate Names: C1804 NCI drug code

Drug Info:

Publications: Blair et al., 2004, Population pharmacokinetics of raltitrexed in patients with advanced solid tumours., Br J Clin Pharmacol

DTC: RALTITREXED

Alternate Names: CHEMBL225071 ChEMBL Drug ID

Drug Info:

PharmGKB: raltitrexed

Alternate Names:

Drug Info:

TTD: Raltitrexed

Alternate Names: D01KKQ TTD Drug ID

Drug Info:

Publications:

GuideToPharmacology: 178103975

Alternate Names: RALTITREXED GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL225071

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name raltitrexed, ZD-1694,Tomudex

Specific Action of the Ligand Inhibition

PMIDs:
10430100 10496350 10592235 10598555 10482907 18773878 10499608 11752352 10047461 17203168 16456808 15353299

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21879757 11705857

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
8698629 9816025

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
10047461

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15025739

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
10785598

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
10047461

Sources:
NCI

Alternate Names:

RALTITREXED Primary Drug Name

Drug Info:

Drug Class antineoplastic agents

Year of Approval not approved by the fda

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval not approved

Alternate Names:

C1804 NCI drug code

Alternate Names:

C1804 NCI drug code

Alternate Names:

C1804 NCI drug code

Publications:

Blair et al., 2004, Population pharmacokinetics of raltitrexed in patients with advanced solid tumours., Br J Clin Pharmacol

Alternate Names:

CHEMBL225071 ChEMBL Drug ID

Alternate Names:

D01KKQ TTD Drug ID

Alternate Names:

RALTITREXED GuideToPharmacology Ligand Name