Diclofenac

drug
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Also known as ArthrotecDiclofenac acidDiclofenac free acidDiclofenacoLAS-41007Las41007Voltaren ophthalmicVoltaren xrZorvolexZorvolex capsulesdiclorenacSID24424557SID174007221DiclofinacDeclofenacDicofenac

Summary

Diclofenac (CHEMBL139) is an approved small-molecule non-steroidal anti-inflammatory drug (ATC M01AB55) targeting SLC36A1, PTGS1, and PTGS2; indicated across 34 conditions including eye disorder and rheumatoid arthritis.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: M01AB55 (+4 more)
  • Targets: 6 (SLC36A1, PTGS1, PTGS2…)
  • Indications: 34 conditions
  • Clinical trials: 227
  • Chemistry: 296.1 Da · C14H11Cl2NO2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL139
NameDiclofenac
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3033
ChEBICHEBI:47381
ATCM01AB55, S01BC03, D11AX18, M01AB05, M02AA15
Molecular formulaC14H11Cl2NO2
Molecular weight296.1
InChIKeyDCOPUUMXTXDBNB-UHFFFAOYSA-N

SMILES: C1=CC=C(C(=C1)CC(=O)O)NC2=C(C=CC=C2Cl)Cl

IUPAC name: 2-[2-(2,6-dichloroanilino)phenyl]acetic acid

ChEBI definition: A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.

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

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

Also known as: Arthrotec, Diclofenac, Diclofenac acid, Diclofenac free acid, Diclofenaco, LAS-41007, Las41007, LAS41007, Voltaren ophthalmic, Voltaren xr, Zorvolex, Zorvolex capsules

Parent form; salt/anhydrous children: CHEMBL1034, CHEMBL1200804, CHEMBL1201180, CHEMBL3350449

Patent coverage: 36,351 distinct patent families (125,009 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 123,829 (99%) 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
SLC36A1Proton-coupled Amino acid Transporter 1Inhibition3.570.2%Q7Z2H8
PTGS1COX-1Inhibition7.920%P23219
PTGS2COX-2Inhibition7.70%P35354
TRPM3TRPM35.20.1%Q9HCF6
PPARGPeroxisome proliferator-activated receptor-γAntagonist6.22.6%P37231
ASIC3ASIC340%Q9UHC3

Broader ChEMBL bioactivity targets: 29 (assay-derived). Sample: UDP-glucuronosyltransferase 1A1, Solute carrier family 22 member 6, UDP-glucuronosyltransferase 1A6, UDP-glucuronosyltransferase 1A7, UDP-glucuronosyltransferase 1A9, UDP-glucuronosyltransferase 1A10, Bile acid receptor, Cyclooxygenase, Interleukin-8, Prostaglandin G/H synthase 1.

Bioactivity

ChEMBL activities: 85 potent at pChembl ≥ 5 of 105 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PTGS18.52IC503nMCHEMBL_ACT_10908202
O626648.52IC503nMCHEMBL_ACT_2392921
PTGS28.3IC505nMCHEMBL_ACT_10908208
PTGS28.3IC505nMCHEMBL_ACT_1610386
CXCL88.1IC508nMCHEMBL_ACT_2695366
PTGS28IC5010nMCHEMBL_ACT_2392946
PTGS17.92IC5012nMCHEMBL_ACT_2065658
PTGS17.92IC5012nMCHEMBL_ACT_2372341
PTGS17.92IC5012nMCHEMBL_ACT_2390352
CXCR17.92IC5012nMCHEMBL_ACT_2695394
PTGS17.89IC5013nMCHEMBL_ACT_7681233
PTGS17.82IC5015nMCHEMBL_ACT_2573359
PTGS27.7IC5020nMCHEMBL_ACT_13862298
PTGS27.7IC5020nMCHEMBL_ACT_16596068
PTGS27.7IC5020nMCHEMBL_ACT_20631474
PTGS27.7IC5020nMCHEMBL_ACT_2069744
PTGS27.7IC5020nMCHEMBL_ACT_24355180
PTGS27.7IC5020nMCHEMBL_ACT_28834775
PTGS17.68AC5020.7nMCHEMBL_ACT_25205173
Q057697.66IC5022nMCHEMBL_ACT_2128847
Q057697.66IC5022nMCHEMBL_ACT_2128900
PTGS17.63AC5023.2nMCHEMBL_ACT_25206106
PTGS27.58IC5026nMCHEMBL_ACT_1610387
PTGS27.55IC5028nMCHEMBL_ACT_2128876
Q057697.52IC5030nMCHEMBL_ACT_13487855
PTGS17.52IC5030nMCHEMBL_ACT_2326107
Q639217.5AC5031.4nMCHEMBL_ACT_25174168
PTGS27.43IC5037nMCHEMBL_ACT_7681235
PTGS27.3IC5050nMCHEMBL_ACT_1082118
PTGS27.3IC5050nMCHEMBL_ACT_18204568

Target pathways

Aggregated over 6 target gene(s): SLC36A1, PTGS1, PTGS2, TRPM3, PPARG, ASIC3.

Top Reactome pathways

25 total, by targets touching each:

PathwayTargetsGenes
Synthesis of Prostaglandins (PG) and Thromboxanes (TX)2PTGS1, PTGS2
Transport of small molecules2ASIC3, SLC36A1
COX reactions1PTGS1
PPARA activates gene expression1PPARG
Synthesis of 15-eicosatetraenoic acid derivatives1PTGS2
Stimuli-sensing channels1ASIC3
TRP channels1TRPM3
Amino acid transport across the plasma membrane1SLC36A1
Transcriptional regulation of white adipocyte differentiation1PPARG
Nuclear Receptor transcription pathway1PPARG
SUMOylation of intracellular receptors1PPARG
R-HSA-4253931SLC36A1
SLC-mediated transmembrane transport1SLC36A1
Proton-coupled neutral amino acid transporters1SLC36A1
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
Ion channel transport1ASIC3
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
monoatomic ion transport3
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

Indications & clinical

Indications

34 indications (14 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
rheumatoid arthritis4MONDO:0008383EFO:0000685
rheumatic disorder4MONDO:0005554EFO:0005755
actinic keratosis4MONDO:0005173EFO:0002496
keratosis4MONDO:0006566EFO:1000720
cataract4MONDO:0005129MONDO:0005129
osteoarthritis4MONDO:0005178MONDO:0005178
migraine disorder4MONDO:0005277MONDO:0005277
osteoarthritis, knee3MONDO:0005416EFO:0004616
ankylosing spondylitis3MONDO:0005306EFO:0003898
infertility disorder3MONDO:0005047EFO:0000545
osteoarthritis, hip3MONDO:0006629EFO:1000786
gastric ulcer3MONDO:0001126EFO:0009454
basal cell carcinoma2MONDO:0020804EFO:0004193
pulmonary embolism2MONDO:0005279EFO:0003827
carcinoma2MONDO:0004993EFO:0000313
injury2MONDO:0021178EFO:0000546
bile duct disorder2MONDO:0002887MONDO:0002887
neoplasm1MONDO:0005070EFO:0000616
periodontitis1MONDO:0005076EFO:0000649
depressive disorder1MONDO:0002050MONDO:0002050
bone fracture1MONDO:0005315EFO:0003931
pancreatitis1MONDO:0004982EFO:0000278
alcohol abuse0MONDO:0002046MONDO:0007079

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

Clinical trials

Total trials: 227.

Phase distribution

PhaseTrials
PHASE464
Not specified60
PHASE347
PHASE122
PHASE221
PHASE2/PHASE35
PHASE1/PHASE25
EARLY_PHASE13

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03781544PHASE4RECRUITINGEffects of Opioids and NSAIDs on Sympathetic Nervous System and Vascular Function
NCT05387525PHASE4ACTIVE_NOT_RECRUITINGA Study of Tirbanibulin Ointment and Diclofenac Sodium Gel for the Treatment of Adult Participants With Actinic Keratosis on the Face or Scalp
NCT06373978PHASE4RECRUITINGNonNarcotic Pain Control in Percutaneous Needle Tenotomy of Elbow
NCT06918340PHASE4ACTIVE_NOT_RECRUITINGEvaluation of Analgesic Efficacy of Lidocaine and Diclofenac Spray in Radial Artery Blood Gas Sampling by Visual Analogue Scale and Perfusion Index
NCT00141102PHASE4COMPLETEDStudy Of Celecoxib Or Diclofenac And Omeprazole For Gastrointestinal (GI) Safety In High GI Risk Patients With Arthritis
NCT00174317PHASE4COMPLETEDCelecoxib Versus Diclofenac In The Treatment Of Osteoarthritis Of The Hip
NCT00204542PHASE4COMPLETEDComparison of the Efficacy and Tolerability of Solaraze for 3 Versus 6 Months in Patients With Mild to Moderate Actinic Keratosis Located on the Face and Head
NCT00247052PHASE4COMPLETEDNon Steroidal Anti Inflammatory Treatment for Post Operative Pericardial Effusion
NCT00428025PHASE4TERMINATEDDiclofenac for the Prevention of Post-ERCP Pancreatitis in Higher Risk Patients
NCT00447759PHASE4COMPLETEDThe Standard Care Versus Celecoxib Outcome Trial
NCT00491192PHASE4UNKNOWNNormothermia in Patients With Acute Cerebral Damage
NCT00568217PHASE4COMPLETEDAntipyretics for Preventing Recurrences of Febrile Seizures
NCT00595543PHASE4COMPLETEDTreatment of Acute Pseudophakic Cystoid Macular Edema: Bromfenac 0.09% Versus Diclofenac Sodium 0.1% Versus Ketorolac Tromethamine 0.5%
NCT00640432PHASE4COMPLETEDSafety And Efficacy Of Celecoxib Versus Sodium Diclofenac In The Treatment Of Acute Low Back Pain
NCT00649610PHASE4COMPLETEDRandomized, Double Blind, Multicenter Study of the Safety and Efficacy of Valdecoxib 40 mg Once Daily Compared With Diclofenac 75 mg Twice Daily in Acute Low Back Pain
NCT00650598PHASE4COMPLETEDA Multicentre, Double-Blind, Double-Dummy, Randomised Study of the Analgesic Efficacy and Safety of Valdecoxib Compared to Diclofenac Sodium in Patients Undergoing Knee Arthroscopy for Anterior Cruciate Ligament (ACL) Reconstruction
NCT00671320PHASE4COMPLETEDA Multi-Center, Randomized, Double-Blind, Parallel Group Study To Compare The Efficacy And Tolerability Of Valdecoxib And Diclofenac In Patients With A Sprained Ankle
NCT00766402PHASE4TERMINATEDAn Efficacy and Safety Study of Tramadol/Acetaminophen Versus Diclofenac in the Treatment of Pain in Participants With Ankylosing Spondylitis Receiving Stable Treatment of Disease Modifying Anti-rheumatic Drugs (DMARDs)
NCT00777127PHASE4COMPLETEDLong-term Effects of Imiquimod and Diclofenac in Actinic Keratoses
NCT00792376PHASE4COMPLETEDNSAIDs in Acute Achilles Tendinopathy: Effect on Pain Control, Leg Stiffness and Functional Recovery in Athletes
NCT00800527PHASE4COMPLETEDEfficacy of Gabapentin in the Treatment of Chest Pain and Paresthesia in Patients With Sternotomy
NCT00801528PHASE4COMPLETEDDiclofenac vs. Ropivacaine for Cesarean Section
NCT00894790PHASE4TERMINATEDCelecoxib Efficacy And Safety Versus Diclofenac In Acute Pain Due To Cervical Sprain Related To A Traffic Accident
NCT01039545PHASE4TERMINATEDSymptomatic Therapy of Uncomplicated Lower Urinary Tract Infections in the Ambulatory Setting.
NCT01067430PHASE4WITHDRAWNComparison of the Effect of Etoricoxib and Diclofenac on Early Morning Activity in Rheumatoid Arthritis (RA)
NCT01190722PHASE4WITHDRAWNA Study Comparing Etoricoxib and Diclofenac Sodium in Post Hallux Valgus Surgery Pain
NCT01453179PHASE4COMPLETEDLong-term Effects of Imiquimod and Diclofenac in Actinic Keratoses (LEIDA 2)
NCT01454791PHASE4COMPLETEDDiclofenac Sodium Topical Gel to Reduce Injection Site Discomfort in Patients Taking Glatiramer Acetate
NCT01458600PHASE4COMPLETEDAdjuvant Treatment of Graves´ Ophthalmopathy With NSAID (aGO Study)
NCT01860833PHASE4COMPLETEDNSAID Treatment in Knee Osteoarthritis
NCT01907984PHASE4COMPLETEDDiclofenac Administered Before Skull Operations Reduces the Severity of Headache After the Intervention
NCT02132247PHASE4COMPLETEDSafety Study of Flector Patch in Children With Minor Soft Tissue Injuries
NCT02181920PHASE4TERMINATEDMetamizol for the Treatment of Neoplastic Chronic Pain
NCT02183129PHASE4COMPLETEDStudy to Assess the Efficacy and Safety of Meloxicam vs. Diclofenac SR in Patients With Osteoarthritis of the Knee
NCT02187614PHASE4COMPLETEDEfficacy Study of Different Analgesic Options in Kidney Stone Pain Management
NCT02229747PHASE4COMPLETEDEfficacy and Safety of Meloxicam Suspension Versus Diclofenac Suspension or Nimesulide Suspension in Patients With a Diagnosis of Acute, Non-bacterial Pharyngitis, Pharyngotonsillitis or Laryngitis
NCT02287376PHASE4COMPLETEDPharmacokinetics & Safety of Cambia® in Migraine With or Without Aura in 12-17 Year Olds
NCT02406014PHASE4COMPLETEDEfficacy and Safety of Ingenol Mebutate Gel 0.015% Compared to Diclofenac Sodium Gel 3% in Subjects With Actinic Keratoses on the Face or Scalp
NCT02445599PHASE4COMPLETEDDiclofenac Premedication, as the Effect of Preemptive Analgesia After Post-thoracotomy Chest and Shoulder Pain
NCT02528201PHASE4COMPLETEDA Study Of Celecoxib Versus Diclofenac In Patients With Ankylosing Spondylitis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (2) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

GuidelineSourceGene(s)DosingRecommendation
Annotation of CPIC Guideline for diclofenac, ibuprofen and CYP2C8CPICCYP2C8
Annotation of CPIC Guideline for aceclofenac, aspirin, diclofenac, dipCPICCYP2C9

PharmGKB also curates 7 clinical and 53 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.

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

MoleculeSourceStatusShared targets
ASPIRINChEMBL + PubChemPhase 4 (approved)ASIC3, PTGS1, PTGS2
MEFENAMIC ACIDChEMBL + PubChemPhase 4 (approved)PTGS1, PTGS2, TRPM3
INDOMETHACINChEMBLPhase 4 (approved)PPARG, PTGS1, PTGS2
LUMIRACOXIBChEMBLPhase 4 (approved)PPARG, PTGS1, PTGS2
TROGLITAZONEChEMBLPhase 4 (approved)PPARG, PTGS1, PTGS2
RESVERATROLChEMBLPhase 3PPARG, PTGS1, PTGS2
CycloserineChEMBL + PubChemPhase 4 (approved)PTGS1, SLC36A1
cysteineChEMBL + PubChemPhase 4 (approved)PTGS1, SLC36A1
FulvestrantChEMBL + PubChemPhase 4 (approved)PPARG, PTGS2
PioglitazoneChEMBL + PubChemPhase 4 (approved)PPARG, TRPM3
RosiglitazoneChEMBL + PubChemPhase 4 (approved)PPARG, TRPM3
3,3’,4’,5-TETRACHLOROSALICYLANILIDEChEMBLPhase 4 (approved)PTGS1, PTGS2
ACEMETACINChEMBLPhase 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
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
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