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DICLOFENAC Drug Record

  • Summary
  • Interactions
  • Claims
  • DICLOFENAC chembl:CHEMBL139 Approved

    Alternate Names:

    ARTHROTEC
    CATAFLAM
    SOLARAZE
    CAMBIA
    VOLTAREN XR
    ZORVOLEX CAPSULES
    VOLTAREN
    VOLTAREN OPHTHALMIC
    DICLOFENAC
    VOLTAREN-XR
    ZORVOLEX
    GP-45840
    DSG318
    2-[(2,6-DICHLOROPHENYL)AMINO]BENZENEACETIC ACID
    CGP-45840B
    CAT458
    [2-(2,6-DICHLOROANILINO)PHENYL]ACETIC ACID
    VOL458
    pubchem.compound:3033
    chembl:CHEMBL139
    chemidplus:15307-86-5
    rxcui:3355
    drugbank:00586

    Drug Info:

    Year of Approval 1988
    Drug Class anti-inflammatory agents, non-steroidal
    Drug Indications for treatment of glaucoma
    Drug Indications analgesic
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications NSAID
    (4 More Sources)

    Publications:

    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Tsutsumi et al., 2004, Endoplasmic reticulum stress response is involved in nonsteroidal anti-inflammatory drug-induced apoptosis., Cell Death Differ.
    Lee SS et al., 2005, Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity., Pharmacogenet Genomics
    Zuurbier et al., 1990, Interaction of myeloperoxidase with diclofenac. Inhibition of the chlorinating activity of myeloperoxidase by diclofenac and oxidation of diclofenac to dihydroxyazobenzene by myeloperoxidase., Biochem. Pharmacol.
    Kämpfer et al., 2003, Cyclooxygenase-1-coupled prostaglandin biosynthesis constitutes an essential prerequisite for skin repair., J. Invest. Dermatol.
    Calkin et al., 2002, Rapid potentiation of endothelium-dependent vasodilation by estradiol in postmenopausal women is mediated via cyclooxygenase 2., J. Clin. Endocrinol. Metab.
    Hinz et al., 2003, Aceclofenac spares cyclooxygenase 1 as a result of limited but sustained biotransformation to diclofenac., Clin. Pharmacol. Ther.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Chavez et al., 2003, Valdecoxib: a review., Clin Ther
    Kirchheiner et al., 2003, Pharmacokinetics of diclofenac and inhibition of cyclooxygenases 1 and 2: no relationship to the CYP2C9 genetic polymorphism in humans., Br J Clin Pharmacol
    Kocaoğlu et al., 1997, Urinary gamma-glutamyl transferase activity in rats with nonsteroidal anti-inflammatory drug-induced nephrotoxicity., Arch. Immunol. Ther. Exp. (Warsz.)
    Blomme et al., 2003, Selective cyclooxygenase-2 inhibition does not affect the healing of cutaneous full-thickness incisional wounds in SKH-1 mice., Br. J. Dermatol.
    Beubler, 2003, [Pharmacology of cyclooxygenase 2 inhibition]., Wien Med Wochenschr
    Rowlinson et al., 2003, A novel mechanism of cyclooxygenase-2 inhibition involving interactions with Ser-530 and Tyr-385., J. Biol. Chem.
    Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med
    Ayuso P et al., 2015, Association study of genetic variants in PLA2G4A, PLCG1, LAT, SYK, and TNFRS11A genes in NSAIDs-induced urticaria and/or angioedema patients., Pharmacogenet Genomics
    Toebak et al., 2008, Differential suppression of dendritic cell cytokine production by anti-inflammatory drugs., Br. J. Dermatol.
    Leemann T et al., 1993, Cytochrome P450TB (CYP2C): a major monooxygenase catalyzing diclofenac 4'-hydroxylation in human liver., Life Sci
    Dai DP et al., 2015, Identification and Functional Assessment of a New CYP2C9 Allelic Variant CYP2C9*59., Drug Metab Dispos
    Llerena A et al., 2014, Interethnic differences in the relevance of CYP2C9 genotype and environmental factors for diclofenac metabolism in Hispanics from Cuba and Spain., Pharmacogenomics J
    Dai DP et al., 2014, CYP2C9 polymorphism analysis in Han Chinese populations: building the largest allele frequency database., Pharmacogenomics J
    Zi J et al., 2010, Effects of CYP2C9*3 and CYP2C9*13 on Diclofenac Metabolism and Inhibition-based Drug-Drug Interactions., Drug Metab Pharmacokinet
    Pilotto A et al., 2007, Genetic susceptibility to nonsteroidal anti-inflammatory drug-related gastroduodenal bleeding: role of cytochrome P450 2C9 polymorphisms., Gastroenterology
    Caviezel et al., 1983, The effect of acetylsalicylic acid and diclofenac on stimulated growth hormone and prolactin secretion in humans., Int J Clin Pharmacol Ther Toxicol
    Kretz-Rommel et al., 1993, Diclofenac covalent protein binding is dependent on acyl glucuronide formation and is inversely related to P450-mediated acute cell injury in cultured rat hepatocytes., Toxicol. Appl. Pharmacol.
    Ware et al., 1998, Immunochemical detection and identification of protein adducts of diclofenac in the small intestine of rats: possible role in allergic reactions., Chem. Res. Toxicol.
    Kim et al., 2004, Cyclooxygenase inhibitors induce apoptosis in oral cavity cancer cells by increased expression of nonsteroidal anti-inflammatory drug-activated gene., Biochem. Biophys. Res. Commun.
    Thorarensen A et al., 2007, Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor., Bioorg Med Chem Lett
  • DICLOFENAC   TNFRSF11A

    Interaction Score: 1.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26398624


    Sources:
    PharmGKB

  • DICLOFENAC   GDF15

    Interaction Score: 1.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15555568


    Sources:
    NCI

  • DICLOFENAC   PLCG1

    Interaction Score: 0.98

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26398624


    Sources:
    PharmGKB

  • DICLOFENAC   CCL17

    Interaction Score: 0.74

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18028503


    Sources:
    NCI

  • DICLOFENAC   PLA2G4A

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26398624


    Sources:
    PharmGKB

  • DICLOFENAC   UGT1A10

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8511777


    Sources:
    NCI

  • DICLOFENAC   CYP2J2

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15861034


    Sources:
    PharmGKB

  • DICLOFENAC   ANPEP

    Interaction Score: 0.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9544613


    Sources:
    NCI

  • DICLOFENAC   UGT1A6

    Interaction Score: 0.45

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8511777


    Sources:
    NCI

  • DICLOFENAC   PTGS1

    Interaction Score: 0.43

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name transdermal diclofenac
    Trial Name PRO-571, diclofenac potassium
    Trial Name NanoEmulsion (diclofenac)

    PMIDs:
    12713596 12414874 12966366 11752352 12852704 12534640


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • DICLOFENAC   PTGS2

    Interaction Score: 0.35

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Cyclooxygenase inhibitor
    Trial Name Cerimon

    PMIDs:
    12588370 12705061 12534640 12925531 12852704 19602986


    Sources:
    TdgClinicalTrial ChemblInteractions TEND PharmGKB

  • DICLOFENAC   GGT1

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9090444


    Sources:
    NCI

  • DICLOFENAC   MPO

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    2173589


    Sources:
    NCI

  • DICLOFENAC   ALB

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17560104


    Sources:
    DTC

  • DICLOFENAC   DDIT3

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15131590


    Sources:
    NCI

  • DICLOFENAC   PRL

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    6642786


    Sources:
    NCI

  • DICLOFENAC   CYP2C9

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300 8417277 25994031 23959274 23400009 20814155 17681167


    Sources:
    DTC PharmGKB

  • DICLOFENAC   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DICLOFENAC   CYP1A2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DICLOFENAC   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • DICLOFENAC   CYP3A4

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • TEND: DICLOFENAC

    • Version: 01-August-2011

    Alternate Names:
    DICLOFENAC Primary Drug Name

    Drug Info:
    Drug Class anti-inflammatory agents, non-steroidal
    Year of Approval 1988

    Publications:

  • TdgClinicalTrial: DICLOFENAC

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications NSAID
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • NCI: DICLOFENAC

    • Version: 14-September-2017

    Alternate Names:
    C28985 NCI drug code

    Drug Info:

    Publications:
    Kretz-Rommel et al., 1993, Diclofenac covalent protein binding is dependent on acyl glucuronide formation and is inversely related to P450-mediated acute cell injury in cultured rat hepatocytes., Toxicol. Appl. Pharmacol.
    Tsutsumi et al., 2004, Endoplasmic reticulum stress response is involved in nonsteroidal anti-inflammatory drug-induced apoptosis., Cell Death Differ.
    Kim et al., 2004, Cyclooxygenase inhibitors induce apoptosis in oral cavity cancer cells by increased expression of nonsteroidal anti-inflammatory drug-activated gene., Biochem. Biophys. Res. Commun.

  • DTC: DICLOFENAC

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL139 ChEMBL Drug ID

    Drug Info:

    Publications:
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Thorarensen A et al., 2007, Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor., Bioorg Med Chem Lett

  • PharmGKB: diclofenac

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Lee SS et al., 2005, Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity., Pharmacogenet Genomics
    Llerena A et al., 2014, Interethnic differences in the relevance of CYP2C9 genotype and environmental factors for diclofenac metabolism in Hispanics from Cuba and Spain., Pharmacogenomics J
    Dai DP et al., 2015, Identification and Functional Assessment of a New CYP2C9 Allelic Variant CYP2C9*59., Drug Metab Dispos

  • TTD: Diclofenac

    • Version: 2020.06.01

    Alternate Names:
    D0TG1H TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL139

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL139

    • 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.

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