Sepetaprost

Summary

Sepetaprost (CHEMBL4297633) is a phase-3 clinical-stage small molecule targeting PTGFR.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (PTGFR)
• Clinical trials: 3
• Chemistry: 482.6 Da · C26H36F2O6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297633
Name	Sepetaprost
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	50902259
Molecular formula	C26H36F2O6
Molecular weight	482.6
InChIKey	BKVUSNOUTQMSBE-XCMGCKIWSA-N

SMILES: CC(C)OC(=O)CCC[C@H]1CC[C@H]2[C@H](C[C@H]([C@@H]2/C=C/[C@H](COC3=C(C=CC(=C3)F)F)O)O)OC1

IUPAC name: propan-2-yl 4-[(3S,5aR,6R,7R,8aS)-6-[(E,3R)-4-(2,5-difluorophenoxy)-3-hydroxybut-1-enyl]-7-hydroxy-3,4,5,5a,6,7,8,8a-octahydro-2H-cyclopenta[b]oxepin-3-yl]butanoate

Also known as: DE-126, Ono-9054, ONO-9054, Sepetaprost, STN-1012600, STN1012600, SEPETAPROST

Patent coverage: 29 distinct patent families (100 SureChEMBL compound mentions), from 2 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
PTGFR	FP receptor	Agonist	5.52	0%	P43088

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Prostaglandin F2-alpha receptor, Prostaglandin E2 receptor EP3 subtype.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PTGER3	8	EC50	10	nM	CHEMBL_ACT_25033841
PTGFR	5.52	EC50	3030	nM	CHEMBL_ACT_25033843

Target pathways

Aggregated over 1 target gene(s): PTGFR.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Prostanoid ligand receptors	1	PTGFR
G alpha (q) signalling events	1	PTGFR

Dominant GO biological processes

GO term	Targets
inflammatory response	1
G protein-coupled receptor signaling pathway	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
parturition	1
positive regulation of cell population proliferation	1
positive regulation of gene expression	1
response to estradiol	1
response to lipopolysaccharide	1
negative regulation of apoptotic process	1
cellular response to prostaglandin D stimulus	1
signal transduction	1
response to lipid	1

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE1	2
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02083289	PHASE2	COMPLETED	A 28 Day Study of ONO-9054 Ophthalmic Solution in Subjects With Ocular Hypertension (OHT) or Open-angle Glaucoma (OAG)
NCT01508988	PHASE1	COMPLETED	Single Dose Escalation Study of ONO-9054 in Healthy Volunteers
NCT01670266	PHASE1	COMPLETED	Single and Multiple Dose Escalation and Two-sequence Crossover Study of ONO-9054 in Patients With Ocular Hypertension or Mild Open-angle Glaucoma

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.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
DINOPROST	ChEMBL + PubChem	Phase 4 (approved)	PTGFR
DINOPROSTONE	ChEMBL + PubChem	Phase 4 (approved)	PTGFR
LAROPIPRANT	ChEMBL	Phase 4 (approved)	PTGFR
CLOPROSTENOL	ChEMBL + PubChem	Phase 2 (approved)	PTGFR
EBOPIPRANT	ChEMBL	Phase 2	PTGFR
FLUPROSTENOL	ChEMBL	Phase 2	PTGFR
Belzutifan	PubChem	Approved	PTGFR
Bimatoprost	PubChem	Approved	PTGFR
Grapiprant	PubChem	Approved	PTGFR
Latanoprost	PubChem	Approved	PTGFR
Latanoprostene Bunod	PubChem	Approved	PTGFR
Nitroglycerin	PubChem	Approved	PTGFR
Tafluprost	PubChem	Approved	PTGFR