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TOPOTECAN Drug Record

  • Summary
  • Interactions
  • Claims
  • TOPOTECAN chembl:CHEMBL84 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    TOPOTECAN
    HYCAMTIN
    NSC-609699
    POTACTASOL
    SKF-104864
    9-[(DIMETHYLAMINO)METHYL]-10-HYDROXY-(4S)-CAMPTOTHECIN
    TOPOTECANE
    SK-S-104864-A
    TOPOTECANUM
    HYCAMTIN®
    chemidplus:123948-87-8
    drugbank:01030
    rxcui:57308
    pubchem.compound:60700
    chembl:CHEMBL84

    Drug Info:

    Year of Approval 1996
    Drug Class antineoplastic agents
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antineoplastic agent
    (6 More Sources)

    Publications:

    Gálvez-Peralta M et al., 2009, On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents., Bioorg Med Chem Lett
    Kiselev E et al., 2014, Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells., J Med Chem
    Kollmannsberger et al., 1999, Topotecan - A novel topoisomerase I inhibitor: pharmacology and clinical experience., Oncology
    Dennis et al., 1997, An overview of the clinical pharmacology of topotecan., Semin. Oncol.
    Schmidt et al., 2001, Glioma cell sensitivity to topotecan: the role of p53 and topotecan-induced DNA damage., Eur. J. Pharmacol.
    strel'tsov et al., [Interaction of topotecan--a DNA topoisomerase I inhibitor--with dual-stranded polydeoxyribonucleotides. II. Formation of a complex containing several DNA molecules in the presence of topotecan]., Mol. Biol. (Mosk.)
    Aisner et al., 2003, Sequencing topotecan and etoposide plus cisplatin to overcome topoisomerase I and II resistance: a pharmacodynamically based Phase I trial., Clin. Cancer Res.
    Zhang et al., 2002, [Preliminary study of apoptosis of human hepatocarcinoma cell line HepG2 induced by topotecan]., Ai Zheng
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Herben et al., 1996, Clinical pharmacokinetics of topotecan., Clin Pharmacokinet
    Streltsov, 2002, Action models for the antitumor drug camptothecin: formation of alkali-labile complex with DNA and inhibition of human DNA topoisomerase I., J. Biomol. Struct. Dyn.
    Kosovsky et al., 1993, Immunological identification of human platelet mitochondrial DNA topoisomerase I., Biochim. Biophys. Acta
    Krytska et al., 2016, Crizotinib Synergizes with Chemotherapy in Preclinical Models of Neuroblastoma., Clin. Cancer Res.
    Brown CC et al., 2014, Genome-wide association and pharmacological profiling of 29 anticancer agents using lymphoblastoid cell lines., Pharmacogenomics
    Fiorino F et al., 2011, Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents., Eur J Med Chem
    Wick et al., 2004, Chemotherapy-induced cell death in primary cerebellar granule neurons but not in astrocytes: in vitro paradigm of differential neurotoxicity., J. Neurochem.
    Koschmann et al., 2016, ATRX loss promotes tumor growth and impairs nonhomologous end joining DNA repair in glioma., Sci Transl Med
    Voeller et al., 2000, Identification and proposed mechanism of action of thymidine kinase inhibition associated with cellular exposure to camptothecin analogs., Cancer Chemother. Pharmacol.
    Coleman et al., 2007, Early changes in CA125 after treatment with pegylated liposomal doxorubicin or topotecan do not always reflect best response in recurrent ovarian cancer patients., Oncologist
    Thanapprapasr et al., 2015, PTEN Expression as a Predictor of Response to Focal Adhesion Kinase Inhibition in Uterine Cancer., Mol. Cancer Ther.
    Bisi et al., 2016, Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression., Mol. Cancer Ther.
    Roberts JK et al., 2016, Population Pharmacokinetics of Oral Topotecan in Infants and Very Young Children with Brain Tumors Demonstrates a Role of ABCG2 rs4148157 on the Absorption Rate Constant., Drug Metab Dispos
    Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.
  • TOPOTECAN   DDO

    Interaction Score: 2.75

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24444404


    Sources:
    PharmGKB

  • TOPOTECAN   TOP1MT

    Interaction Score: 2.75

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    8390858


    Sources:
    TEND

  • TOPOTECAN   MUC16

    Interaction Score: 1.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17227902


    Sources:
    NCI

  • TOPOTECAN   ATRX

    Interaction Score: 0.92

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    26936505


    Sources:
    JAX-CKB

  • TOPOTECAN   TOP1

    Interaction Score: 0.74

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name topotecan,Hycamtin
    Novel drug target Established target

    PMIDs:
    19501511 24502276 9885371 9122737 11166732 11443926 12855624 12520736 11752352 8853931 12437383


    Sources:
    DTC ClearityFoundationBiomarkers TdgClinicalTrial ClearityFoundationClinicalTrial TEND TTD

  • TOPOTECAN   RB1

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell line xenograft
    Response Type sensitive

    PMIDs:
    26826116


    Sources:
    JAX-CKB

  • TOPOTECAN   TYMS

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10803925


    Sources:
    NCI

  • TOPOTECAN   ALK

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Crizotinib + Cyclophosphamide + Topotecan
    Indication/Tumor Type neuroblastoma
    Response Type no benefit

    PMIDs:
    26438783


    Sources:
    JAX-CKB

  • TOPOTECAN   ABCG2

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27052877


    Sources:
    PharmGKB

  • TOPOTECAN   BDNF

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15569250


    Sources:
    NCI

  • TOPOTECAN   AKT1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21440338


    Sources:
    DTC

  • TOPOTECAN   PTEN

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    25833835


    Sources:
    JAX-CKB

  • TOPOTECAN   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bortezomib + Temsirolimus + Topotecan
    Indication/Tumor Type small intestine adenocarcinoma
    Response Type resistant

    PMIDs:
    21216929


    Sources:
    JAX-CKB

  • TOPOTECAN   TP53

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Crizotinib + Cyclophosphamide + Topotecan
    Indication/Tumor Type neuroblastoma
    Response Type no benefit

    PMIDs:
    26438783


    Sources:
    JAX-CKB

  • TOPOTECAN   ABCB1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • TEND: TOPOTECAN

    • Version: 01-August-2011

    Alternate Names:
    TOPOTECAN Primary Drug Name

    Drug Info:
    Drug Class antineoplastic agents
    Year of Approval 1996

    Publications:

  • TdgClinicalTrial: TOPOTECAN

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • NCI: TOPOTECAN

    • Version: 14-September-2017

    Alternate Names:
    C1413 NCI drug code

    Drug Info:

    Publications:
    Wick et al., 2004, Chemotherapy-induced cell death in primary cerebellar granule neurons but not in astrocytes: in vitro paradigm of differential neurotoxicity., J. Neurochem.
    Voeller et al., 2000, Identification and proposed mechanism of action of thymidine kinase inhibition associated with cellular exposure to camptothecin analogs., Cancer Chemother. Pharmacol.
    Coleman et al., 2007, Early changes in CA125 after treatment with pegylated liposomal doxorubicin or topotecan do not always reflect best response in recurrent ovarian cancer patients., Oncologist

  • DTC: TOPOTECAN

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL84 ChEMBL Drug ID

    Drug Info:

    Publications:
    Gálvez-Peralta M et al., 2009, On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents., Bioorg Med Chem Lett
    Kiselev E et al., 2014, Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells., J Med Chem
    Fiorino F et al., 2011, Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents., Eur J Med Chem

  • PharmGKB: topotecan

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Roberts JK et al., 2016, Population Pharmacokinetics of Oral Topotecan in Infants and Very Young Children with Brain Tumors Demonstrates a Role of ABCG2 rs4148157 on the Absorption Rate Constant., Drug Metab Dispos
    Brown CC et al., 2014, Genome-wide association and pharmacological profiling of 29 anticancer agents using lymphoblastoid cell lines., Pharmacogenomics

  • JAX-CKB: Topotecan

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Koschmann et al., 2016, ATRX loss promotes tumor growth and impairs nonhomologous end joining DNA repair in glioma., Sci Transl Med
    Thanapprapasr et al., 2015, PTEN Expression as a Predictor of Response to Focal Adhesion Kinase Inhibition in Uterine Cancer., Mol. Cancer Ther.
    Krytska et al., 2016, Crizotinib Synergizes with Chemotherapy in Preclinical Models of Neuroblastoma., Clin. Cancer Res.

  • TTD: Topotecan

    • Version: 2020.06.01

    Alternate Names:
    D02PMO TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL84

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: TOPOTECAN

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: TOPOTECAN

    • Version: 26-July-2013

    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