Sarpogrelate

Summary

Sarpogrelate (CHEMBL52939) is a phase-3 clinical-stage small molecule targeting HTR2A, HTR2B, and HTR2C; indicated across 2 conditions including peripheral arterial disease and cerebral infarction.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 3 (HTR2A, HTR2B, HTR2C)
• Indications: 2 conditions
• Clinical trials: 11
• Chemistry: 429.5 Da · C24H31NO6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL52939
Name	Sarpogrelate
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5160
Molecular formula	C24H31NO6
Molecular weight	429.5
InChIKey	FFYNAVGJSYHHFO-UHFFFAOYSA-N

SMILES: CN(C)CC(COC1=CC=CC=C1CCC2=CC(=CC=C2)OC)OC(=O)CCC(=O)O

IUPAC name: 4-[1-(dimethylamino)-3-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]propan-2-yl]oxy-4-oxobutanoic acid

Also known as: Sarpogrelate, Sarpogrelato, SID124893325, SID50112742, SID174006666, SARPOGRELATE, SARPOGRELATE (HYDROCHLORIDE), Sarpogrelate (hydrochloride)

Parent form; salt/anhydrous children: CHEMBL541829

Patent coverage: 465 distinct patent families (1,493 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 1,475 (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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
HTR2A	5-HT2A receptor	Antagonist	8.5	0%	P28223
HTR2B	5-HT2B receptor	Antagonist	6.6	0.4%	P41595
HTR2C	5-HT2C receptor	Antagonist	7.4	0%	P28335

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 3 target gene(s): HTR2A, HTR2B, HTR2C.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	3	HTR2A, HTR2B, HTR2C
Signaling by GPCR	3	HTR2A, HTR2B, HTR2C
Class A/1 (Rhodopsin-like receptors)	3	HTR2A, HTR2B, HTR2C
Amine ligand-binding receptors	3	HTR2A, HTR2B, HTR2C
GPCR downstream signalling	3	HTR2A, HTR2B, HTR2C
Serotonin receptors	3	HTR2A, HTR2B, HTR2C
G alpha (q) signalling events	3	HTR2A, HTR2B, HTR2C
GPCR ligand binding	3	HTR2A, HTR2B, HTR2C

Dominant GO biological processes

GO term	Targets
intracellular calcium ion homeostasis	3
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	3
phospholipase C-activating serotonin receptor signaling pathway	3
serotonin receptor signaling pathway	3
chemical synaptic transmission	3
positive regulation of phosphatidylinositol biosynthetic process	3
release of sequestered calcium ion into cytosol	3
positive regulation of ERK1 and ERK2 cascade	3
G protein-coupled serotonin receptor signaling pathway	3
signal transduction	3
G protein-coupled receptor signaling pathway	3
positive regulation of cell population proliferation	2
response to xenobiotic stimulus	2
positive regulation of fat cell differentiation	2
obsolete cGMP-mediated signaling	2

Indications & clinical

Indications

2 indications (0 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).

Indication	Trial phase	MONDO	EFO
peripheral arterial disease	3	MONDO:0005386	EFO:0004265
cerebral infarction	3	MONDO:0002679	MONDO:0002679

Clinical trials

Total trials: 11.

Phase distribution

Phase	Trials
PHASE4	4
PHASE1	3
Not specified	3
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01165567	PHASE4	UNKNOWN	The Prevention of Contrast Induced Nephropathy by Sarpogrelate in Patients With Chronic Kidney Disease
NCT01674686	PHASE4	UNKNOWN	The Effect of Sarpogrelate and High Dose Statin on the Reduction of Coronary Spasm
NCT02607436	PHASE4	COMPLETED	Effect of Sarpogrelate, a Serotonin Receptor Antagonist, on Coronary Artery Disease
NCT06046196	PHASE4	COMPLETED	Clinical Trial to Evaluate the Efficacy and Safety of Sarpogrelate SR in Patients With Chronic Artery Occlusive Disease
NCT02294643	PHASE3	COMPLETED	Study Design of ‘Influence of Sarpogrelate in Patients With Renal Impairment or Diabetes Mellitus’ Study
NCT02097511	PHASE1	COMPLETED	Sarpogrelate Drug Interaction
NCT03947489	PHASE1	COMPLETED	Bioavailability Study of Two Formulations of Sarpogrelate HCl 300mg Tablets Under Fasting Conditions
NCT03947528	PHASE1	UNKNOWN	Bioavailability Study of Two Formulations of Sarpogrelate HCl 300mg Tablets Under Fed Conditions
NCT06424548	Not specified	NOT_YET_RECRUITING	Comparison of the Improvement and Safety of the Ankle Brachial Arterial Pressure Index of Sarpogrelate and Clopidogrel in Stroke Patients With Decreased Ankle Brachial Arterial Pressure Index and Intermittent Claudication of Lower Limb Vascular Atherosclerosis.
NCT01548274	Not specified	UNKNOWN	Impact of Sarpogrelate in the Function of Endothelial Progenitor Cells
NCT05083299	Not specified	COMPLETED	Multicenter, Therapeutic Use Observational Study to Evaluate the Effects of Concurrent Therapy of Sarpogrelate

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.

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

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
FIDAXOMICIN	ChEMBL + PubChem	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
PIMAVANSERIN	ChEMBL + PubChem	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
PROPOXYPHENE	ChEMBL + PubChem	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ALOSETRON	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AMIODARONE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AMLODIPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AMOXAPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
APOMORPHINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ASENAPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ATOMOXETINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AZATADINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AZELASTINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BENFLUOREX	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BENPERIDOL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BENZTROPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BUSPIRONE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CANNABIDIOL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CARIPRAZINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CARVEDILOL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CINACALCET	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CISAPRIDE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CITALOPRAM	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CLEMASTINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CLOZAPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CYCLIZINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DAPIPRAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DASATINIB	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DESIPRAMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DESLORATADINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DICYCLOMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DIMENHYDRINATE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DOMPERIDONE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DOTHIEPIN	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DOXAZOSIN	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DOXEPIN	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DROPERIDOL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DULOXETINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
EBASTINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ECONAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ENCAINIDE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ERGOTAMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
FLUOXETINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
GUANABENZ	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C