Esflurbiprofen

Summary

Esflurbiprofen (CHEMBL435298) is an approved small molecule (ATC M02AA29) targeting PTGS2; indicated across 3 conditions.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: M02AA29
• Targets: 1 (PTGS2)
• Indications: 3 conditions
• Clinical trials: 45
• Chemistry: 244.26 Da · C15H13FO2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL435298
Name	Esflurbiprofen
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	72099
ChEBI	CHEBI:42446
ATC	M02AA29
Molecular formula	C15H13FO2
Molecular weight	244.26
InChIKey	SYTBZMRGLBWNTM-JTQLQIEISA-N

SMILES: C[C@@H](C1=CC(=C(C=C1)C2=CC=CC=C2)F)C(=O)O

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

Also known as: BTS 24332, BTS-24332, Esflurbiprofen, Esflurbiprofene, Esflurbiprofeno, Flurbiprofen, (s)-, S-flurbiprofen, SID47193727, ESFLURBIPROFEN, FLURBIPROFEN, flurbiprofen-(S)-(+), Flurbiprofen

Patent coverage: 155 distinct patent families (301 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
PTGS2	COX-2	Inhibition	6.04	0%	P35354

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Prostaglandin G/H synthase 1, Prostaglandin G/H synthase 2, Prostaglandin G/H synthase 1.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q63921	7.52	IC50	30	nM	CHEMBL_ACT_1606542
PTGS2	6.04	IC50	910	nM	CHEMBL_ACT_1606543
PTGS1	5.7	IC50	2000	nM	CHEMBL_ACT_1707744

Target pathways

Aggregated over 1 target gene(s): PTGS2.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Synthesis of 15-eicosatetraenoic acid derivatives	1	PTGS2
Synthesis of Prostaglandins (PG) and Thromboxanes (TX)	1	PTGS2
Interleukin-10 signaling	1	PTGS2
Interleukin-4 and Interleukin-13 signaling	1	PTGS2
Biosynthesis of DHA-derived SPMs	1	PTGS2
Biosynthesis of EPA-derived SPMs	1	PTGS2
Biosynthesis of DPAn-3 SPMs	1	PTGS2
Biosynthesis of electrophilic ω-3 PUFA oxo-derivatives	1	PTGS2

Dominant GO biological processes

GO term	Targets
prostaglandin biosynthetic process	1
response to oxidative stress	1
embryo implantation	1
regulation of blood pressure	1
response to nematode	1
response to selenium ion	1
positive regulation of vascular endothelial growth factor production	1
cyclooxygenase pathway	1
lipoxygenase pathway	1
positive regulation of prostaglandin biosynthetic process	1
positive regulation of fever generation	1
prostaglandin secretion	1
regulation of cell population proliferation	1
long-chain fatty acid biosynthetic process	1
positive regulation of nitric oxide biosynthetic process	1

Indications & clinical

Indications

3 indications (2 at ChEMBL trial phase 4).

The 3 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 45.

Phase distribution

Phase	Trials
PHASE1	19
PHASE4	8
Not specified	7
PHASE3	4
PHASE2	3
EARLY_PHASE1	3
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07531147	PHASE4	NOT_YET_RECRUITING	Effects of Flurbiprofen Spray and Ice Cream for Pain and Voice Outcomes After Thyroidectomy
NCT01998217	PHASE4	COMPLETED	Combination of Remifentanil and Flurbiprofen in Sedation and Analgesia for ESWL of Pancreatic Stone
NCT02114463	PHASE4	UNKNOWN	Comparison of Two Kinds of Postoperative Analgesia After Amputation
NCT02569905	PHASE4	COMPLETED	Effect of Parecoxib Sodium and Flurbiprofen Injection on Postoperative Shivering
NCT03745599	PHASE4	COMPLETED	Evaluation of the Effects of Different Analgesics on Pericoronitis Pain and Quality of Life
NCT04602845	PHASE4	COMPLETED	Remimazolam Tosilate Sedation and Midazolam Sedation in Dental Patients
NCT06041178	PHASE4	COMPLETED	Flurbiprofen Versus Aloe Vera Gel in the Treatment of Chronic Periodontitis in Smoking Patients.
NCT06238154	PHASE4	COMPLETED	Flurbiprofen Tablet vs Spray In Oral Soft Tissue Wounds
NCT01048866	PHASE3	COMPLETED	A Study of Flurbiprofen 8.75 mg Lozenge in Patients With Pharyngitis
NCT01049334	PHASE3	COMPLETED	A Study of Flurbiprofen 8.75 mg Lozenge in Patient With Pharyngitis
NCT01986361	PHASE3	COMPLETED	Placebo-Controlled Onset-of-Action Study of Flurbiprofen Utilizing the Double-Stopwatch Method
NCT03434197	PHASE3	COMPLETED	Safety and Efficacy of SFPP in Knee Osteoarthritis
NCT00001724	PHASE2	COMPLETED	Local Flurbiprofen to Treat Pain Following Wisdom Tooth Extraction
NCT01026714	PHASE1/PHASE2	COMPLETED	CYP2C9 Activity Evaluated With a Simple Finger Prick
NCT01040286	PHASE2	COMPLETED	The Efficacy and Safety of Flurbiprofen Chip Versus Chlorhexidine Chip (Periochip®) in Therapy of Adult Chronic Periodontitis
NCT04708964	PHASE2	UNKNOWN	Oro-tracheal Intubation: Flurbiprofen Subglottic Instillation to Prevent Laryngeal Inflammation
NCT07307794	PHASE1	RECRUITING	To Evaluate the Adhesion of TK-254RX on Healthy Participants
NCT00443170	PHASE1	COMPLETED	A Placebo-controlled Study to Investigate the Safety, and Pharmacokinetics of Oral GSK626616AC in Healthy Subjects
NCT00615212	PHASE1	COMPLETED	Effect of GSK376501 on CYP450 Activity in Healthy Adult Subjects
NCT00920088	PHASE1	COMPLETED	Drug Interaction Study of Darunavir/Ritonavir and Lopinavir/Ritonavir on GSK2248761 PK and CYP450 Probe Drugs
NCT00964106	PHASE1	COMPLETED	Validation Study of Multiple Probe Compounds for Drug Interaction Evaluation
NCT02227173	PHASE1	COMPLETED	A Phase 1 Drug-drug Interaction Study in Healthy Volunteers
NCT02391688	PHASE1	COMPLETED	Evaluation of the Potential Pharmacokinetic Interactions Between Probe Drugs in the Geneva Phenotyping Cocktail
NCT03131973	PHASE1	COMPLETED	Effects of Concomitant Administration of BMS-986195 on Methotrexate, Caffeine, Montelukast, Flurbiprofen, Omeprazole, Midazolam, Digoxin, and Pravastatin
NCT04425902	PHASE1	COMPLETED	Evaluation of Pharmacokinetic Interaction Between GSK3640254 and Caffeine, Metoprolol, Montelukast, Flurbiprofen, Omeprazole, Midazolam, Digoxin, and Pravastatin in Healthy Adults
NCT04643249	PHASE1	COMPLETED	Drug-drug Interaction Study of KL1333 in Healthy Subjects
NCT05254548	PHASE1	COMPLETED	A 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
NCT05512013	PHASE1	COMPLETED	The Effects of NSAIDs on Bone Metabolism Following Exercise
NCT05852769	PHASE1	COMPLETED	A Study to Evaluate the Drug-drug Interaction Potential of BMS-986196 in Healthy Participants
NCT05932277	PHASE1	COMPLETED	A Study to Assess the Effect of BMS-986419 on the Single Dose Drug Levels of Probe Substrates in Healthy Participants
NCT05981365	PHASE1	COMPLETED	Voxelotor CYP and Transporter Cocktail Interaction Study
NCT06823284	PHASE1	COMPLETED	To Assess the Bioavailability of TK-254RX in Comparison with Oral Flurbiprofen Tablets and the Adhesion of TK-254RX in Healthy Subjects
NCT06870422	PHASE1	COMPLETED	To Assess the Effect of the Special Condition on the Pharmacokinetics and Tolerability of the Esflurbiprofen Topical System (EFTS) in Healthy Volunteers.
NCT07223671	PHASE1	COMPLETED	Study to Evaluate the Effect of Repotrectinib on the Drug Levels of Transporter and CYP P450 Probe Substrates in Healthy Adult Participants
NCT07235748	PHASE1	COMPLETED	Drug-drug Interaction Study of Vorasidenib With Bupropion, Repaglinide, Flurbiprofen, Omeprazole, Midazolam, and Rosuvastatin in Healthy Adult Participants
NCT03090009	EARLY_PHASE1	UNKNOWN	Microbiome Shift in Peri-mucositis by Anti-inflammatory Drugs
NCT03165929	EARLY_PHASE1	COMPLETED	Oral Flurbiprofen Spray for Mucosal Graft Harvesting at the Palatal Area
NCT05955885	EARLY_PHASE1	COMPLETED	Effect of Over-the-counter NSAIDS on Cough Reflex Sensitivity in Patients with Upper Respiratory Tract Infections
NCT00162474	Not specified	RECRUITING	Determinants of Warfarin Metabolism
NCT07163429	Not specified	ACTIVE_NOT_RECRUITING	Efficacy of Flurbiprofen Spray for Postoperative Sore Throat Following Double-Lumen Endobronchial Intubation

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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.

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

Molecule	Source	Status	Shared targets
FIDAXOMICIN	ChEMBL + PubChem	Phase 4 (approved)	PTGS2
3,3’,4’,5-TETRACHLOROSALICYLANILIDE	ChEMBL	Phase 4 (approved)	PTGS2
ABEMACICLIB	ChEMBL	Phase 4 (approved)	PTGS2
ACALABRUTINIB	ChEMBL	Phase 4 (approved)	PTGS2
ACEMETACIN	ChEMBL	Phase 4 (approved)	PTGS2
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	PTGS2
ACETYLCYSTEINE	ChEMBL	Phase 4 (approved)	PTGS2
ACRIVASTINE	ChEMBL	Phase 4 (approved)	PTGS2
AMODIAQUINE	ChEMBL	Phase 4 (approved)	PTGS2
AMPHOTERICIN B	ChEMBL	Phase 4 (approved)	PTGS2
AMSACRINE	ChEMBL	Phase 4 (approved)	PTGS2
ANISINDIONE	ChEMBL	Phase 4 (approved)	PTGS2
APOMORPHINE	ChEMBL	Phase 4 (approved)	PTGS2
ARFORMOTEROL	ChEMBL	Phase 4 (approved)	PTGS2
ASPIRIN	ChEMBL	Phase 4 (approved)	PTGS2
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	PTGS2
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	PTGS2
BEPRIDIL	ChEMBL	Phase 4 (approved)	PTGS2
BIPERIDEN	ChEMBL	Phase 4 (approved)	PTGS2
BROMFENAC	ChEMBL	Phase 4 (approved)	PTGS2
CALCIPOTRIENE	ChEMBL	Phase 4 (approved)	PTGS2
CALCITRIOL	ChEMBL	Phase 4 (approved)	PTGS2
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	PTGS2
CANNABIDIOL	ChEMBL	Phase 4 (approved)	PTGS2
CAPSAICIN	ChEMBL	Phase 4 (approved)	PTGS2
CAPTOPRIL	ChEMBL	Phase 4 (approved)	PTGS2
CARPROFEN	ChEMBL	Phase 4 (approved)	PTGS2
CEFAZOLIN	ChEMBL	Phase 4 (approved)	PTGS2
CEFTIZOXIME	ChEMBL	Phase 4 (approved)	PTGS2
CELECOXIB	ChEMBL	Phase 4 (approved)	PTGS2
CEPHRADINE	ChEMBL	Phase 4 (approved)	PTGS2
CIANIDANOL	ChEMBL	Phase 4 (approved)	PTGS2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	PTGS2
CRIZOTINIB	ChEMBL	Phase 4 (approved)	PTGS2
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	PTGS2
DESERPIDINE	ChEMBL	Phase 4 (approved)	PTGS2
DEXIBUPROFEN	ChEMBL	Phase 4 (approved)	PTGS2
DEXKETOPROFEN	ChEMBL	Phase 4 (approved)	PTGS2
DICLOFENAC	ChEMBL	Phase 4 (approved)	PTGS2
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	PTGS2
DOBUTAMINE	ChEMBL	Phase 4 (approved)	PTGS2
DOXORUBICIN	ChEMBL	Phase 4 (approved)	PTGS2
EPINEPHRINE	ChEMBL	Phase 4 (approved)	PTGS2
ERGOTAMINE	ChEMBL	Phase 4 (approved)	PTGS2
ETODOLAC	ChEMBL	Phase 4 (approved)	PTGS2
ETORICOXIB	ChEMBL	Phase 4 (approved)	PTGS2
FLUPIRTINE	ChEMBL	Phase 4 (approved)	PTGS2
FLURBIPROFEN	ChEMBL	Phase 4 (approved)	PTGS2
FLUVASTATIN	ChEMBL	Phase 4 (approved)	PTGS2
FOLIC ACID	ChEMBL	Phase 4 (approved)	PTGS2
GLAFENINE	ChEMBL	Phase 4 (approved)	PTGS2
HALOPERIDOL	ChEMBL	Phase 4 (approved)	PTGS2
HEXACHLOROPHENE	ChEMBL	Phase 4 (approved)	PTGS2
IBUPROFEN	ChEMBL	Phase 4 (approved)	PTGS2
ICOSAPENT ETHYL	ChEMBL	Phase 4 (approved)	PTGS2
INDAPAMIDE	ChEMBL	Phase 4 (approved)	PTGS2
INDOCYANINE GREEN ACID FORM	ChEMBL	Phase 4 (approved)	PTGS2
INDOMETHACIN	ChEMBL	Phase 4 (approved)	PTGS2
IPRONIAZID	ChEMBL	Phase 4 (approved)	PTGS2
ISOCARBOXAZID	ChEMBL	Phase 4 (approved)	PTGS2