Ralinepag

Summary

Ralinepag (CHEMBL3301604) is a phase-3 clinical-stage small molecule targeting PTGER3; indicated across 1 condition including pulmonary arterial hypertension.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (PTGER3)
• Indications: 1 condition
• Clinical trials: 6
• Chemistry: 431.9 Da · C23H26ClNO5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3301604
Name	Ralinepag
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	44219292
Molecular formula	C23H26ClNO5
Molecular weight	431.9
InChIKey	NPDKXVKJRHPDQT-UHFFFAOYSA-N

SMILES: C1CC(CCC1COCC(=O)O)COC(=O)N(C2=CC=CC=C2)C3=CC=C(C=C3)Cl

IUPAC name: 2-[[4-[[(4-chlorophenyl)-phenylcarbamoyl]oxymethyl]cyclohexyl]methoxy]acetic acid

Also known as: APD-811, APD811, Ralinepag, RALINEPAG

Parent form; salt/anhydrous children: CHEMBL3961431

Patent coverage: 70 distinct patent families (260 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
PTGER3	EP3 receptor	Agonist	6.84	2.6%	P43115

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Prostaglandin E2 receptor EP1 subtype, Prostaglandin E2 receptor EP4 subtype, Prostaglandin E2 receptor EP2 subtype, Prostacyclin receptor, Prostacyclin receptor, Prostaglandin E2 receptor EP3 subtype, Prostaglandin D2 receptor.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 12 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PTGIR	8.57	EC50	2.7	nM	CHEMBL_ACT_16888487
PTGIR	8.52	Ki	3	nM	CHEMBL_ACT_18017709
PTGIR	8.07	EC50	8.5	nM	CHEMBL_ACT_18017525
PTGIR	7.42	IC50	38	nM	CHEMBL_ACT_18017457
P43253	7.12	Ki	76	nM	CHEMBL_ACT_18017727
PTGER3	6.84	Ki	143	nM	CHEMBL_ACT_18017721
P43253	6.28	EC50	530	nM	CHEMBL_ACT_18017570
PTGER2	6.21	Ki	610	nM	CHEMBL_ACT_18017718
PTGER4	6.17	Ki	678	nM	CHEMBL_ACT_18017724
PTGDR	6.07	EC50	850	nM	CHEMBL_ACT_18017506
PTGDR	5.58	Ki	2600	nM	CHEMBL_ACT_18017712
PTGER1	5.02	Ki	9600	nM	CHEMBL_ACT_18017715

Target pathways

Aggregated over 1 target gene(s): PTGER3.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Prostanoid ligand receptors	1	PTGER3
G alpha (i) signalling events	1	PTGER3

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
phospholipase C-activating G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
cell death	1
intestine smooth muscle contraction	1
positive regulation of fever generation	1
negative regulation of gastric acid secretion	1
signal transduction	1

Indications & clinical

Indications

1 indication (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
pulmonary arterial hypertension	3	MONDO:0015924	EFO:0001361

Clinical trials

Total trials: 6.

Phase distribution

Phase	Trials
PHASE3	3
PHASE2	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03683186	PHASE3	ENROLLING_BY_INVITATION	A Study Evaluating the Long-Term Efficacy and Safety of Ralinepag in Subjects With PAH Via an Open-Label Extension
NCT03626688	PHASE3	COMPLETED	A Study Evaluating the Efficacy and Safety of Ralinepag to Improve Treatment Outcomes in PAH Patients
NCT04084678	PHASE3	TERMINATED	A Study of Ralinepag to Evaluate Effects on Exercise Capacity by CPET in Subjects With WHO Group 1 PH
NCT02279160	PHASE2	COMPLETED	Safety and Efficacy of APD811 in Pulmonary Arterial Hypertension
NCT02279745	PHASE2	COMPLETED	Long-term Safety and Efficacy of Ralinepag in Pulmonary Arterial Hypertension
NCT04613999	PHASE1	COMPLETED	A Study of Ralinepag in Healthy Chinese Adult Subjects

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.

11 molecules share ≥1 primary target. Top 11 by shared-target count:

Molecule	Source	Status	Shared targets
DINOPROST	ChEMBL	Phase 4 (approved)	PTGER3
DINOPROSTONE	ChEMBL	Phase 4 (approved)	PTGER3
ILOPROST	ChEMBL	Phase 4 (approved)	PTGER3
LAROPIPRANT	ChEMBL	Phase 4 (approved)	PTGER3
SEPETAPROST	ChEMBL	Phase 3	PTGER3
CLOPROSTENOL	ChEMBL	Phase 2	PTGER3
FLUPROSTENOL	ChEMBL	Phase 2	PTGER3
Belzutifan	PubChem	Approved	PTGER3
Grapiprant	PubChem	Approved	PTGER3
Omidenepag	PubChem	Approved	PTGER3
omidenepag isopropyl	PubChem	Approved	PTGER3