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ETOPOSIDE Drug Record

  • Summary
  • Interactions
  • Claims
  • ETOPOSIDE chembl:CHEMBL44657 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    NSC-141540
    VP-16-213
    TOPOSAR
    VEPESID
    ETOPOSIDE
    TRANS-ETOPOSIDE
    ETOPOSIDO
    VP-16
    VEPESID®
    ETOPOSIDUM
    9-((4,6-O-ETHYLIDINE-BETA-D-GLUCOPYRANOSYL)OXY)-5,8,8A,9-TETRAHYDRO-5-(4-HYDROXY-3,4-DIMETHYLOXYPHENYL)FURO(3',4'':6,7)NAPTHO-(2,3-D)-1,3-DIOXOL-6(5AH)-ONE
    ETOPOPHOS®
    VP 16-213
    4'-DEMETHYLEPIPODOPHYLLOTOXIN 9-(4,6-O-(R)-ETHYLIDENE-BETA-D-GLUCOPYRANOSIDE)
    (−)-ETOPOSIDE
    TOPOSAR®
    4-DEMETHYLEPIPODOPHYLLOTOXIN Β-D-ETHYLIDENEGLUCOSIDE
    4-DEMETHYLEPIPODOPHYLLOTOXIN BETA-D-ETHYLIDENEGLUCOSIDE
    (-)-ETOPOSIDE
    pubchem.compound:36462
    drugbank:00773
    chembl:CHEMBL44657
    chemidplus:33419-42-0
    rxcui:4179

    Drug Info:

    FDA Approval 1983
    Drug Class small molecule
    Drug Indications Antineoplastic Agents
    Year of Approval 1983
    Drug Class antineoplastic agents
    (7 More Sources)

    Publications:

    Kamal A et al., 2013, Synthesis and study of benzothiazole conjugates in the control of cell proliferation by modulating Ras/MEK/ERK-dependent pathway in MCF-7 cells., Bioorg Med Chem Lett
    Kaneko et al., 2002, Intensified chemotherapy increases the survival rates in patients with stage 4 neuroblastoma with MYCN amplification., J. Pediatr. Hematol. Oncol.
    Stachelek et al., 2015, YU238259 Is a Novel Inhibitor of Homology-Dependent DNA Repair That Exhibits Synthetic Lethality and Radiosensitization in Repair-Deficient Tumors., Mol. Cancer Res.
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Jeffrey et al., 2002, Inhibition of protein synthesis in apoptosis: differential requirements by the tumor necrosis factor alpha family and a DNA-damaging agent for caspases and the double-stranded RNA-dependent protein kinase., Cancer Res.
    Hida et al., 2004, Nitric oxide acts on the mitochondria and protects human endothelial cells from apoptosis., J. Lab. Clin. Med.
    de Lucio et al., 2005, Characterization of human NSCLC cell line with innate etoposide-resistance mediated by cytoplasmic localization of topoisomerase II alpha., Cancer Sci.
    Winnicka et al., Cardiac glycosides in cancer research and cancer therapy., Acta Pol Pharm
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    López-Lázaro et al., 2005, Digitoxin inhibits the growth of cancer cell lines at concentrations commonly found in cardiac patients., J. Nat. Prod.
    Moneypenny et al., 2006, MLL rearrangements are induced by low doses of etoposide in human fetal hematopoietic stem cells., Carcinogenesis
    Uesaka et al., 2007, Enhanced expression of DNA topoisomerase II genes in human medulloblastoma and its possible association with etoposide sensitivity., J. Neurooncol.
    McPherson et al., Selective sensitization of adriamycin-resistant P388 murine leukemia cells to antineoplastic agents following transfection with human DNA topoisomerase II alpha., Anticancer Res.
    Nitiss et al., 1998, The bis(naphthalimide) DMP-840 causes cytotoxicity by its action against eukaryotic topoisomerase II., Biochemistry
    Brown et al., 1998, Immunohistochemical staining for DNA topoisomerase IIa in Hodgkin's disease., Am. J. Clin. Pathol.
    Asano et al., 1996, Transfection of human topoisomerase II alpha into etoposide-resistant cells: transient increase in sensitivity followed by down-regulation of the endogenous gene., Biochem. J.
    Asano et al., 1996, Transfection of a human topoisomerase II alpha gene into etoposide-resistant human breast tumor cells sensitizes the cells to etoposide., Oncol. Res.
    Negi A et al., 2015, Imine/amide-imidazole conjugates derived from 5-amino-4-cyano-N1-substituted benzyl imidazole: Microwave-assisted synthesis and anticancer activity via selective topoisomerase-II-α inhibition., Bioorg Med Chem
    Zhang X et al., 2013, The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase., Bioorg Med Chem
    Chee GL et al., 2010, A diazirine-based photoaffinity etoposide probe for labeling topoisomerase II., Bioorg Med Chem
    Chaniyara R et al., 2013, Novel antitumor indolizino[6,7-b]indoles with multiple modes of action: DNA cross-linking and topoisomerase I and II inhibition., J Med Chem
    de Oliveira Figueiredo P et al., 2014, Further constituents of Galianthe thalictroides (Rubiaceae) and inhibition of DNA topoisomerases I and IIα by its cytotoxic β-carboline alkaloids., Bioorg Med Chem Lett
    Li YB et al., 2013, Discovery, synthesis and biological evaluation of cycloprotoberberine derivatives as potential antitumor agents., Eur J Med Chem
    Shankaraiah N et al., 2015, One-pot synthesis of podophyllotoxin-thiourea congeners by employing NH₂SO₃H/NaI: Anticancer activity, DNA topoisomerase-II inhibition, and apoptosis inducing agents., Bioorg Med Chem Lett
    Jiménez-Alonso S et al., 2008, Design and synthesis of a novel series of pyranonaphthoquinones as topoisomerase II catalytic inhibitors., J Med Chem
    Liu LP et al., 2014, Topoisomerase II inhibitors from the roots of Stellera chamaejasme L., Bioorg Med Chem
    Zhao W et al., 2014, A rational design strategy of the novel topoisomerase II inhibitors for the synthesis of the 4-O-(2-pyrazinecarboxylic)-4'-demethylepipodophyllotoxin with antitumor activity by diminishing the relaxation reaction of topoisomerase II-DNA decatenation., Bioorg Med Chem
    Tan S et al., 2013, Oxo-heterocyclic fused naphthalimides as antitumor agents: synthesis and biological evaluation., Eur J Med Chem
    Yadav AA et al., 2015, Structure-based design, synthesis and biological testing of piperazine-linked bis-epipodophyllotoxin etoposide analogs., Bioorg Med Chem
    Chen W et al., 2014, Design and synthesis of 2-phenylnaphthalenoids as inhibitors of DNA topoisomeraseIIα and antitumor agents., Eur J Med Chem
    Kamal A et al., 2012, Synthesis and biological evaluation of 4β-sulphonamido and 4β-[(4'-sulphonamido)benzamide]podophyllotoxins as DNA topoisomerase-IIα and apoptosis inducing agents., Bioorg Med Chem
    Qiu J et al., 2015, Synthesis, biological evaluation and modeling studies of terphenyl topoisomerase IIα inhibitors as anticancer agents., Eur J Med Chem
    Hajbi Y et al., 2010, Synthesis and biological activities of new furo[3,4-b]carbazoles: potential topoisomerase II inhibitors., Eur J Med Chem
    Chen TC et al., 2015, Structure-based hybridization, synthesis and biological evaluation of novel tetracyclic heterocyclic azathioxanthone analogues as potential antitumor agents., Eur J Med Chem
    Oppegard LM et al., 2012, Inhibition of human topoisomerases I and II by simocyclinone D8., J Nat Prod
    He S et al., 2015, Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors., ACS Med Chem Lett
    Genès C et al., 2011, Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents., Eur J Med Chem
    Baviskar AT et al., 2015, Switch in Site of Inhibition: A Strategy for Structure-Based Discovery of Human Topoisomerase IIα Catalytic Inhibitors., ACS Med Chem Lett
    Aleksić M et al., 2014, Anilides and quinolones with nitrogen-bearing substituents from benzothiophene and thienothiophene series: synthesis, photochemical synthesis, cytostatic evaluation, 3D-derived QSAR analysis and DNA-binding properties., Eur J Med Chem
    Lemster T et al., 2009, Photochemical electrocyclisation of 3-vinylindoles to pyrido[2,3-a]-, pyrido[4,3-a]- and thieno[2,3-a]-carbazoles: design, synthesis, DNA binding and antitumor cell cytotoxicity., Eur J Med Chem
    Hasinoff et al., 2008, The structure-based design, synthesis and biological evaluation of DNA-binding bisintercalating bisanthrapyrazole anticancer compounds., Bioorg. Med. Chem.
    Hao H et al., 2015, Design and synthesis of 2-phenylnaphthalenoids and 2-phenylbenzofuranoids as DNA topoisomerase inhibitors and antitumor agents., Eur J Med Chem
    Baviskar AT et al., 2011, N-fused imidazoles as novel anticancer agents that inhibit catalytic activity of topoisomerase IIα and induce apoptosis in G1/S phase., J Med Chem
    Zhou Y et al., 2013, Synthesis, cytotoxicity and topoisomerase II inhibitory activity of lomefloxacin derivatives., Bioorg Med Chem Lett
    Sperry J et al., 2009, Pyranonaphthoquinone derivatives of eleutherin, ventiloquinone L, thysanone and nanaomycin A possessing a diverse topoisomerase II inhibition and cytotoxicity spectrum., Bioorg Med Chem
    Kamal A et al., 2015, Design and synthesis of dithiocarbamate linked β-carboline derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability., Bioorg Med Chem
    Wang MJ et al., 2014, Design, synthesis, mechanisms of action, and toxicity of novel 20(s)-sulfonylamidine derivatives of camptothecin as potent antitumor agents., J Med Chem
    Furbacher TR et al., 2001, Catalytic inhibition of topoisomerase IIalpha by demethylzeylasterone, a 6-oxophenolic triterpenoid from Kokoona zeylanica., J Nat Prod
    Baviskar AT et al., 2013, Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity., Bioorg Med Chem
    Huang ZH et al., 2013, Design, synthesis and biological evaluation of novel mansonone E derivatives prepared via CuAAC click chemistry as topoisomerase II inhibitors., Eur J Med Chem
    Aleksić M et al., 2012, Novel substituted benzothiophene and thienothiophene carboxanilides and quinolones: synthesis, photochemical synthesis, DNA-binding properties, antitumor evaluation and 3D-derived QSAR analysis., J Med Chem
    Ashour A et al., 2014, Rational design and synthesis of topoisomerase I and II inhibitors based on oleanolic acid moiety for new anti-cancer drugs., Bioorg Med Chem
    Bar FM et al., 2009, Rational design and semisynthesis of betulinic acid analogues as potent topoisomerase inhibitors., J Nat Prod
    Mariani A et al., 2015, Differential Targeting of Human Topoisomerase II Isoforms with Small Molecules., J Med Chem
    Dunlap N et al., 2014, Synthesis and evaluation of ether-linked demethylepipodophyllotoxin dimers., Bioorg Med Chem Lett
    Dong G et al., 2012, New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure-activity relationship analysis and biological evaluations., J Med Chem
    Su TL et al., 2006, Potent antitumor 9-anilinoacridines and acridines bearing an alkylating N-mustard residue on the acridine chromophore: synthesis and biological activity., J Med Chem
    Liu JF et al., 2013, Synthesis and cytotoxic activity on human cancer cells of carbamate derivatives of 4β-(1,2,3-triazol-1-yl)podophyllotoxin., Eur J Med Chem
    Kishi S et al., 2004, Effects of prednisone and genetic polymorphisms on etoposide disposition in children with acute lymphoblastic leukemia., Blood
    Benderra et al., 1998, Role of the vacuolar H+-ATPase in daunorubicin distribution in etoposide-resistant MCF7 cells overexpressing the multidrug-resistance associated protein., Int. J. Oncol.
    Lorico et al., 1995, Increased rate of adenosine triphosphate-dependent etoposide (VP-16) efflux in a murine leukemia cell line overexpressing the multidrug resistance-associated protein (MRP) gene., Cancer Res.
    Drenberg CD et al., 2016, Inherited variation in OATP1B1 is associated with treatment outcome in acute myeloid leukemia., Clin Pharmacol Ther
    Azarova et al., 2007, Roles of DNA topoisomerase II isozymes in chemotherapy and secondary malignancies., Proc. Natl. Acad. Sci. U.S.A.
    Munshi et al., 2001, Chemotherapy in patients with prostate specific antigen-only disease after primary therapy for prostate carcinoma: a phase II trial of oral estramustine and oral etoposide., Cancer
    Imamura et al., 1986, [Successful chemotherapy in undescended testicular and extragonadal germ cell tumors: report of 2 cases]., Gan To Kagaku Ryoho
    Whelan et al., 1992, Successful treatment of a primary endodermal sinus tumor of the liver., Cancer
    Wu C et al., 2010, Genome-wide interrogation identifies YAP1 variants associated with survival of small-cell lung cancer patients., Cancer Res
    Jabado et al., 1997, Treatment of familial hemophagocytic lymphohistiocytosis with bone marrow transplantation from HLA genetically nonidentical donors., Blood
    Keller et al., 2016, A Novel EGFR Extracellular Domain Mutant, EGFRΔ768, Possesses Distinct Biological and Biochemical Properties in Neuroblastoma., Mol. Cancer Res.
    Lund et al., 2004, Autocrine inhibition of chemotherapy response in human liver tumor cells by insulin-like growth factor-II., Cancer Lett.
    Watanabe et al., 2003, Glucuronidation of etoposide in human liver microsomes is specifically catalyzed by UDP-glucuronosyltransferase 1A1., Drug Metab. Dispos.
    Tan et al., 2000, PTGF-beta, a type beta transforming growth factor (TGF-beta) superfamily member, is a p53 target gene that inhibits tumor cell growth via TGF-beta signaling pathway., Proc. Natl. Acad. Sci. U.S.A.
    Zhang et al., 1998, Regulation of membrane release in apoptosis., Biochem. J.
    Harding et al., 2013, Blockade of nonhormonal fibroblast growth factors by FP-1039 inhibits growth of multiple types of cancer., Sci Transl Med
    Bataille F et al., 2003, Alterations in p53 predict response to preoperative high dose chemotherapy in patients with gastric cancer., Mol Pathol
    Carrillo et al., 2015, Pharmacologically Increasing Mdm2 Inhibits DNA Repair and Cooperates with Genotoxic Agents to Kill p53-Inactivated Ovarian Cancer Cells., Mol. Cancer Res.
    Brachova P et al., 2013, The consequence of oncomorphic TP53 mutations in ovarian cancer., Int J Mol Sci
    Yamagishi et al., 2001, Reciprocal control of expression of mRNAs for osteoclast differentiation factor and OPG in osteogenic stromal cells by genistein: evidence for the involvement of topoisomerase II in osteoclastogenesis., Endocrinology
    Banerjee et al., 1998, Role of E2F-1 in chemosensitivity., Cancer Res.
    Russo et al., 2006, E2F-1 overexpression in U2OS cells increases cyclin B1 levels and cdc2 kinase activity and sensitizes cells to antimitotic agents., Cancer Res.
    Yamasaki S et al., 2015, UGT1A1 *6 polymorphism predicts outcome in elderly patients with relapsed or refractory diffuse large B-cell lymphoma treated with carboplatin, dexamethasone, etoposide and irinotecan., Ann Hematol
    Ciotti M et al., 1999, Glucuronidation of 7-ethyl-10-hydroxycamptothecin (SN-38) by the human UDP-glucuronosyltransferases encoded at the UGT1 locus., Biochem Biophys Res Commun
    Hu ZY et al., 2010, Dose-dependent association between UGT1A1*28 genotype and irinotecan-induced neutropenia: low doses also increase risk., Clin Cancer Res
    Ramesh et al., 2010, Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives., Biomed. Chromatogr.
    Onoue M et al., 2009, UGT1A1*6 polymorphism is most predictive of severe neutropenia induced by irinotecan in Japanese cancer patients., Int J Clin Oncol
    Cecchin E et al., 2009, Predictive role of the UGT1A1, UGT1A7, and UGT1A9 genetic variants and their haplotypes on the outcome of metastatic colorectal cancer patients treated with fluorouracil, leucovorin, and irinotecan., J Clin Oncol
    Obradovic M et al., 2008, Cost-effectiveness of UGT1A1 genotyping in second-line, high-dose, once every 3 weeks irinotecan monotherapy treatment of colorectal cancer., Pharmacogenomics
    Lankisch TO et al., 2008, Gilbert's Syndrome and irinotecan toxicity: combination with UDP-glucuronosyltransferase 1A7 variants increases risk., Cancer Epidemiol Biomarkers Prev
    Hoskins JM et al., 2007, UGT1A1*28 genotype and irinotecan-induced neutropenia: dose matters., J Natl Cancer Inst
    Lankisch TO et al., 2006, Gilbert's disease and atazanavir: from phenotype to UDP-glucuronosyltransferase haplotype., Hepatology
    Kawato Y et al., 1991, Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11., Cancer Res
    Danoff TM et al., 2004, A Gilbert's syndrome UGT1A1 variant confers susceptibility to tranilast-induced hyperbilirubinemia., Pharmacogenomics J
    Gagné JF et al., 2002, Common human UGT1A polymorphisms and the altered metabolism of irinotecan active metabolite 7-ethyl-10-hydroxycamptothecin (SN-38)., Mol Pharmacol
    Kemp DC et al., 2002, Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance., Drug Metab Dispos
    Guillemette C et al., 2000, Structural heterogeneity at the UDP-glucuronosyltransferase 1 locus: functional consequences of three novel missense mutations in the human UGT1A7 gene., Pharmacogenetics
    Tao et al., 2003, Profiling of differentially expressed apoptosis-related genes by cDNA arrays in human cord blood CD34+ cells treated with etoposide., Exp. Hematol.
    Eymin et al., 1997, Increased gadd153 messenger RNA level is associated with apoptosis in human leukemic cells treated with etoposide., Cancer Res.
    Ballestrero et al., 2004, Tumor necrosis factor-related apoptosis-inducing ligand cooperates with anticancer drugs to overcome chemoresistance in antiapoptotic Bcl-2 family members expressing jurkat cells., Clin. Cancer Res.
    Baltaci et al., 2001, P53, bcl-2 and bax immunoreactivity as predictors of response and outcome after chemotherapy for metastatic germ cell testicular tumours., BJU Int.
    Mannherz et al., 2005, Activated cofilin colocalises with Arp2/3 complex in apoptotic blebs during programmed cell death., Eur. J. Cell Biol.
    Brown CC et al., 2014, Genome-wide association and pharmacological profiling of 29 anticancer agents using lymphoblastoid cell lines., Pharmacogenomics
    Wang et al., 2005, Activation of transforming growth factor-beta1/p38/Smad3 signaling in stromal cells requires reactive oxygen species-mediated MMP-2 activity during bone marrow damage., Stem Cells
    Thomadaki et al., PAP modulations in Daudi cells and Molt-3 cells treated with etoposide are mutually associated with morphological evidence of apoptosis., Int. J. Biol. Markers
    Fanning et al., 1991, Serial CA 125 levels during chemotherapy for metastatic or recurrent endometrial cancer., Obstet Gynecol
  • ETOPOSIDE   PAPOLA

    Interaction Score: 2.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15503822


    Sources:
    NCI

  • ETOPOSIDE   PLA2G6

    Interaction Score: 2.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24444404


    Sources:
    PharmGKB

  • ETOPOSIDE   ACTR2

    Interaction Score: 2.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15900709


    Sources:
    NCI

  • ETOPOSIDE   DYNC2H1

    Interaction Score: 2.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21118971


    Sources:
    PharmGKB

  • ETOPOSIDE   TOP2A

    Interaction Score: 0.85

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction DNA topoisomerase II inhibitor
    Trial Name -

    PMIDs:
    16271071 17514873 11752352 16309315 16377807 17361331 9494516 9485461 9426516 8870683 8823806 26216018 24095018 20006518 23360284 24507920 24012683 26292628 18816045 24931277 24775914 23353750 25922181 25240702 22364746 25800514 20863598 25799376 22867097 25815139 21435753 25941559 24334150 19386396 18258442 26291037 21644529 23566520 19783445 26264845 25003995 11678653 23920485 23968711 22620261 24326278 19691293 25945730 25466187 22867019 16759114 23711769


    Sources:
    DTC TdgClinicalTrial ChemblInteractions NCI TEND

  • ETOPOSIDE   EIF4E

    Interaction Score: 0.79

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11956083


    Sources:
    NCI

  • ETOPOSIDE   BTF3P11

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11459812


    Sources:
    NCI

  • ETOPOSIDE   SLIT1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ETOPOSIDE   UGT1A1

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25055799 10381366 20562211 19852077 19390945 19364970 18466101 18349289 17728214 17058217 1651156 14647407 12969965 12181437 12019197 11037804


    Sources:
    PharmGKB

  • ETOPOSIDE   TNFSF13B

    Interaction Score: 0.48

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12644023


    Sources:
    NCI

  • ETOPOSIDE   GDF15

    Interaction Score: 0.48

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10618379


    Sources:
    NCI

  • ETOPOSIDE   PGP

    Interaction Score: 0.4

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers

  • ETOPOSIDE   MUC16

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1988893


    Sources:
    NCI

  • ETOPOSIDE   AFP

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2427033 1382827


    Sources:
    NCI

  • ETOPOSIDE   NCOA1

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ETOPOSIDE   MYCN

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12439032


    Sources:
    NCI

  • ETOPOSIDE   UGT1A10

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12695347


    Sources:
    NCI

  • ETOPOSIDE   TOP2B

    Interaction Score: 0.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction DNA topoisomerase II inhibitor
    Direct Interaction yes

    PMIDs:
    26264845 16309315 25945730 22364746 17578914


    Sources:
    DTC ChemblInteractions TTD

  • ETOPOSIDE   E2F1

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9766655 16849574


    Sources:
    NCI

  • ETOPOSIDE   IGF2

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15019164


    Sources:
    NCI

  • ETOPOSIDE   ITGAL

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9389690


    Sources:
    NCI

  • ETOPOSIDE   NCOA3

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ETOPOSIDE   KLK3

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11391599


    Sources:
    NCI

  • ETOPOSIDE   ERCC2

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ETOPOSIDE   GSTT1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ETOPOSIDE   PLA2G1B

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9716508


    Sources:
    NCI

  • ETOPOSIDE   BRCA2

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    26116172


    Sources:
    JAX-CKB

  • ETOPOSIDE   TYMSOS

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ETOPOSIDE   DDIT3

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9044846


    Sources:
    NCI

  • ETOPOSIDE   BCL2

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14977850 11350408


    Sources:
    NCI

  • ETOPOSIDE   CHEK1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22364746


    Sources:
    DTC

  • ETOPOSIDE   ABCC1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9472114 7671247


    Sources:
    NCI

  • ETOPOSIDE   ERCC1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ETOPOSIDE   TGFB1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16002781


    Sources:
    NCI

  • ETOPOSIDE   MAPK3

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23999041


    Sources:
    DTC

  • ETOPOSIDE   GSTP1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12969965


    Sources:
    PharmGKB

  • ETOPOSIDE   BAX

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15454884


    Sources:
    NCI

  • ETOPOSIDE   SLCO1B1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26663398


    Sources:
    PharmGKB

  • ETOPOSIDE   ATM

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22364746


    Sources:
    DTC

  • ETOPOSIDE   TYMS

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ETOPOSIDE   FGFR1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Cisplatin + Etoposide + GSK3052230
    Indication/Tumor Type lung small cell carcinoma
    Response Type sensitive

    PMIDs:
    23536011


    Sources:
    JAX-CKB

  • ETOPOSIDE   TP53

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Nutlin-3 + Etoposide
    Indication/Tumor Type ovarian cancer
    Response Type sensitive

    PMIDs:
    14514923 25964101 24065105


    Sources:
    JAX-CKB CIViC

  • ETOPOSIDE   MAPK1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23999041


    Sources:
    DTC

  • ETOPOSIDE   EGFR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type neuroblastoma
    Response Type resistant
    Approval Status Preclinical - Cell culture

    PMIDs:
    27216155


    Sources:
    JAX-CKB

  • ETOPOSIDE   ABCB1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12969965


    Sources:
    PharmGKB

  • ETOPOSIDE   GLP1R

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ETOPOSIDE   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ETOPOSIDE   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ETOPOSIDE   CYP1A2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ETOPOSIDE   CYP2D6

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ETOPOSIDE   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC PharmGKB

  • ETOPOSIDE   GMNN

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TEND: ETOPOSIDE

    • Version: 01-August-2011

    Alternate Names:
    ETOPOSIDE Primary Drug Name

    Drug Info:
    Drug Class antineoplastic agents
    Year of Approval 1983

    Publications:

  • TdgClinicalTrial: ETOPOSIDE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Antineoplastic Agents
    Drug Class small molecule
    FDA Approval 1983

    Publications:

  • NCI: ETOPOSIDE

    • Version: 14-September-2017

    Alternate Names:
    C491 NCI drug code

    Drug Info:

    Publications:
    Yamagishi et al., 2001, Reciprocal control of expression of mRNAs for osteoclast differentiation factor and OPG in osteogenic stromal cells by genistein: evidence for the involvement of topoisomerase II in osteoclastogenesis., Endocrinology
    Tao et al., 2003, Profiling of differentially expressed apoptosis-related genes by cDNA arrays in human cord blood CD34+ cells treated with etoposide., Exp. Hematol.
    Eymin et al., 1997, Increased gadd153 messenger RNA level is associated with apoptosis in human leukemic cells treated with etoposide., Cancer Res.

  • DTC: ETOPOSIDE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL44657 ChEMBL Drug ID

    Drug Info:

    Publications:
    López-Lázaro et al., 2005, Digitoxin inhibits the growth of cancer cell lines at concentrations commonly found in cardiac patients., J. Nat. Prod.
    Mariani A et al., 2015, Differential Targeting of Human Topoisomerase II Isoforms with Small Molecules., J Med Chem
    Kamal A et al., 2015, Design and synthesis of dithiocarbamate linked β-carboline derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability., Bioorg Med Chem

  • PharmGKB: etoposide

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Cecchin E et al., 2009, Predictive role of the UGT1A1, UGT1A7, and UGT1A9 genetic variants and their haplotypes on the outcome of metastatic colorectal cancer patients treated with fluorouracil, leucovorin, and irinotecan., J Clin Oncol
    Ramesh et al., 2010, Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives., Biomed. Chromatogr.
    Lankisch TO et al., 2008, Gilbert's Syndrome and irinotecan toxicity: combination with UDP-glucuronosyltransferase 1A7 variants increases risk., Cancer Epidemiol Biomarkers Prev

  • JAX-CKB: Etoposide

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Stachelek et al., 2015, YU238259 Is a Novel Inhibitor of Homology-Dependent DNA Repair That Exhibits Synthetic Lethality and Radiosensitization in Repair-Deficient Tumors., Mol. Cancer Res.
    Harding et al., 2013, Blockade of nonhormonal fibroblast growth factors by FP-1039 inhibits growth of multiple types of cancer., Sci Transl Med
    Keller et al., 2016, A Novel EGFR Extracellular Domain Mutant, EGFRΔ768, Possesses Distinct Biological and Biochemical Properties in Neuroblastoma., Mol. Cancer Res.

  • CIViC: ETOPOSIDE

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Bataille F et al., 2003, Alterations in p53 predict response to preoperative high dose chemotherapy in patients with gastric cancer., Mol Pathol
    Brachova P et al., 2013, The consequence of oncomorphic TP53 mutations in ovarian cancer., Int J Mol Sci

  • TTD: Etoposide

    • Version: 2020.06.01

    Alternate Names:
    D0B7EB TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL44657

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: ETOPOSIDE

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL44657

    • Version: chembl_23

    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.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

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