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7-ETHYL-10-HYDROXYCAMPTOTHECIN Drug Record

  • Summary
  • Interactions
  • Claims
  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN chembl:CHEMBL837 Antineoplastic

    Alternate Names:

    7-ETHYL-10-HYDROXYCAMPTOTHECIN
    NK-012
    NK012
    IRINOTECAN RELATED COMPOUND B
    NK 012
    SN 38
    SN-38
    7-ETHYL-10-HYDROXY-CAMPTOTHECIN
    IT-141

    Drug Info:

    Drug Type small molecule
    Drug Groups investigational
    Drug Categories alkaloids
    Drug Categories antineoplastic agents
    Drug Categories cytochrome p-450 cyp3a inhibitors
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a4 substrates
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories enzyme inhibitors
    Drug Categories topoisomerase i inhibitors
    Drug Categories topoisomerase inhibitors
    (1 More Sources)

    Publications:

    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
    Luo Y et al., 2012, Synthesis and biological evaluation of new homocamptothecin analogs., Eur J Med Chem
    Parrino B et al., 2015, Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action., Eur J Med Chem
    Cananzi S et al., 2011, Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D., Bioorg Med Chem
    Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett
    Clericuzio M et al., 2006, Cucurbitane triterpenes from the fruiting bodies and cultivated mycelia of Leucopaxillus gentianeus., J Nat Prod
    Samorì C et al., 2009, Semisynthesis, biological activity, and molecular modeling studies of C-ring-modified camptothecins., J Med Chem
    Wang L et al., 2015, Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents., Bioorg Med Chem
    Han JY et al., 2006, Comprehensive analysis of UGT1A polymorphisms predictive for pharmacokinetics and treatment outcome in patients with non-small-cell lung cancer treated with irinotecan and cisplatin., J Clin Oncol
    Wang H et al., 2014, Association analysis of UGT1A genotype and haplotype with SN-38 glucuronidation in human livers., Pharmacogenomics
    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
    Han JY et al., 2009, Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer., Lung Cancer
    Li M et al., 2018, ABC transporter polymorphisms are associated with irinotecan pharmacokinetics and neutropenia., Pharmacogenomics J
    Kim KP et al., 2015, A phase I study of UGT1A1 *28/*6 genotype-directed dosing of irinotecan (CPT-11) in Korean patients with metastatic colorectal cancer receiving FOLFIRI., Oncology
    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.
    Stewart CF et al., 2007, UGT1A1 promoter genotype correlates with SN-38 pharmacokinetics, but not severe toxicity in patients receiving low-dose irinotecan., J Clin Oncol
    Mbatchi LC et al., 2016, Effect of Single Nucleotide Polymorphisms in the Xenobiotic-sensing Receptors NR1I2 and NR1I3 on the Pharmacokinetics and Toxicity of Irinotecan in Colorectal Cancer Patients., Clin Pharmacokinet
    Lankisch TO et al., 2008, Gilbert's Syndrome and irinotecan toxicity: combination with UDP-glucuronosyltransferase 1A7 variants increases risk., Cancer Epidemiol Biomarkers Prev
    Jada SR et al., 2007, Role of UGT1A1*6, UGT1A1*28 and ABCG2 c.421C>A polymorphisms in irinotecan-induced neutropenia in Asian cancer patients., Cancer Sci
    Lankisch TO et al., 2006, Gilbert's disease and atazanavir: from phenotype to UDP-glucuronosyltransferase haplotype., Hepatology
    de Jong FA et al., 2007, Irinotecan-induced diarrhea: functional significance of the polymorphic ABCC2 transporter protein., Clin Pharmacol Ther
    Kishi S et al., 2004, Effects of prednisone and genetic polymorphisms on etoposide disposition in children with acute lymphoblastic leukemia., Blood
    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
    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
    Danoff TM et al., 2004, A Gilbert's syndrome UGT1A1 variant confers susceptibility to tranilast-induced hyperbilirubinemia., Pharmacogenomics J
    Hu ZY et al., 2010, Dose-dependent association between UGT1A1*28 genotype and irinotecan-induced neutropenia: low doses also increase risk., Clin Cancer Res
    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
    Hoskins JM et al., 2007, UGT1A1*28 genotype and irinotecan-induced neutropenia: dose matters., J Natl Cancer Inst
    Kemp DC et al., 2002, Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance., Drug Metab Dispos
    Iyer L et al., 2002, UGT1A1*28 polymorphism as a determinant of irinotecan disposition and toxicity., Pharmacogenomics J
    Sai K et al., 2004, UGT1A1 haplotypes associated with reduced glucuronidation and increased serum bilirubin in irinotecan-administered Japanese patients with cancer., Clin Pharmacol Ther
    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
    de Jong FA et al., 2006, Prophylaxis of irinotecan-induced diarrhea with neomycin and potential role for UGT1A1*28 genotype screening: a double-blind, randomized, placebo-controlled study., Oncologist
    Innocenti F et al., 2004, Genetic variants in the UDP-glucuronosyltransferase 1A1 gene predict the risk of severe neutropenia of irinotecan., J Clin Oncol
    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
  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   UGT1A1

    Interaction Score: 1.46

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25427841 16636344 19364970 19852077 17577039 27116457 18349289 17627617 12181437 17058217 17185998 12969965 1651156 18466101 14647407 20562211 19390945 17728214 12019197 18221820 11990381 15179405 10381366 16951398 15007088 11037804


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   CES2

    Interaction Score: 1.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   UGT1A9

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16636344 24897286 12181437 18221820


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   TOP1

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25003995 22647222 25768699 21783369 23622981 17190463 19530720 25835359


    Sources:
    DTC PharmGKB TTD DrugBank

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   UGT1A10

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   UGT1A8

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   UGT1A6

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   UGT1A3

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   UGT1A4

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC11

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC9

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC10

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC7

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC5

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC4

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC3

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC6

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   CES1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC8

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC2

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   HDAC1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23622981


    Sources:
    DTC

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   ABCC1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27845419


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   SLCO1B1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18221820


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   BCHE

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   ABCC2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   ABCG2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • 7-ETHYL-10-HYDROXYCAMPTOTHECIN   ABCB1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • DrugBank: DB05482

    • Version: 5.1.7

    Alternate Names:
    86639-52-3 CAS Number
    NeoLipid Camptosar Drug Brand
    CHEMBL837 ChEMBL ID

    Drug Info:
    Drug Type small molecule
    Drug Groups investigational
    Drug Categories alkaloids

    Publications:

  • DTC: 7-ETHYL-10-HYDROXY-CAMPTOTHECIN

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL837 ChEMBL Drug ID

    Drug Info:

    Publications:
    Guerrant W et al., 2013, Dual-acting histone deacetylase-topoisomerase I inhibitors., Bioorg Med Chem Lett
    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
    Luo Y et al., 2012, Synthesis and biological evaluation of new homocamptothecin analogs., Eur J Med Chem

  • PharmGKB: SN-38

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Han JY et al., 2009, Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer., Lung Cancer
    Kim KP et al., 2015, A phase I study of UGT1A1 *28/*6 genotype-directed dosing of irinotecan (CPT-11) in Korean patients with metastatic colorectal cancer receiving FOLFIRI., Oncology
    Han JY et al., 2006, Comprehensive analysis of UGT1A polymorphisms predictive for pharmacokinetics and treatment outcome in patients with non-small-cell lung cancer treated with irinotecan and cisplatin., J Clin Oncol

  • TTD: IT-141

    • Version: 2020.06.01

    Alternate Names:
    D0K6QU TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL837

    • 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