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Ketorolac

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Also known as KetorolacoSID90341692SID174007295

Summary

Ketorolac (CHEMBL469) is an approved small-molecule cyclooxygenase 2 inhibitor (ATC S01BC05) targeting PTGS1 and PTGS2; indicated across 36 conditions including eye disorder and rheumatic disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: S01BC05 (+1 more)
  • Targets: 2 (PTGS1, PTGS2)
  • Indications: 36 conditions
  • Clinical trials: 257
  • Chemistry: 255.27 Da · C15H13NO3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL469
NameKetorolac
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3826
ChEBICHEBI:6129
ATCS01BC05, M01AB15
Molecular formulaC15H13NO3
Molecular weight255.27
InChIKeyOZWKMVRBQXNZKK-UHFFFAOYSA-N

SMILES: C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O

IUPAC name: 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid

ChEBI definition: A racemate comprising equimolar amounts of (R)-(+)- and (S)-(−)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(−) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.

Pharmacological roles (ChEBI): cyclooxygenase 2 inhibitor, cyclooxygenase 1 inhibitor, non-steroidal anti-inflammatory drug, analgesic.

Also known as: Ketorolac, Ketorolaco, ketorolac, SID90341692, KETOROLAC, SID174007295

Parent form; salt/anhydrous children: CHEMBL1201124

Patent coverage: 13,219 distinct patent families (53,920 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
PTGS1COX-1Inhibition4.50%P23219
PTGS2COX-2Inhibition4.220%P35354

Broader ChEMBL bioactivity targets: 12 (assay-derived). Sample: NPC intracellular cholesterol transporter 1, Ras-related protein Rab-9A, Prostaglandin G/H synthase 1, Prostaglandin G/H synthase 2, Mu-type opioid receptor, Muscarinic acetylcholine receptor M3, Aldo-keto reductase family 1 member B1, Prostaglandin G/H synthase 1, Rho GTPase Rac1/CDC42, Prostaglandin-H2 D-isomerase.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 16 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
OPRM18.89AC501.3nMCHEMBL_ACT_25146817
PTGS17.89IC5013nMCHEMBL_ACT_7778229
Q639217.62AC5023.9nMCHEMBL_ACT_25174214
PTGS26.85IC50140nMCHEMBL_ACT_18003608
O091146.64IC50230nMCHEMBL_ACT_361756
PTGS26.37IC50424nMCHEMBL_ACT_7778231
PTGS26.09AC50812.4nMCHEMBL_ACT_25166010
PTGS15.91IC501230nMCHEMBL_ACT_25087784
CDC425.7IC502000nMCHEMBL_ACT_18003617
PTGS25.46IC503500nMCHEMBL_ACT_25087781
RAB9A5.44Potency3663nMCHEMBL_ACT_3853186
P079435.21IC506109nMCHEMBL_ACT_7776208

Target pathways

Aggregated over 2 target gene(s): PTGS1, PTGS2.

Top Reactome pathways

9 total, by targets touching each:

PathwayTargetsGenes
Synthesis of Prostaglandins (PG) and Thromboxanes (TX)2PTGS1, PTGS2
COX reactions1PTGS1
Synthesis of 15-eicosatetraenoic acid derivatives1PTGS2
Interleukin-10 signaling1PTGS2
Interleukin-4 and Interleukin-13 signaling1PTGS2
Biosynthesis of DHA-derived SPMs1PTGS2
Biosynthesis of EPA-derived SPMs1PTGS2
Biosynthesis of DPAn-3 SPMs1PTGS2
Biosynthesis of electrophilic ω-3 PUFA oxo-derivatives1PTGS2

Dominant GO biological processes

GO termTargets
prostaglandin biosynthetic process2
response to oxidative stress2
regulation of blood pressure2
cyclooxygenase pathway2
regulation of cell population proliferation2
long-chain fatty acid biosynthetic process2
lipid metabolic process2
fatty acid metabolic process2
fatty acid biosynthetic process2
prostaglandin metabolic process2
prostanoid biosynthetic process2
cellular oxidant detoxification2
embryo implantation1
response to nematode1
response to selenium ion1

Indications & clinical

Indications

36 indications (2 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
eye disorder4MONDO:0005328EFO:0005752
rheumatic disorder4MONDO:0005554EFO:0005755
breast neoplasm3MONDO:0021100EFO:0003869
injury3MONDO:0021178EFO:0000546
nephrolithiasis3MONDO:0008171EFO:0004253
cataract3MONDO:0005129MONDO:0005129
migraine disorder3MONDO:0005277MONDO:0005277
osteoarthritis3MONDO:0005178MONDO:0005178
heart disorder2MONDO:0005267EFO:0003777
retinopathy of prematurity2MONDO:0006952EFO:1001158
periodontitis2MONDO:0005076EFO:0000649
preeclampsia2MONDO:0005081EFO:0000668
scoliosis2MONDO:0005392EFO:0004273
viral conjunctivitis2MONDO:0043541EFO:0008571
rotator cuff syndrome2MONDO:0007028EFO:1001250
osteoarthritis, knee2MONDO:0005416EFO:0004616
acute pancreatitis2MONDO:0006515EFO:1000652
tonsillitis2MONDO:0001039HP:0011110
musculoskeletal system disorder2MONDO:0002081EFO:0009676
kidney cancer2MONDO:0002367MONDO:0002367
kidney neoplasm2MONDO:0021163EFO:0003865
diabetic retinopathy1MONDO:0005266EFO:0003770
peritoneal neoplasm0MONDO:0006901MONDO:0002087
fallopian tube neoplasm0MONDO:0021092MONDO:0002158
ovarian cancer0MONDO:0008170MONDO:0008170

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

Clinical trials

Total trials: 257.

Phase distribution

PhaseTrials
PHASE4107
Not specified48
PHASE334
PHASE234
PHASE113
PHASE2/PHASE39
EARLY_PHASE18
PHASE1/PHASE24

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04040452PHASE4RECRUITINGContinuous vs Intermittent Ketorolac for Pain Control in Peds CV Surgery
NCT04771156PHASE4RECRUITINGKetorolac in Palatoplasty
NCT05488847PHASE4ACTIVE_NOT_RECRUITINGOpioid-Free Pain Protocol After Shoulder Arthroplasty
NCT05776953PHASE4RECRUITINGEvaluation of the Effects of Ketorolac Dose on Duration of Analgesia in Emergency Department (ED) Renal Colic Patients
NCT05875571PHASE4RECRUITINGIntravenous Ketorolac Administration to Attenuate Post-procedural Pain Associated With Intrauterine Device Placement
NCT06201676PHASE4RECRUITINGLow-Dose Short-Term Ketorolac to Reduce Chronic Opioid Use in Orthopaedic Polytrauma Patients
NCT06484192PHASE4ENROLLING_BY_INVITATIONPain Control After Lumbar Spine Fusion
NCT06498440PHASE4NOT_YET_RECRUITINGEfficacy of NSAID vs. Steroid-NSAID Combo Post-Selective Laser Trabeculoplasty: Phase 4, Single-Center RCT
NCT06579703PHASE4NOT_YET_RECRUITINGKetorolac for Acute Vaso-Occlusive Crisis in Pediatric Sickle Cell Disease
NCT07006168PHASE4RECRUITINGEffects Of Intra-Operative Intra-Articular Cocktail Injection In Patella Open Reduction And Internal Fixation
NCT07037888PHASE4RECRUITINGEfficacy of Ketorolac for Postoperative Pain Management in Hip Arthroscopy: A Prospective Double-Blinded Randomized Controlled Trial
NCT07276906PHASE4NOT_YET_RECRUITINGComparing Intramuscular Fentanyl and Ketorolac With Nerve of Arnold (NOA) Block for Bilateral Myringotomy
NCT07430085PHASE4NOT_YET_RECRUITINGPost-Operative Pain Relief: Zynrelef or Periarticular Injections in RATKA
NCT00115336PHASE4TERMINATEDKetorolac Versus Ibuprofen to Treat Painful Episodes of Sickle Cell Disease
NCT00161577PHASE4COMPLETEDUse of Ketorolac in Management of Post-Operative Pain After Heart Surgery
NCT00330798PHASE4COMPLETEDA Comparison of Topical Nepafenac to Placebo in Corneal Epithelial Healing Times and Postoperative Pain Relief
NCT00347503PHASE4COMPLETEDAqueous Concentrations and PGE2 Inhibition of Ketorolac 0.4% vs. Bromfenac 0.09% in Cataract Patients
NCT00348244PHASE4COMPLETEDKetorolac vs. Steroid in the Prevention of CME
NCT00348582PHASE4COMPLETEDAcular LS vs. Nevanac in Post op Inflammation Following Cataract Surgery
NCT00421967PHASE4TERMINATEDPostoperative Analgesia After Total Knee Arthroplasty
NCT00433225PHASE4COMPLETEDEfficacy of Topical Ketorolac Versus Placebo for Improving Visual Outcomes Following Multifocal IOL Implantation
NCT00520260PHASE4COMPLETEDBromfenac 0.09% vs Ketorolac 0.4% for Cyclosporine Induction Phase
NCT00560443PHASE4COMPLETEDRCT on Ketorolac and Tramadol in Bone Fractures Pain of Child
NCT00562627PHASE4COMPLETEDEfficacy of Multimodal Peri- and Intraarticular Drug Injections in Total Knee Arthroplasty
NCT00595543PHASE4COMPLETEDTreatment of Acute Pseudophakic Cystoid Macular Edema: Bromfenac 0.09% Versus Diclofenac Sodium 0.1% Versus Ketorolac Tromethamine 0.5%
NCT00638508PHASE4COMPLETEDON-Q Pump Infusion of Ketorolac and Ropivacaine at the Wound Site for Postoperative Pain Management
NCT00765128PHASE4COMPLETEDIntravenous Ketorolac for Postoperative Pain in Percutaneous Nephrolithotomy
NCT00765232PHASE4COMPLETEDIntravenous Ketorolac for Postoperative Pain in Laparoscopic Donor Nephrectomy
NCT00785863PHASE4COMPLETEDModulation of Remifentanil-induced Postinfusion Hyperalgesia
NCT00791323PHASE4COMPLETEDEfficacy of Ketorolac 0.4% in Prostaglandin Suppression
NCT00868348PHASE4COMPLETEDA Comparison of Naropin and Ketorolac for Postoperative Analgesia After Total Knee Arthroplasty
NCT00901628PHASE4COMPLETEDPeriarticular Multimodal Drug Injections in Total Knee Arthroplasty
NCT00981435PHASE4COMPLETEDSteroids After Laser Trabeculoplasty for Glaucoma
NCT01011673PHASE4COMPLETEDMetoclopramide Versus Ketorolac for Tension-type Headache
NCT01267864PHASE4COMPLETEDValproate Versus Ketorolac Versus Metoclopramide
NCT01304212PHASE4COMPLETEDEffectiveness of Analgesia in Total Knee Arthroplasty
NCT01344395PHASE4COMPLETEDUse of Local Infiltration Analgesia Following Total Hip Arthroplasty
NCT01345162PHASE4COMPLETEDAssessment and Prevention of Acute Post-herniotomy Pain
NCT01395069PHASE4COMPLETEDProphylactic Nepafenac and Ketorolac Versus Placebo in Patients Undergoing Cataract Surgery
NCT01534806PHASE4WITHDRAWNProchlorperazine Versus Prochlorperazine & Ketorolac in Treatment of Pediatric Migraine in the Emergency Department

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 3 clinical and 8 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.

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

MoleculeSourceStatusShared targets
3,3’,4’,5-TETRACHLOROSALICYLANILIDEChEMBLPhase 4 (approved)PTGS1, PTGS2
ACEMETACINChEMBLPhase 4 (approved)PTGS1, PTGS2
ASPIRINChEMBLPhase 4 (approved)PTGS1, PTGS2
BROMFENACChEMBLPhase 4 (approved)PTGS1, 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
INDOMETHACINChEMBLPhase 4 (approved)PTGS1, PTGS2
KETOPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
LEVODOPAChEMBLPhase 4 (approved)PTGS1, PTGS2
LOXOPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
LUMIRACOXIBChEMBLPhase 4 (approved)PTGS1, 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
SUPROFENChEMBLPhase 4 (approved)PTGS1, PTGS2
TEGASERODChEMBLPhase 4 (approved)PTGS1, PTGS2
TELOTRISTATChEMBLPhase 4 (approved)PTGS1, PTGS2
TOLMETINChEMBLPhase 4 (approved)PTGS1, PTGS2
TROGLITAZONEChEMBLPhase 4 (approved)PTGS1, PTGS2
VALDECOXIBChEMBLPhase 4 (approved)PTGS1, PTGS2
VORTIOXETINEChEMBLPhase 4 (approved)PTGS1, PTGS2
CURCUMINChEMBLPhase 3PTGS1, PTGS2
RESVERATROLChEMBLPhase 3PTGS1, PTGS2
CIMICOXIBChEMBLPhase 2PTGS1, PTGS2
DERACOXIBChEMBLPhase 2PTGS1, PTGS2
ENOFELASTChEMBLPhase 2PTGS1, PTGS2
FIROCOXIBChEMBLPhase 2PTGS1, PTGS2
FLUFENAMIC ACIDChEMBLPhase 2PTGS1, PTGS2
LICOFELONEChEMBLPhase 2PTGS1, PTGS2
MAVACOXIBChEMBLPhase 2PTGS1, PTGS2
MIROPROFENChEMBLPhase 2PTGS1, PTGS2
NIFLUMIC ACIDChEMBLPhase 2PTGS1, PTGS2
PHENOTHIAZINEChEMBLPhase 2PTGS1, PTGS2
PIRMAGRELChEMBLPhase 2PTGS1, 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