DGIdb - DICLOFENAC Drug Record

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 CYP2C93 and CYP2C913 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:

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

Direct Interaction	yes
Mechanism of Interaction	Cyclooxygenase inhibitor
Trial Name	Cerimon

DICLOFENAC Drug Record

DICLOFENAC chembl:CHEMBL139 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26398624

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15555568

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26398624

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18028503

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26398624

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8511777

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15861034

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9544613

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8511777

Sources: NCI

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

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9090444

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2173589

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17560104

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15131590

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 6642786

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300 8417277 25994031 23959274 23400009 20814155 17681167

Sources: DTC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Interaction Types & Directionality:

n/a

PMIDs:
26398624

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15555568

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
26398624

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18028503

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
26398624

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
8511777

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
15861034

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9544613

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8511777

Sources:
NCI

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

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

Interaction Types & Directionality:

n/a

PMIDs:
9090444

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
2173589

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
17560104

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
15131590

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
6642786

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
22931300 8417277 25994031 23959274 23400009 20814155 17681167

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Alternate Names:

DICLOFENAC Primary Drug Name

Drug Info:

Drug Class anti-inflammatory agents, non-steroidal

Year of Approval 1988

Drug Info:

Drug Indications NSAID

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C28985 NCI drug code

Alternate Names:

CHEMBL139 ChEMBL Drug ID

Alternate Names:

D0TG1H TTD Drug ID