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Flurbiprofen

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Also known as AnsaidBTS 18,322BTS-18322CebutidFlubiprofenFlurbiprofeneFlurbiprofenoFrobenFroben srNSC-757037StrefenTransactU-27,182U-27182FluriprofenSID26747178SID855731SID860839SID49732000

Summary

Flurbiprofen (CHEMBL563) is an approved small-molecule non-steroidal anti-inflammatory drug (ATC M02AA19) targeting SLC36A1, PTGS1, and PTGS2; indicated across 16 conditions including eye disorder and rheumatic disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: M02AA19 (+3 more)
  • Targets: 4 (SLC36A1, PTGS1, PTGS2…)
  • Indications: 16 conditions
  • Clinical trials: 45
  • Chemistry: 244.26 Da · C15H13FO2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL563
NameFlurbiprofen
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3394
ChEBICHEBI:5130
ATCM02AA19, S01BC04, M01AE09, R02AX01
Molecular formulaC15H13FO2
Molecular weight244.26
InChIKeySYTBZMRGLBWNTM-UHFFFAOYSA-N

SMILES: CC(C1=CC(=C(C=C1)C2=CC=CC=C2)F)C(=O)O

IUPAC name: 2-(3-fluoro-4-phenylphenyl)propanoic acid

ChEBI definition: A monocarboxylic acid that is a 2-fluoro-[1,1’-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.

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

Also known as: Ansaid, BTS 18,322, BTS-18322, Cebutid, Flubiprofen, Flurbiprofen, Flurbiprofene, Flurbiprofeno, Froben, Froben sr, NSC-757037, Strefen

Parent form; salt/anhydrous children: CHEMBL1200990, CHEMBL3989754, CHEMBL5416694

Patent coverage: 18,958 distinct patent families (71,809 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 71,264 (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 1Inhibition3.550.2%Q7Z2H8
PTGS1COX-1Inhibition7.120%P23219
PTGS2COX-2Inhibition80%P35354
ASIC1ASIC13.52.6%P78348

Broader ChEMBL bioactivity targets: 18 (assay-derived). Sample: Solute carrier family 22 member 6, Alpha-2B adrenergic receptor, Thyrotropin receptor, Menin/Histone-lysine N-methyltransferase MLL, Prostaglandin G/H synthase 1, 5-hydroxytryptamine receptor 2C, Prostaglandin G/H synthase 2, D(3) dopamine receptor, Muscarinic acetylcholine receptor M3, Prostaglandin G/H synthase 1.

Bioactivity

ChEMBL activities: 32 potent at pChembl ≥ 5 of 36 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PTGS18.52AC503nMCHEMBL_ACT_25205454
PTGS18IC5010nMCHEMBL_ACT_2069749
PTGS28IC5010nMCHEMBL_ACT_2069750
PTGS28IC5010nMCHEMBL_ACT_929376
P059797.96IC5011nMCHEMBL_ACT_929375
P059797.92IC5012nMCHEMBL_ACT_473613
PTGS17.8AC5015.9nMCHEMBL_ACT_25206385
PTGS17.68IC5021nMCHEMBL_ACT_7676454
DRD37.07AC5086nMCHEMBL_ACT_25193664
P059796.82IC50150nMCHEMBL_ACT_16498461
Q639216.77IC50170nMCHEMBL_ACT_1605969
PTGS26.45IC50359nMCHEMBL_ACT_7676456
PTGS26.39IC50410nMCHEMBL_ACT_29210035
AKR1C36.34IC50460nMCHEMBL_ACT_25568380
P059796.32IC50480nMCHEMBL_ACT_29210027
Q057696.3IC50500nMCHEMBL_ACT_3117831
P059796.3IC50500nMCHEMBL_ACT_3117833
CHRM36.27AC50540nMCHEMBL_ACT_25136821
AKR1C26.26IC50550nMCHEMBL_ACT_25568312
P059796Ki1000nMCHEMBL_ACT_473614
PTGS25.98IC501040nMCHEMBL_ACT_27192827
PTGS25.97IC501060nMCHEMBL_ACT_16498501
P026925.93Ki1180nMCHEMBL_ACT_2445231
SLC22A65.82IC501500nMCHEMBL_ACT_11000921
AKR1C35.81IC501560nMCHEMBL_ACT_12105574
ADRA2B5.72AC501900nMCHEMBL_ACT_25143838
PTGS15.7IC501995nMCHEMBL_ACT_16804600
PTGS25.7IC501995nMCHEMBL_ACT_16804601
AKR1C15.69IC502050nMCHEMBL_ACT_25568516
HTR2C5.58AC502600nMCHEMBL_ACT_25131943

Target pathways

Aggregated over 4 target gene(s): SLC36A1, PTGS1, PTGS2, ASIC1.

Top Reactome pathways

16 total, by targets touching each:

PathwayTargetsGenes
Synthesis of Prostaglandins (PG) and Thromboxanes (TX)2PTGS1, PTGS2
Transport of small molecules2ASIC1, SLC36A1
COX reactions1PTGS1
Synthesis of 15-eicosatetraenoic acid derivatives1PTGS2
Stimuli-sensing channels1ASIC1
Amino acid transport across the plasma membrane1SLC36A1
R-HSA-4253931SLC36A1
SLC-mediated transmembrane transport1SLC36A1
Proton-coupled neutral amino acid transporters1SLC36A1
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
Ion channel transport1ASIC1

Dominant GO biological processes

GO termTargets
monoatomic ion transport2
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
amino acid transport1
taurine transmembrane transport1

Indications & clinical

Indications

16 indications (5 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
pharyngitis3MONDO:0002258MONDO:0002258
periodontitis2MONDO:0005076EFO:0000649
rheumatoid arthritis1MONDO:0008383EFO:0000685
HIV infectious disease1MONDO:0005109EFO:0000764
anemia1MONDO:0002280EFO:0004272
type 2 diabetes mellitus1MONDO:0005148MONDO:0005148
inborn mitochondrial metabolism disorder1MONDO:0004069MONDO:0044970
bone fracture1MONDO:0005315EFO:0003931
sickle cell disease1MONDO:0011382MONDO:0011382

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

Clinical trials

Total trials: 45.

Phase distribution

PhaseTrials
PHASE117
PHASE49
Not specified8
PHASE24
PHASE33
EARLY_PHASE13
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07531147PHASE4NOT_YET_RECRUITINGEffects of Flurbiprofen Spray and Ice Cream for Pain and Voice Outcomes After Thyroidectomy
NCT01998217PHASE4COMPLETEDCombination of Remifentanil and Flurbiprofen in Sedation and Analgesia for ESWL of Pancreatic Stone
NCT02114463PHASE4UNKNOWNComparison of Two Kinds of Postoperative Analgesia After Amputation
NCT02569905PHASE4COMPLETEDEffect of Parecoxib Sodium and Flurbiprofen Injection on Postoperative Shivering
NCT03014713PHASE4UNKNOWNEffect of Dexmedetomidine for Postoperative Intravenous Patient Controlled Analgesia
NCT03745599PHASE4COMPLETEDEvaluation of the Effects of Different Analgesics on Pericoronitis Pain and Quality of Life
NCT04602845PHASE4COMPLETEDRemimazolam Tosilate Sedation and Midazolam Sedation in Dental Patients
NCT06041178PHASE4COMPLETEDFlurbiprofen Versus Aloe Vera Gel in the Treatment of Chronic Periodontitis in Smoking Patients.
NCT06238154PHASE4COMPLETEDFlurbiprofen Tablet vs Spray In Oral Soft Tissue Wounds
NCT01048866PHASE3COMPLETEDA Study of Flurbiprofen 8.75 mg Lozenge in Patients With Pharyngitis
NCT01049334PHASE3COMPLETEDA Study of Flurbiprofen 8.75 mg Lozenge in Patient With Pharyngitis
NCT01986361PHASE3COMPLETEDPlacebo-Controlled Onset-of-Action Study of Flurbiprofen Utilizing the Double-Stopwatch Method
NCT00001724PHASE2COMPLETEDLocal Flurbiprofen to Treat Pain Following Wisdom Tooth Extraction
NCT01026714PHASE1/PHASE2COMPLETEDCYP2C9 Activity Evaluated With a Simple Finger Prick
NCT01040286PHASE2COMPLETEDThe Efficacy and Safety of Flurbiprofen Chip Versus Chlorhexidine Chip (Periochip®) in Therapy of Adult Chronic Periodontitis
NCT01535079PHASE2COMPLETEDAcute Sore Throat Pain Study
NCT04708964PHASE2UNKNOWNOro-tracheal Intubation: Flurbiprofen Subglottic Instillation to Prevent Laryngeal Inflammation
NCT00443170PHASE1COMPLETEDA Placebo-controlled Study to Investigate the Safety, and Pharmacokinetics of Oral GSK626616AC in Healthy Subjects
NCT00615212PHASE1COMPLETEDEffect of GSK376501 on CYP450 Activity in Healthy Adult Subjects
NCT00920088PHASE1COMPLETEDDrug Interaction Study of Darunavir/Ritonavir and Lopinavir/Ritonavir on GSK2248761 PK and CYP450 Probe Drugs
NCT00964106PHASE1COMPLETEDValidation Study of Multiple Probe Compounds for Drug Interaction Evaluation
NCT02227173PHASE1COMPLETEDA Phase 1 Drug-drug Interaction Study in Healthy Volunteers
NCT02391688PHASE1COMPLETEDEvaluation of the Potential Pharmacokinetic Interactions Between Probe Drugs in the Geneva Phenotyping Cocktail
NCT03131973PHASE1COMPLETEDEffects of Concomitant Administration of BMS-986195 on Methotrexate, Caffeine, Montelukast, Flurbiprofen, Omeprazole, Midazolam, Digoxin, and Pravastatin
NCT04425902PHASE1COMPLETEDEvaluation of Pharmacokinetic Interaction Between GSK3640254 and Caffeine, Metoprolol, Montelukast, Flurbiprofen, Omeprazole, Midazolam, Digoxin, and Pravastatin in Healthy Adults
NCT04643249PHASE1COMPLETEDDrug-drug Interaction Study of KL1333 in Healthy Subjects
NCT05254548PHASE1COMPLETEDA Study to Investigate the Effect of Single and Repeated Oral Doses of ACT-539313 on What the Body Does to Flurbiprofen, Omeprazole, Midazolam in Healthy Subjects
NCT05512013PHASE1COMPLETEDThe Effects of NSAIDs on Bone Metabolism Following Exercise
NCT05852769PHASE1COMPLETEDA Study to Evaluate the Drug-drug Interaction Potential of BMS-986196 in Healthy Participants
NCT05932277PHASE1COMPLETEDA Study to Assess the Effect of BMS-986419 on the Single Dose Drug Levels of Probe Substrates in Healthy Participants
NCT05981365PHASE1COMPLETEDVoxelotor CYP and Transporter Cocktail Interaction Study
NCT06823284PHASE1COMPLETEDTo Assess the Bioavailability of TK-254RX in Comparison with Oral Flurbiprofen Tablets and the Adhesion of TK-254RX in Healthy Subjects
NCT07223671PHASE1COMPLETEDStudy to Evaluate the Effect of Repotrectinib on the Drug Levels of Transporter and CYP P450 Probe Substrates in Healthy Adult Participants
NCT07235748PHASE1COMPLETEDDrug-drug Interaction Study of Vorasidenib With Bupropion, Repaglinide, Flurbiprofen, Omeprazole, Midazolam, and Rosuvastatin in Healthy Adult Participants
NCT03090009EARLY_PHASE1UNKNOWNMicrobiome Shift in Peri-mucositis by Anti-inflammatory Drugs
NCT03165929EARLY_PHASE1COMPLETEDOral Flurbiprofen Spray for Mucosal Graft Harvesting at the Palatal Area
NCT05955885EARLY_PHASE1COMPLETEDEffect of Over-the-counter NSAIDS on Cough Reflex Sensitivity in Patients with Upper Respiratory Tract Infections
NCT00162474Not specifiedRECRUITINGDeterminants of Warfarin Metabolism
NCT07163429Not specifiedACTIVE_NOT_RECRUITINGEfficacy of Flurbiprofen Spray for Postoperative Sore Throat Following Double-Lumen Endobronchial Intubation
NCT02403687Not specifiedCOMPLETEDProspective Analgesic Compound Efficacy (PACE) Study

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 celecoxib, flurbiprofen, ibuprofen, lCPICCYP2C9yesyes

PharmGKB also curates 2 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.

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

MoleculeSourceStatusShared targets
CycloserineChEMBL + PubChemPhase 4 (approved)PTGS1, SLC36A1
cysteineChEMBL + PubChemPhase 4 (approved)PTGS1, SLC36A1
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
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
KETOROLACChEMBLPhase 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

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