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RALTITREXED Drug Record

  • Summary
  • Interactions
  • Claims
  • 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
    (5 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: 3.58

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name raltitrexed, ZD-1694,Tomudex

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


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • RALTITREXED   SLC19A1

    Interaction Score: 3.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21879757 11705857


    Sources:
    DTC PharmGKB

  • RALTITREXED   DHFR

    Interaction Score: 1.77

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8698629 9816025


    Sources:
    NCI

  • RALTITREXED   CDKN1B

    Interaction Score: 1.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10047461


    Sources:
    NCI

  • RALTITREXED   ALB

    Interaction Score: 0.84

    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: 0.29

    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:

  • ChemblDrugs: chembl:CHEMBL225071

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21