DGIdb - INDOMETHACIN Drug Record

INDOMETHACIN chembl:CHEMBL6 ApprovedImmunotherapy

Alternate Names:

INDOMAX-25
INDOCID-R
ARTRACIN SR
INDOLAR
INDOMETHACIN
INDOTARD MR 75
INDOMOD
MOBILAN
INDOMETACIN FARNESIL
ARTRACIN
RHEUMACIN LA
INDOLAR SR
NSC-77541
BERLIND 75 RET
MAXIMET SR
IMBRILON
FLEXIN-50 CONTINUS
INDODERM
INDOMAX-75 SR
INDOFLEX
LEDMECIN
INDOCIN
FLEXIN-75 CONTINUS
INDOPTOL
INDOCID RET
INDO-PAED
RIMACID
TIVORBEX
INDO-LEMMON
INDOMETACIN
FLEXIN-25 CONTINUS
PARDELPRIN MR
SLO-INDO
INDOCIN SR
INDOCID®
INDOMETACINE
INDOMETACINA
ACONIP
1-(P-CHLOROBENZOYL)-5-METHOXY-2-METHYLINDOLE-3-ACETIC ACID
INDOMETACINUM
{1-[(4-CHLOROPHENYL)CARBONYL]-5-METHOXY-2-METHYL-1H-INDOL-3-YL}ACETIC ACID
INDOCIN®
rxcui:5781
chembl:CHEMBL6
pubchem.compound:3715
drugbank:00328
chemidplus:53-86-1

Drug Info:

Year of Approval	approved before 1982
Drug Class	anti-inflammatory agents, non-steroidal
Drug Categories	anti-inflammatory agents
Drug Categories	analgesics
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	NSAID
Drug Categories	acetic acid derivatives and related substances
Drug Categories	agents causing hyperkalemia
Drug Categories	agents that produce hypertension
Drug Categories	anti-inflammatory agents, non-steroidal (non-selective)
Drug Categories	antigout preparations
Drug Categories	antiinflammatory and antirheumatic products
Drug Categories	antiinflammatory and antirheumatic products, non-steroids
Drug Categories	antiinflammatory preparations, non-steroids for topical use
Drug Categories	bsep/abcb11 substrates
Drug Categories	cytochrome p-450 cyp2c19 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	hypoglycemia-associated agents
Drug Categories	immunosuppressive agents
Drug Categories	musculo-skeletal system
Drug Categories	myelosuppressive agents
Drug Categories	nephrotoxic agents
Drug Categories	non cox-2 selective nsaids
Drug Categories	oat1/slc22a6 inhibitors
Drug Categories	oat1/slc22a6 substrates
Drug Categories	oat3/slc22a8 inhibitors
Drug Categories	oat3/slc22a8 substrates
Drug Categories	oatp1b1/slco1b1 inhibitors
Drug Categories	ophthalmologicals
Drug Categories	other nonsteroidal anti-inflammatory agents
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	sensory organs
Drug Categories	topical products for joint and muscular pain
Drug Categories	ugt1a1 substrates
Drug Categories	ugt1a9 substrates
Drug Categories	ugt2b7 inhibitors
Drug Categories	ugt2b7 substrates

(6 More Sources)

Publications:

Higuchi et al., 2004, Indomethacin, but not Helicobacter pylori, inhibits adaptive relaxation in isolated guinea-pig stomach., Drugs Exp Clin Res
Moth et al., 2005, Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1., J. Med. Chem.
Bobadilla L et al., 2005, Effect of pregnancy on the roles of nitric oxide and prostaglandins in 5-hydroxytryptamine-induced contractions in rat isolated thoracic and abdominal aorta., Clin. Exp. Pharmacol. Physiol.
Kundu et al., 2005, Cyclooxygenase inhibitors modulate NK activities that control metastatic disease., Cancer Immunol. Immunother.
Fornai et al., 2005, Role of cyclooxygenases 1 and 2 in the modulation of neuromuscular functions in the distal colon of humans and mice., Gut
Christ AN et al., 2010, Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D(2) synthases., J Med Chem
Hanna MM, 2012, New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies., Eur J Med Chem
Vitale P et al., 2013, Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors., J Med Chem
Blanco et al., 1999, Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes., J. Rheumatol.
Liedtke AJ et al., 2013, Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer., J Med Chem
Lovering et al., 2004, Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin., Cancer Res.
Mathiesen et al., 2005, Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2., Mol. Pharmacol.
Hata et al., 2005, Structural determinants of arylacetic acid nonsteroidal anti-inflammatory drugs necessary for binding and activation of the prostaglandin D2 receptor CRTH2., Mol. Pharmacol.
Hata et al., 2005, Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2., J. Biol. Chem.
Mohagheghpour et al., 1997, Mycobacterium avium reduces expression of costimulatory/adhesion molecules by human monocytes., Cell. Immunol.
Tsukamoto et al., 1989, Effect of glucocorticoid on liver regeneration after partial hepatectomy in the rat., Gut
Fujita et al., 2007, Successful treatment of primary Sjögren's syndrome with chronic natural killer lymphocytosis by high-dose prednisolone and indomethacin farnesil., Intern. Med.
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Xu et al., 2003, Effect of indomethacin on the c-fos expression in AVP and TH neurons in rat brain induced by lipopolysaccharide., Brain Res.
Lehmann et al., 1997, Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs., J. Biol. Chem.
Cho et al., 2003, A simple ELISA for screening ligands of peroxisome proliferator-activated receptor-gamma., J. Biochem. Mol. Biol.
Ashjian et al., 2003, In vitro differentiation of human processed lipoaspirate cells into early neural progenitors., Plast. Reconstr. Surg.
Kocaoğlu et al., 1997, Urinary gamma-glutamyl transferase activity in rats with nonsteroidal anti-inflammatory drug-induced nephrotoxicity., Arch. Immunol. Ther. Exp. (Warsz.)
Zarza J, 2003, Major bleeding during combined treatment with indomethacin and low doses of acenocoumarol in a homozygous patient for 2C9*3 variant of cytochrome p-450 CYP2C9., Thromb Haemost
Stadnyk et al., 2002, Neutrophil migration into indomethacin induced rat small intestinal injury is CD11a/CD18 and CD11b/CD18 co-dependent., Gut
Duncan et al., 2005, Connective tissue growth factor expression in the human corpus luteum: paracrine regulation by human chorionic gonadotropin., J. Clin. Endocrinol. Metab.
Liakos et al., 1997, ANG II AT1 and AT2 receptors both inhibit bFGF-induced proliferation of bovine adrenocortical cells., Am. J. Physiol.
Duric et al., 2006, Effects of analgesic or antidepressant drugs on pain- or stress-evoked hippocampal and spinal neurokinin-1 receptor and brain-derived neurotrophic factor gene expression in the rat., J. Pharmacol. Exp. Ther.
Szabó et al., 2005, Role of transient receptor potential vanilloid 1 receptors in adjuvant-induced chronic arthritis: in vivo study using gene-deficient mice., J. Pharmacol. Exp. Ther.
Ogawa et al., 1985, No role for prostaglandins and bradykinin in the autoregulation of renal blood flow., Jpn. J. Pharmacol.
Pergola C et al., 2014, Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase., J Med Chem
Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med
Armstrong et al., 2005, Suppression of experimental aortic aneurysms: comparison of inducible nitric oxide synthase and cyclooxygenase inhibitors., Ann Vasc Surg
Jerde et al., 2005, Celecoxib inhibits ureteral contractility and prostanoid release., Urology
Zhang et al., 2004, [Proliferation inhibition effect of indomethacin on CML cells associated with down-regulation of phosphorylated STAT1/STAT5 and inhibition of COX-2 expression]., Zhonghua Xue Ye Xue Za Zhi
Yokota et al., 2005, Rofecoxib produces intestinal but not gastric damage in the presence of a low dose of indomethacin in rats., J. Pharmacol. Exp. Ther.
Pilane et al., 2005, Nitric oxide stimulated vascular smooth muscle cells undergo apoptosis induced in part by arachidonic acid derived eicosanoids., J. Cell. Physiol.
Andreis et al., 2000, Adrenomedullin enhances cell proliferation and deoxyribonucleic acid synthesis in rat adrenal zona glomerulosa: receptor subtype involved and signaling mechanism., Endocrinology
Long et al., 1996, Regulation of GLUT4 gene expression by arachidonic acid. Evidence for multiple pathways, one of which requires oxidation to prostaglandin E2., J. Biol. Chem.
Zhu et al., 1999, Differential apoptosis by indomethacin in gastric epithelial cells through the constitutive expression of wild-type p53 and/or up-regulation of c-myc., Biochem. Pharmacol.
Tsutsumi et al., 2004, Endoplasmic reticulum stress response is involved in nonsteroidal anti-inflammatory drug-induced apoptosis., Cell Death Differ.
Koeberle A et al., 2008, Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase., J Med Chem
Aussel et al., 1987, Effect of alpha-fetoprotein and indomethacin on arachidonic acid metabolism in P388D1 macrophages: role of leukotrienes., Prostaglandins Leukot Med
Hull et al., 1997, Healing with basic fibroblast growth factor is associated with reduced indomethacin induced relapse in a human model of gastric ulceration., Gut
Sakoguchi-Okada et al., 2007, Celecoxib inhibits the expression of survivin via the suppression of promoter activity in human colon cancer cells., Biochem. Pharmacol.
Wu et al., 2008, Structural basis for catalytic and inhibitory mechanisms of human prostaglandin reductase PTGR2., Structure
Zhou et al., 2008, Cyclooxygenase inhibition during allergic sensitization increases STAT6-independent primary and memory Th2 responses., J. Immunol.
Sekhar et al., 2002, Redox-sensitive interaction between KIAA0132 and Nrf2 mediates indomethacin-induced expression of gamma-glutamylcysteine synthetase., Free Radic. Biol. Med.
Sato et al., 2007, Polyproline-rod approach to isolating protein targets of bioactive small molecules: isolation of a new target of indomethacin., J. Am. Chem. Soc.
Lee WY et al., 2010, Cytotoxic effects of tanshinones from Salvia miltiorrhiza on doxorubicin-resistant human liver cancer cells., J Nat Prod
Jaramillo et al., 1992, Modulation of immune responses by cyclo-oxygenase inhibitors during intraocular inflammation., Curr. Eye Res.

INDOMETHACIN SLC46A1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

INDOMETHACIN PTGS1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:

Higuchi et al., 2004, Indomethacin, but not Helicobacter pylori, inhibits adaptive relaxation in isolated guinea-pig stomach., Drugs Exp Clin Res

Moth et al., 2005, Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1., J. Med. Chem.

Bobadilla L et al., 2005, Effect of pregnancy on the roles of nitric oxide and prostaglandins in 5-hydroxytryptamine-induced contractions in rat isolated thoracic and abdominal aorta., Clin. Exp. Pharmacol. Physiol.

INDOMETHACIN AKR1C3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Liedtke AJ et al., 2013, Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer., J Med Chem

Lovering et al., 2004, Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin., Cancer Res.

INDOMETHACIN PTGDR2

Interaction Types & Directionality:

agonist (activating)

other/unknown

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Publications:

Mathiesen et al., 2005, Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2., Mol. Pharmacol.

Hata et al., 2005, Structural determinants of arylacetic acid nonsteroidal anti-inflammatory drugs necessary for binding and activation of the prostaglandin D2 receptor CRTH2., Mol. Pharmacol.

Hata et al., 2005, Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2., J. Biol. Chem.

INDOMETHACIN PPARG

Interaction Types & Directionality:

agonist (activating)

activator (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

Publications:

Lehmann et al., 1997, Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs., J. Biol. Chem.

Cho et al., 2003, A simple ELISA for screening ligands of peroxisome proliferator-activated receptor-gamma., J. Biochem. Mol. Biol.

INDOMETHACIN PTGS2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Specific Action of the Ligand Inhibition

Publications:

Christ AN et al., 2010, Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D(2) synthases., J Med Chem

Hanna MM, 2012, New pyrimido[5,4-e]pyrrolo[1,2-c]pyrimidines: synthesis, 2D-QSAR, anti-inflammatory, analgesic and ulcerogenicity studies., Eur J Med Chem

Pergola C et al., 2014, Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase., J Med Chem

INDOMETHACIN PTGR2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Wu et al., 2008, Structural basis for catalytic and inhibitory mechanisms of human prostaglandin reductase PTGR2., Structure
INDOMETHACIN GLO1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Sato et al., 2007, Polyproline-rod approach to isolating protein targets of bioactive small molecules: isolation of a new target of indomethacin., J. Am. Chem. Soc.
INDOMETHACIN PPARA

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Publications:

Lehmann et al., 1997, Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs., J. Biol. Chem.
INDOMETHACIN PLA2G2A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
INDOMETHACIN KCNE1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Indaflex

Novel drug target Established target

Publications:
INDOMETHACIN KCNQ1

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Indaflex

Publications:
INDOMETHACIN CD86

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Mohagheghpour et al., 1997, Mycobacterium avium reduces expression of costimulatory/adhesion molecules by human monocytes., Cell. Immunol.
INDOMETHACIN TYMS

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Tsukamoto et al., 1989, Effect of glucocorticoid on liver regeneration after partial hepatectomy in the rat., Gut
INDOMETHACIN FCGR3A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Fujita et al., 2007, Successful treatment of primary Sjögren's syndrome with chronic natural killer lymphocytosis by high-dose prednisolone and indomethacin farnesil., Intern. Med.
INDOMETHACIN CYP2D6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
INDOMETHACIN CYP3A4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
INDOMETHACIN CYP2C19

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
INDOMETHACIN TH

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Xu et al., 2003, Effect of indomethacin on the c-fos expression in AVP and TH neurons in rat brain induced by lipopolysaccharide., Brain Res.
INDOMETHACIN ENO2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ashjian et al., 2003, In vitro differentiation of human processed lipoaspirate cells into early neural progenitors., Plast. Reconstr. Surg.
INDOMETHACIN GGT1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Kocaoğlu et al., 1997, Urinary gamma-glutamyl transferase activity in rats with nonsteroidal anti-inflammatory drug-induced nephrotoxicity., Arch. Immunol. Ther. Exp. (Warsz.)

INDOMETHACIN CYP2C9

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Zarza J, 2003, Major bleeding during combined treatment with indomethacin and low doses of acenocoumarol in a homozygous patient for 2C9*3 variant of cytochrome p-450 CYP2C9., Thromb Haemost

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

INDOMETHACIN ITGB2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Stadnyk et al., 2002, Neutrophil migration into indomethacin induced rat small intestinal injury is CD11a/CD18 and CD11b/CD18 co-dependent., Gut
INDOMETHACIN FST

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Duncan et al., 2005, Connective tissue growth factor expression in the human corpus luteum: paracrine regulation by human chorionic gonadotropin., J. Clin. Endocrinol. Metab.
INDOMETHACIN AGTR1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Liakos et al., 1997, ANG II AT1 and AT2 receptors both inhibit bFGF-induced proliferation of bovine adrenocortical cells., Am. J. Physiol.

INDOMETHACIN BDNF

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Duric et al., 2006, Effects of analgesic or antidepressant drugs on pain- or stress-evoked hippocampal and spinal neurokinin-1 receptor and brain-derived neurotrophic factor gene expression in the rat., J. Pharmacol. Exp. Ther.

INDOMETHACIN TRPV1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Szabó et al., 2005, Role of transient receptor potential vanilloid 1 receptors in adjuvant-induced chronic arthritis: in vivo study using gene-deficient mice., J. Pharmacol. Exp. Ther.
INDOMETHACIN ACE

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ogawa et al., 1985, No role for prostaglandins and bradykinin in the autoregulation of renal blood flow., Jpn. J. Pharmacol.

INDOMETHACIN ADM

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Andreis et al., 2000, Adrenomedullin enhances cell proliferation and deoxyribonucleic acid synthesis in rat adrenal zona glomerulosa: receptor subtype involved and signaling mechanism., Endocrinology

INDOMETHACIN SLC2A4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Long et al., 1996, Regulation of GLUT4 gene expression by arachidonic acid. Evidence for multiple pathways, one of which requires oxidation to prostaglandin E2., J. Biol. Chem.
INDOMETHACIN MYC

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Zhu et al., 1999, Differential apoptosis by indomethacin in gastric epithelial cells through the constitutive expression of wild-type p53 and/or up-regulation of c-myc., Biochem. Pharmacol.
INDOMETHACIN DDIT3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Tsutsumi et al., 2004, Endoplasmic reticulum stress response is involved in nonsteroidal anti-inflammatory drug-induced apoptosis., Cell Death Differ.
INDOMETHACIN FCGR3B

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Fujita et al., 2007, Successful treatment of primary Sjögren's syndrome with chronic natural killer lymphocytosis by high-dose prednisolone and indomethacin farnesil., Intern. Med.
INDOMETHACIN PTGES

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Koeberle A et al., 2008, Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase., J Med Chem
INDOMETHACIN AFP

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Aussel et al., 1987, Effect of alpha-fetoprotein and indomethacin on arachidonic acid metabolism in P388D1 macrophages: role of leukotrienes., Prostaglandins Leukot Med
INDOMETHACIN FGF2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Hull et al., 1997, Healing with basic fibroblast growth factor is associated with reduced indomethacin induced relapse in a human model of gastric ulceration., Gut
INDOMETHACIN BIRC5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakoguchi-Okada et al., 2007, Celecoxib inhibits the expression of survivin via the suppression of promoter activity in human colon cancer cells., Biochem. Pharmacol.
INDOMETHACIN STAT6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Zhou et al., 2008, Cyclooxygenase inhibition during allergic sensitization increases STAT6-independent primary and memory Th2 responses., J. Immunol.
INDOMETHACIN NFE2L2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sekhar et al., 2002, Redox-sensitive interaction between KIAA0132 and Nrf2 mediates indomethacin-induced expression of gamma-glutamylcysteine synthetase., Free Radic. Biol. Med.
INDOMETHACIN ABCC1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Lee WY et al., 2010, Cytotoxic effects of tanshinones from Salvia miltiorrhiza on doxorubicin-resistant human liver cancer cells., J Nat Prod
INDOMETHACIN SAG

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Jaramillo et al., 1992, Modulation of immune responses by cyclo-oxygenase inhibitors during intraocular inflammation., Curr. Eye Res.
INDOMETHACIN CYP1A2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

DrugBank: DB00328

Version: 5.1.7

Alternate Names:

INDOMETHACIN DrugBank Drug Name

53-86-1 CAS Number

Aconip Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Bobadilla L et al., 2005, Effect of pregnancy on the roles of nitric oxide and prostaglandins in 5-hydroxytryptamine-induced contractions in rat isolated thoracic and abdominal aorta., Clin. Exp. Pharmacol. Physiol.

Higuchi et al., 2004, Indomethacin, but not Helicobacter pylori, inhibits adaptive relaxation in isolated guinea-pig stomach., Drugs Exp Clin Res

Blanco et al., 1999, Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes., J. Rheumatol.

TEND: INDOMETHACIN
- Version: 01-August-2011
Alternate Names:

INDOMETHACIN Primary Drug Name

Drug Info:

Drug Class anti-inflammatory agents, non-steroidal

Year of Approval approved before 1982

Publications:
TdgClinicalTrial: INDOMETHACIN
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications NSAID

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: INDOMETHACIN

Version: 14-September-2017

Alternate Names:

C576 NCI drug code

Drug Info:

Publications:

Ashjian et al., 2003, In vitro differentiation of human processed lipoaspirate cells into early neural progenitors., Plast. Reconstr. Surg.

Kocaoğlu et al., 1997, Urinary gamma-glutamyl transferase activity in rats with nonsteroidal anti-inflammatory drug-induced nephrotoxicity., Arch. Immunol. Ther. Exp. (Warsz.)

Ogawa et al., 1985, No role for prostaglandins and bradykinin in the autoregulation of renal blood flow., Jpn. J. Pharmacol.

DTC: INDOMETHACIN

Version: 02-September-2020

Alternate Names:

CHEMBL6 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

Liedtke AJ et al., 2013, Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer., J Med Chem

Vitale P et al., 2013, Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors., J Med Chem

PharmGKB: indomethacin

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Zarza J, 2003, Major bleeding during combined treatment with indomethacin and low doses of acenocoumarol in a homozygous patient for 2C9*3 variant of cytochrome p-450 CYP2C9., Thromb Haemost

Grosser T, 2009, Variability in the response to cyclooxygenase inhibitors: toward the individualization of nonsteroidal anti-inflammatory drug therapy., J Investig Med

TTD: Indomethacin
- Version: 2020.06.01
Alternate Names:

D0R1RS TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 135650390
- Version: 29-September-2020
Alternate Names:

INDOMETHACIN GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL6
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL6
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Mechanism of Interaction	Cyclooxygenase inhibitor
Direct Interaction	yes
Specific Action of the Ligand	Inhibition

INDOMETHACIN	DrugBank Drug Name
53-86-1	CAS Number
Aconip	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

Trial Name	Indaflex
Novel drug target	Established target

Novel drug target	Established target
Trial Name	Indaflex

INDOMETHACIN Drug Record

INDOMETHACIN chembl:CHEMBL6 ApprovedImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cyclooxygenase inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: agonist (activating) other/unknown

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Full agonist

Interaction Types & Directionality: agonist (activating) activator (activating)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Partial agonist

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cyclooxygenase inhibitor Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Wu et al., 2008, Structural basis for catalytic and inhibitory mechanisms of human prostaglandin reductase PTGR2., Structure

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications: Sato et al., 2007, Polyproline-rod approach to isolating protein targets of bioactive small molecules: isolation of a new target of indomethacin., J. Am. Chem. Soc.

Interaction Types & Directionality: agonist (activating)

Interaction Info:

Publications: Lehmann et al., 1997, Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs., J. Biol. Chem.

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Trial Name Indaflex Novel drug target Established target

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name Indaflex

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Mohagheghpour et al., 1997, Mycobacterium avium reduces expression of costimulatory/adhesion molecules by human monocytes., Cell. Immunol.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Tsukamoto et al., 1989, Effect of glucocorticoid on liver regeneration after partial hepatectomy in the rat., Gut

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Fujita et al., 2007, Successful treatment of primary Sjögren's syndrome with chronic natural killer lymphocytosis by high-dose prednisolone and indomethacin farnesil., Intern. Med.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Xu et al., 2003, Effect of indomethacin on the c-fos expression in AVP and TH neurons in rat brain induced by lipopolysaccharide., Brain Res.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Ashjian et al., 2003, In vitro differentiation of human processed lipoaspirate cells into early neural progenitors., Plast. Reconstr. Surg.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Kocaoğlu et al., 1997, Urinary gamma-glutamyl transferase activity in rats with nonsteroidal anti-inflammatory drug-induced nephrotoxicity., Arch. Immunol. Ther. Exp. (Warsz.)

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Stadnyk et al., 2002, Neutrophil migration into indomethacin induced rat small intestinal injury is CD11a/CD18 and CD11b/CD18 co-dependent., Gut

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Duncan et al., 2005, Connective tissue growth factor expression in the human corpus luteum: paracrine regulation by human chorionic gonadotropin., J. Clin. Endocrinol. Metab.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Liakos et al., 1997, ANG II AT1 and AT2 receptors both inhibit bFGF-induced proliferation of bovine adrenocortical cells., Am. J. Physiol.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Duric et al., 2006, Effects of analgesic or antidepressant drugs on pain- or stress-evoked hippocampal and spinal neurokinin-1 receptor and brain-derived neurotrophic factor gene expression in the rat., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Szabó et al., 2005, Role of transient receptor potential vanilloid 1 receptors in adjuvant-induced chronic arthritis: in vivo study using gene-deficient mice., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cyclooxygenase inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

agonist (activating)

other/unknown

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Interaction Types & Directionality:

agonist (activating)

activator (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cyclooxygenase inhibitor

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Wu et al., 2008, Structural basis for catalytic and inhibitory mechanisms of human prostaglandin reductase PTGR2., Structure

Interaction Types & Directionality:

inhibitor (inhibitory)

Publications:

Sato et al., 2007, Polyproline-rod approach to isolating protein targets of bioactive small molecules: isolation of a new target of indomethacin., J. Am. Chem. Soc.

Interaction Types & Directionality:

agonist (activating)

Publications:

Lehmann et al., 1997, Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs., J. Biol. Chem.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Indaflex

Novel drug target Established target

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Indaflex

Interaction Types & Directionality:

n/a

Publications:

Mohagheghpour et al., 1997, Mycobacterium avium reduces expression of costimulatory/adhesion molecules by human monocytes., Cell. Immunol.

Interaction Types & Directionality:

n/a

Publications:

Tsukamoto et al., 1989, Effect of glucocorticoid on liver regeneration after partial hepatectomy in the rat., Gut

Interaction Types & Directionality:

n/a

Publications:

Fujita et al., 2007, Successful treatment of primary Sjögren's syndrome with chronic natural killer lymphocytosis by high-dose prednisolone and indomethacin farnesil., Intern. Med.

Interaction Types & Directionality:

n/a

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Interaction Types & Directionality:

n/a

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Interaction Types & Directionality:

n/a

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Interaction Types & Directionality:

n/a

Publications:

Xu et al., 2003, Effect of indomethacin on the c-fos expression in AVP and TH neurons in rat brain induced by lipopolysaccharide., Brain Res.

Interaction Types & Directionality:

n/a

Publications:

Ashjian et al., 2003, In vitro differentiation of human processed lipoaspirate cells into early neural progenitors., Plast. Reconstr. Surg.

Interaction Types & Directionality:

n/a

Publications:

Kocaoğlu et al., 1997, Urinary gamma-glutamyl transferase activity in rats with nonsteroidal anti-inflammatory drug-induced nephrotoxicity., Arch. Immunol. Ther. Exp. (Warsz.)

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Publications:

Stadnyk et al., 2002, Neutrophil migration into indomethacin induced rat small intestinal injury is CD11a/CD18 and CD11b/CD18 co-dependent., Gut

Interaction Types & Directionality:

n/a

Publications:

Duncan et al., 2005, Connective tissue growth factor expression in the human corpus luteum: paracrine regulation by human chorionic gonadotropin., J. Clin. Endocrinol. Metab.

Interaction Types & Directionality:

n/a

Publications:

Liakos et al., 1997, ANG II AT1 and AT2 receptors both inhibit bFGF-induced proliferation of bovine adrenocortical cells., Am. J. Physiol.

Interaction Types & Directionality:

n/a

Publications:

Duric et al., 2006, Effects of analgesic or antidepressant drugs on pain- or stress-evoked hippocampal and spinal neurokinin-1 receptor and brain-derived neurotrophic factor gene expression in the rat., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality:

n/a

Publications:

Szabó et al., 2005, Role of transient receptor potential vanilloid 1 receptors in adjuvant-induced chronic arthritis: in vivo study using gene-deficient mice., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality:

n/a

Publications:

Ogawa et al., 1985, No role for prostaglandins and bradykinin in the autoregulation of renal blood flow., Jpn. J. Pharmacol.

Interaction Types & Directionality:

n/a

Publications:

Andreis et al., 2000, Adrenomedullin enhances cell proliferation and deoxyribonucleic acid synthesis in rat adrenal zona glomerulosa: receptor subtype involved and signaling mechanism., Endocrinology

Interaction Types & Directionality:

n/a

Publications:

Long et al., 1996, Regulation of GLUT4 gene expression by arachidonic acid. Evidence for multiple pathways, one of which requires oxidation to prostaglandin E2., J. Biol. Chem.

Interaction Types & Directionality:

n/a

Publications:

Zhu et al., 1999, Differential apoptosis by indomethacin in gastric epithelial cells through the constitutive expression of wild-type p53 and/or up-regulation of c-myc., Biochem. Pharmacol.

Interaction Types & Directionality:

n/a

Publications:

Tsutsumi et al., 2004, Endoplasmic reticulum stress response is involved in nonsteroidal anti-inflammatory drug-induced apoptosis., Cell Death Differ.

Interaction Types & Directionality:

n/a

Publications:

Fujita et al., 2007, Successful treatment of primary Sjögren's syndrome with chronic natural killer lymphocytosis by high-dose prednisolone and indomethacin farnesil., Intern. Med.

Interaction Types & Directionality:

n/a

Publications:

Koeberle A et al., 2008, Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase., J Med Chem

Interaction Types & Directionality:

n/a

Publications:

Aussel et al., 1987, Effect of alpha-fetoprotein and indomethacin on arachidonic acid metabolism in P388D1 macrophages: role of leukotrienes., Prostaglandins Leukot Med

Interaction Types & Directionality:

n/a

Publications:

Hull et al., 1997, Healing with basic fibroblast growth factor is associated with reduced indomethacin induced relapse in a human model of gastric ulceration., Gut