Beraprost

Summary

Beraprost (CHEMBL1207745) is a phase-3 clinical-stage small-molecule vasodilator agent (ATC B01AC19) targeting PTGER3, PTGER4, and PTGIR; indicated across 2 conditions including thrombotic disease and chronic kidney disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: B01AC19
• Targets: 3 (PTGER3, PTGER4, PTGIR)
• Indications: 2 conditions
• Clinical trials: 10
• Chemistry: 398.5 Da · C24H30O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1207745
Name	Beraprost
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	6917951
ChEBI	CHEBI:135633
ATC	B01AC19
Molecular formula	C24H30O5
Molecular weight	398.5
InChIKey	CTPOHARTNNSRSR-APJZLKAGSA-N

SMILES: CC#CCC(C)[C@@H](/C=C/[C@H]1[C@@H](C[C@H]2[C@@H]1C3=CC=CC(=C3O2)CCCC(=O)O)O)O

IUPAC name: 4-[(1R,2R,3aS,8bS)-2-hydroxy-1-[(E,3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoic acid

ChEBI definition: An organic heterotricyclic compound that is (3aS,8bS)-2,3,3a,8b-tetrahydro-1H-benzo[b]cyclopenta[d]furan in which the hydrogens at positions 1R, 2R and 5 are replaced by (3S)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl, hydroxy and 3-carboxypropyl groups, respectively. It is a prostaglandin receptor agonist which is approved to treat pulmonary arterial hypertension in Asia.

Pharmacological roles (ChEBI): vasodilator agent, platelet aggregation inhibitor, antihypertensive agent, prostaglandin receptor agonist, anti-inflammatory agent.

Also known as: Beraprost, MDL-201229, ML-1229, TRK-100STP FREE ACID, BERAPROST

Parent form; salt/anhydrous children: CHEMBL435883

Patent coverage: 1,660 distinct patent families (6,541 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 6,502 (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
PTGER3	EP3 receptor	Agonist	6.17	2.6%	P43115
PTGER4	EP4 receptor	Agonist	5.14	0.5%	P35408
PTGIR	IP receptor	Agonist	7.41	0.2%	P43119

Bioactivity

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

Target pathways

Aggregated over 3 target gene(s): PTGER3, PTGER4, PTGIR.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
Prostanoid ligand receptors	3	PTGER3, PTGER4, PTGIR
G alpha (s) signalling events	2	PTGER4, PTGIR
Prostacyclin signalling through prostacyclin receptor	1	PTGIR
G alpha (i) signalling events	1	PTGER3

Dominant GO biological processes

GO term	Targets
inflammatory response	3
G protein-coupled receptor signaling pathway	3
adenylate cyclase-activating G protein-coupled receptor signaling pathway	3
positive regulation of cytosolic calcium ion concentration	3
signal transduction	3
phospholipase C-activating G protein-coupled receptor signaling pathway	1
cell death	1
intestine smooth muscle contraction	1
positive regulation of fever generation	1
negative regulation of gastric acid secretion	1
negative regulation of cytokine production	1
positive regulation of cytokine production	1
immune response	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1

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
thrombotic disease	2	MONDO:0000831	HP:0004419
chronic kidney disease	2	MONDO:0005300	EFO:0003884

Clinical trials

Total trials: 10.

Phase distribution

Phase	Trials
PHASE2	5
PHASE3	2
PHASE4	1
PHASE1	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02786979	PHASE4	TERMINATED	Efficacy and Safety of Dorner Tablets and Aspirin for Prevention of Arteriosclerosis Progress in Type 2 Diabetes Mellitus Patients
NCT01458236	PHASE3	WITHDRAWN	A Multinational, Multicenter, Study to Assess the Efficacy and Safety of BPS-314d-MR in Subjects With Pulmonary Arterial Hypertension Currently Receiving Treatment With an Endothelin Receptor Antagonist and/or a Phosphodiesterase-5 Inhibitor
NCT01908699	PHASE3	COMPLETED	Beraprost-314d Added-on to Tyvaso® (BEAT)
NCT00781885	PHASE2	COMPLETED	A Multi-Center, Open-Label, Multiple Dose, Dose Finding Study Exploring the Safety and Tolerability of Beraprost Sodium Modified Release in PAH Patients
NCT00792571	PHASE2	COMPLETED	An Open-Label Extension of BPS-MR-PAH-201 in Pulmonary Arterial Hypertension (PAH) Patients
NCT00989963	PHASE2	COMPLETED	Dose-response Study of the Safety and Efficacy of Beraprost Sodium Modified Release (BPS-MR) in Patients With Pulmonary Arterial Hypertension (PAH)
NCT00990314	PHASE2	COMPLETED	Extension of BPS-MR-PAH-203 in Pulmonary Arterial Hypertension (PAH) Patients
NCT02480751	PHASE2	COMPLETED	TRK-100STP PhaseII Clinical Study -Chronic Renal Failure (Primary Glomerular Disease/Nephrosclerosis)
NCT01443429	PHASE1	COMPLETED	A Pharmacokinetic Study of TRK-100STP in Japanese Patients With Renal Impairment
NCT03142360	Not specified	UNKNOWN	Effect of Beraprost Sodium (Berasil) on Hemodialysis

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.

25 molecules share ≥1 primary target. Top 25 by shared-target count:

Molecule	Source	Status	Shared targets
DINOPROST	ChEMBL + PubChem	Phase 4 (approved)	PTGER3, PTGER4, PTGIR
DINOPROSTONE	ChEMBL + PubChem	Phase 4 (approved)	PTGER3, PTGER4, PTGIR
RALINEPAG	ChEMBL	Phase 3	PTGER3, PTGER4, PTGIR
Grapiprant	ChEMBL + PubChem	Phase 2 (approved)	PTGER3, PTGER4, PTGIR
ILOPROST	ChEMBL + PubChem	Phase 4 (approved)	PTGER3, PTGIR
LAROPIPRANT	ChEMBL	Phase 4 (approved)	PTGER3, PTGIR
Omidenepag	ChEMBL + PubChem	Phase 2 (approved)	PTGER3, PTGER4
Belzutifan	PubChem	Approved	PTGER3, PTGIR
omidenepag isopropyl	PubChem	Approved	PTGER3, PTGER4
ALPROSTADIL	ChEMBL + PubChem	Phase 4 (approved)	PTGIR
TREPROSTINIL	ChEMBL + PubChem	Phase 4 (approved)	PTGIR
SELEXIPAG	ChEMBL	Phase 4 (approved)	PTGIR
SEPETAPROST	ChEMBL	Phase 3	PTGER3
TIMAPIPRANT	ChEMBL	Phase 3	PTGIR
BGC-20-1531	ChEMBL	Phase 2	PTGER4
BGC-20-1531 FREE BASE	ChEMBL	Phase 2	PTGER4
BMS-986310	ChEMBL	Phase 2	PTGER4
BUTAPROST	ChEMBL	Phase 2	PTGIR
CLOPROSTENOL	ChEMBL	Phase 2	PTGER3
FLUPROSTENOL	ChEMBL	Phase 2	PTGER3
LASELIPAG	ChEMBL	Phase 2	PTGIR
PALUPIPRANT	ChEMBL	Phase 2	PTGER4
epoprostenol	PubChem	Approved	PTGIR
Indomethacin	PubChem	Approved	PTGIR
Yohimbine	PubChem	Approved	PTGIR