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Atlas / Drug / Indomethacin

Indomethacin

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Also known as AconipArtracinArtracin srBerlind 75 retDurametacinFlexin-25 continusFlexin-50 continusFlexin-75 continusImbrilonIndo-lemmonIndo-paedIndocid retIndocid-rIndocinIndocin srIndodermIndoflexIndolarIndolar srIndomax-25

Summary

Indomethacin (CHEMBL6) is an approved small-molecule non-steroidal anti-inflammatory drug (ATC C01EB03) targeting SLC46A1, PTGS1, and PTGS2; indicated across 35 conditions including ankylosing spondylitis and eye disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C01EB03 (+4 more)
  • Targets: 5 (SLC46A1, PTGS1, PTGS2…)
  • Indications: 35 conditions
  • Clinical trials: 124
  • Chemistry: 357.8 Da · C19H16ClNO4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL6
NameIndomethacin
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3715
ChEBICHEBI:49662
ATCC01EB03, M02AA23, M01AB51, S01BC01, M01AB01
Molecular formulaC19H16ClNO4
Molecular weight357.8
InChIKeyCGIGDMFJXJATDK-UHFFFAOYSA-N

SMILES: CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)O

IUPAC name: 2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetic acid

ChEBI definition: A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.

Pharmacological roles (ChEBI): non-steroidal anti-inflammatory drug, EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor, analgesic, gout suppressant.

Other ChEBI roles (chemical / environmental): drug metabolite, xenobiotic metabolite, xenobiotic, environmental contaminant.

Also known as: Aconip, Artracin, Artracin sr, Berlind 75 ret, Durametacin, Flexin-25 continus, Flexin-50 continus, Flexin-75 continus, Imbrilon, Indo-lemmon, Indo-paed, Indocid ret

Parent form; salt/anhydrous children: CHEMBL2028292, CHEMBL3989410, CHEMBL4590319

Patent coverage: 45,829 distinct patent families (156,366 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 155,846 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
SLC46A1Proton-coupled folate transporterInhibition3.72.7%Q96NT5
PTGS1COX-1Inhibition6.590%P23219
PTGS2COX-2Inhibition5.580%P35354
PTGDR2DP2 receptorFull agonist7.70%Q9Y5Y4
PPARGPeroxisome proliferator-activated receptor-γPartial agonist7.382.6%P37231

Broader ChEMBL bioactivity targets: 69 (assay-derived). Sample: Uracil nucleotide/cysteinyl leukotriene receptor, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Fructose-bisphosphate aldolase, Prelamin-A/C, Ras-related protein Rab-9A, Peripheral myelin protein 22, Solute carrier family 22 member 6, Organic anion transporter 3.

Bioactivity

ChEMBL activities: 385 potent at pChembl ≥ 5 of 462 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
AR9.85EC500.14nMCHEMBL_ACT_12651619
PTGS19.85IC500.14nMCHEMBL_ACT_25553877
PTGS29.85IC500.14nMCHEMBL_ACT_25553879
NAPRT9.82Ki0.15nMCHEMBL_ACT_19323251
PTGS18.7IC502nMCHEMBL_ACT_132512
P224378.7IC502nMCHEMBL_ACT_1507837
P353558.54IC502.9nMCHEMBL_ACT_781727
PTGS18.52IC503nMCHEMBL_ACT_84677
PTGS18.52IC503nMCHEMBL_ACT_874568
P059798.4IC504nMCHEMBL_ACT_1759941
O626648.39IC504.1nMCHEMBL_ACT_10961892
PTGS18.3IC505nMCHEMBL_ACT_1759893
PTGS28.23IC505.9nMCHEMBL_ACT_84676
PTGS18.22IC506nMCHEMBL_ACT_2069733
P059798.22IC506nMCHEMBL_ACT_3369555
Q639218.22IC506nMCHEMBL_ACT_390935
P059798.22IC506nMCHEMBL_ACT_6337366
Q639218.22IC506nMCHEMBL_ACT_719250
Q057698.19IC506.4nMCHEMBL_ACT_403143
Q057698.19IC506.4nMCHEMBL_ACT_730232
P059798.17IC506.7nMCHEMBL_ACT_12072252
PTGS18.09IC508.2nMCHEMBL_ACT_403144
PTGS18.09IC508.2nMCHEMBL_ACT_730233
PTGS28.05IC509nMCHEMBL_ACT_132513
Q057698.05IC509nMCHEMBL_ACT_1507838
PTGS28.05IC509nMCHEMBL_ACT_874569
P059798IC5010nMCHEMBL_ACT_12098193
PTGS28IC5010nMCHEMBL_ACT_2069734
PTGS18IC5010nMCHEMBL_ACT_2323375
PTGS28IC5010nMCHEMBL_ACT_3369762

Target pathways

Aggregated over 5 target gene(s): SLC46A1, PTGS1, PTGS2, PTGDR2, PPARG.

Top Reactome pathways

22 total, by targets touching each:

PathwayTargetsGenes
Synthesis of Prostaglandins (PG) and Thromboxanes (TX)2PTGS1, PTGS2
COX reactions1PTGS1
Metabolism of folate and pterines1SLC46A1
PPARA activates gene expression1PPARG
Synthesis of 15-eicosatetraenoic acid derivatives1PTGS2
Transcriptional regulation of white adipocyte differentiation1PPARG
Nuclear Receptor transcription pathway1PPARG
Prostanoid ligand receptors1PTGDR2
SUMOylation of intracellular receptors1PPARG
G alpha (i) signalling events1PTGDR2
Interleukin-10 signaling1PTGS2
Interleukin-4 and Interleukin-13 signaling1PTGS2
Regulation of PTEN gene transcription1PPARG
Biosynthesis of DHA-derived SPMs1PTGS2
Biosynthesis of EPA-derived SPMs1PTGS2
MECP2 regulates transcription factors1PPARG
Biosynthesis of DPAn-3 SPMs1PTGS2
Biosynthesis of electrophilic ω-3 PUFA oxo-derivatives1PTGS2
Iron uptake and transport1SLC46A1
Heme signaling1SLC46A1
MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis1PPARG
Transcriptional regulation of brown and beige adipocyte differentiation by EBF21PPARG

Dominant GO biological processes

GO termTargets
regulation of blood pressure3
fatty acid metabolic process3
prostaglandin biosynthetic process2
response to oxidative stress2
cyclooxygenase pathway2
regulation of cell population proliferation2
long-chain fatty acid biosynthetic process2
lipid metabolic process2
fatty acid biosynthetic process2
prostaglandin metabolic process2
prostanoid biosynthetic process2
cellular oxidant detoxification2
brown fat cell differentiation2
cellular response to hypoxia2
G protein-coupled receptor signaling pathway2

Indications & clinical

Indications

35 indications (12 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
ankylosing spondylitis4MONDO:0005306EFO:0003898
eye disorder4MONDO:0005328EFO:0005752
cardiovascular disorder4MONDO:0004995EFO:0000319
rheumatic disorder4MONDO:0005554EFO:0005755
gout4MONDO:0005393EFO:0004274
patent ductus arteriosus4MONDO:0011827HP:0001643
rheumatoid arthritis4MONDO:0008383EFO:0000685
spondylitis4MONDO:0003937MONDO:0003937
osteoarthritis4MONDO:0005178MONDO:0005178
pancreatitis3MONDO:0004982EFO:0000278
acute pancreatitis3MONDO:0006515EFO:1000652
oral cavity squamous cell carcinoma3MONDO:0004958EFO:0000199
severe acute respiratory syndrome3MONDO:0005091MONDO:0100096
Alzheimer disease3MONDO:0004975MONDO:0004975
head and neck squamous cell carcinoma2MONDO:0010150EFO:0000181
metastatic prostate carcinoma2MONDO:0004956EFO:0000196
cutaneous melanoma2MONDO:0005012EFO:0000389
Langerhans cell histiocytosis2MONDO:0018310EFO:1000318
prostate adenocarcinoma2MONDO:0005082EFO:0000673
orthostatic hypotension1MONDO:0005469EFO:0005252
chronic pancreatitis1MONDO:0005003EFO:0000342
breast neoplasm1MONDO:0021100MONDO:0007254
asthma1MONDO:0004979MONDO:0004979
ulcerative colitis1MONDO:0005101EFO:0000729

11 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 124.

Phase distribution

PhaseTrials
Not specified29
PHASE425
PHASE325
PHASE214
PHASE111
PHASE1/PHASE210
EARLY_PHASE17
PHASE2/PHASE33

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06433453PHASE4RECRUITINGThree Dimensional Ultrasonographic Detection of Human Ovulation
NCT00116623PHASE4TERMINATEDMagnesium Sulfate Versus Indomethacin for Preterm Labor
NCT00226122PHASE4COMPLETEDThe Effect of Indomethacin in Monosymptomatic Enuresis Nocturnal
NCT00462111PHASE4COMPLETEDIndomethacin and Mechanisms Underlying Risk of Falling
NCT00470743PHASE4WITHDRAWNComparing Ibuprofen And Indomethacin For The Treatment Of The Patent Ductus Arteriosus in Very Premature Babies
NCT00473980PHASE4COMPLETEDPreoperative Non-steroidal Anti-inflammatory Drugs(NSAID) to Colorectal Cancer Patients
NCT00820612PHASE4TERMINATEDRectal Indomethacin in the Prevention of Post-endoscopic Retrograde Cholangiopancreatography (ERCP) Pancreatitis in High Risk Patients
NCT01073670PHASE4COMPLETEDIndomethacin and Cardiac Bypass Surgery
NCT01830335PHASE4COMPLETEDCerebral Blood Flow and PETCO2 on Neuromuscular Function During Environmental Stress
NCT01848665PHASE4COMPLETEDThe Influence of Cerebral Blood Flow and PETCO2 on Neuromuscular Function During Passive Heat Stress
NCT01957215PHASE4COMPLETEDEfficacy of Topical Indomethacin Patch Over Placebo in Ankle Sprain Pain Relief
NCT02183155PHASE4COMPLETEDEffect of Meloxicam Tablets on Bleeding Time in Healthy Subjects
NCT02438371PHASE4TERMINATEDNifedipine or Nifedipine Plus Indomethacin for Treatment of Acute Preterm Labor
NCT02577809PHASE4COMPLETEDIntrathecal Opioid Study
NCT02711358PHASE4COMPLETEDIndomethacin Use in Pain Relief During Intrauterine Device Insertion
NCT02770950PHASE4COMPLETEDZushima Plaster for Treating Knee Osteoarthritis
NCT02797067PHASE4COMPLETEDRectal Indomethacin to Prevent Post ESWL-pancreatitis
NCT02947932PHASE4UNKNOWNOral Resveratrol to Prevent Post-ERCP Pancreatitis
NCT02964403PHASE4UNKNOWNCOX-2 Inhibitor to Prevent Post-ERCP Pancreatitis
NCT03261635PHASE4COMPLETEDRanibizumab Plus Indomethacin
NCT03473665PHASE4TERMINATEDNon-Steroidal Anti-inflammatory Drugs in Axial Spondyloarthritis
NCT03708458PHASE4UNKNOWNPharmacological Prophylaxis of Post- Endoscopic Retrograde Cholangiopancreatography (ERCP) Pancreatitis
NCT05132829PHASE4UNKNOWNAzithromycin to Improve Latency in Exam Indicated Cerclage Control Trial
NCT05664074PHASE4COMPLETEDRectal Indomethacin vs Intravenous Ketorolac
NCT06253702PHASE4COMPLETEDBrain Blood Flow Responses to Stress: Sex Differences
NCT02205762PHASE2/PHASE3ACTIVE_NOT_RECRUITINGLCH-IV, International Collaborative Treatment Protocol for Children and Adolescents With Langerhans Cell Histiocytosis
NCT03713879PHASE3RECRUITINGComparative Effectiveness Between Indomethacin and Pancreatic Stenting in the Prevention of Post ERCP Pancreatitis
NCT05252754PHASE3RECRUITINGRectal Indomethacin and Oral Tacrolimus Versus Combination to Prevent Post-ERCP Pancreatitis
NCT00000494PHASE3COMPLETEDManagement of Patent Ductus in Premature Infants
NCT00009646PHASE3COMPLETEDTrial of Indomethacin Prophylaxis in Preterm Infants (TIPP)
NCT00033917PHASE3COMPLETEDIndomethacin Germinal Matrix Hemorrhage/Intraventricular Hemorrhage (GMH/IVH) Prevention Trial
NCT00432081PHASE3COMPLETEDEffect of Indomethacin on the Progression of Alzheimer’s Disease
NCT00485160PHASE3COMPLETEDIbuprofen vs. Continuous Indomethacin in the Treatment of PDA
NCT00549549PHASE3COMPLETEDCelebrex In Acute Gouty Arthritis Study
NCT00750581PHASE2/PHASE3TERMINATEDAn Escalating Dose Indomethacin for the Treatment of Persistent Patent Ductus Arteriosus (PDA) In Preterm Infants
NCT00855920PHASE3COMPLETEDStudy Utilizing Rilonacept in Gout Exacerbations
NCT01265849PHASE3COMPLETEDEfficacy and Safety Study of Leukocyte Interleukin,Injection (LI) to Treat Cancer of the Oral Cavity
NCT01360034PHASE3UNKNOWNNifedipine Versus Indomethacin in the Treatment of Preterm Labour
NCT01543685PHASE3COMPLETEDStudy of Indomethacin Capsules to Treat Pain Following Bunionectomy
NCT01626118PHASE3COMPLETEDStudy of Indomethacin Capsules to Treat Pain Following Bunionectomy

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

GuidelineSourceGene(s)DosingRecommendation
Annotation of CPIC Guideline for aceclofenac, aspirin, diclofenac, dipCPICCYP2C9

PharmGKB also curates 2 clinical and 13 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

483 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
LUMIRACOXIBChEMBLPhase 4 (approved)PPARG, PTGS1, PTGS2
TROGLITAZONEChEMBLPhase 4 (approved)PPARG, PTGS1, PTGS2
RESVERATROLChEMBLPhase 3PPARG, PTGS1, PTGS2
FulvestrantChEMBL + PubChemPhase 4 (approved)PPARG, PTGS2
3,3’,4’,5-TETRACHLOROSALICYLANILIDEChEMBLPhase 4 (approved)PTGS1, PTGS2
ACEMETACINChEMBLPhase 4 (approved)PTGS1, PTGS2
ASPIRINChEMBLPhase 4 (approved)PTGS1, PTGS2
BROMFENACChEMBLPhase 4 (approved)PTGS1, PTGS2
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)PPARG, PTGS2
CANNABIDIOLChEMBLPhase 4 (approved)PPARG, PTGS2
CAPSAICINChEMBLPhase 4 (approved)PTGS1, PTGS2
CAPTOPRILChEMBLPhase 4 (approved)PTGS1, PTGS2
CARPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
CELECOXIBChEMBLPhase 4 (approved)PTGS1, PTGS2
CIANIDANOLChEMBLPhase 4 (approved)PTGS1, PTGS2
DEXIBUPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
DEXKETOPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
DICLOFENACChEMBLPhase 4 (approved)PTGS1, PTGS2
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)PTGS1, PTGS2
DOXORUBICINChEMBLPhase 4 (approved)PTGS1, PTGS2
ESFLURBIPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
ETODOLACChEMBLPhase 4 (approved)PTGS1, PTGS2
ETORICOXIBChEMBLPhase 4 (approved)PTGS1, PTGS2
FLURBIPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
GLAFENINEChEMBLPhase 4 (approved)PTGS1, PTGS2
HEXACHLOROPHENEChEMBLPhase 4 (approved)PTGS1, PTGS2
IBUPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
KETOPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
KETOROLACChEMBLPhase 4 (approved)PTGS1, PTGS2
LASOFOXIFENEChEMBLPhase 4 (approved)PPARG, PTGS2
LEVODOPAChEMBLPhase 4 (approved)PTGS1, PTGS2
LEVOTHYROXINEChEMBLPhase 4 (approved)PPARG, PTGS2
LOXOPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
MASOPROCOLChEMBLPhase 4 (approved)PPARG, PTGS2
MECLOFENAMIC ACIDChEMBLPhase 4 (approved)PTGS1, PTGS2
MEFENAMIC ACIDChEMBLPhase 4 (approved)PTGS1, PTGS2
MELOXICAMChEMBLPhase 4 (approved)PTGS1, PTGS2
MOFEZOLACChEMBLPhase 4 (approved)PTGS1, PTGS2
MONOBENZONEChEMBLPhase 4 (approved)PTGS1, PTGS2
NAPROXENChEMBLPhase 4 (approved)PTGS1, PTGS2
NIMESULIDEChEMBLPhase 4 (approved)PTGS1, PTGS2
OMADACYCLINEChEMBLPhase 4 (approved)PTGS1, PTGS2
OXAPROZINChEMBLPhase 4 (approved)PTGS1, PTGS2
PIROXICAMChEMBLPhase 4 (approved)PTGS1, PTGS2
PRIMAQUINEChEMBLPhase 4 (approved)PTGS1, PTGS2
RANITIDINEChEMBLPhase 4 (approved)PTGS1, PTGS2
ROFECOXIBChEMBLPhase 4 (approved)PTGS1, PTGS2
SELINEXORChEMBLPhase 4 (approved)PTGS1, PTGS2
SULINDACChEMBLPhase 4 (approved)PPARG, PTGS2
SUPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
TEGASERODChEMBLPhase 4 (approved)PTGS1, PTGS2
TELOTRISTATChEMBLPhase 4 (approved)PTGS1, PTGS2
TIPRANAVIRChEMBLPhase 4 (approved)PPARG, PTGS2
TOLMETINChEMBLPhase 4 (approved)PTGS1, PTGS2
VALDECOXIBChEMBLPhase 4 (approved)PTGS1, PTGS2
VORTIOXETINEChEMBLPhase 4 (approved)PTGS1, PTGS2
CURCUMINChEMBLPhase 3PTGS1, PTGS2
GAMOLENIC ACIDChEMBLPhase 3PPARG, PTGS1
ICOSAPENTChEMBLPhase 3PPARG, PTGS1
QUERCETINChEMBLPhase 3PPARG, PTGS2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot