Asapiprant

Summary

Asapiprant (CHEMBL3545043) is a phase-3 clinical-stage small molecule targeting PTGDR; indicated across 2 conditions including seasonal allergic rhinitis and severe acute respiratory syndrome.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (PTGDR)
• Indications: 2 conditions
• Clinical trials: 2
• Chemistry: 501.6 Da · C24H27N3O7S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3545043
Name	Asapiprant
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	59232326
Molecular formula	C24H27N3O7S
Molecular weight	501.6
InChIKey	ZMZNWNTZRWXTJU-UHFFFAOYSA-N

SMILES: CC(C)OC1=CC=C(C=C1)S(=O)(=O)N2CCN(CC2)C3=CC(=C(C=C3)C4=NC=CO4)OCC(=O)O

IUPAC name: 2-[2-(1,3-oxazol-2-yl)-5-[4-(4-propan-2-yloxyphenyl)sulfonylpiperazin-1-yl]phenoxy]acetic acid

Also known as: Asapiprant, Bge 175, Bge-175, BGE175, S-555739, ASAPIPRANT

Patent coverage: 52 distinct patent families (146 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 127 (87%) 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
PTGDR	DP1 receptor	Antagonist	6.62	0.4%	Q13258

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Prostaglandin D2 receptor.

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
PTGDR	6.62	Ki	240	nM	CHEMBL_ACT_16885837
PTGDR	6.28	IC50	520	nM	CHEMBL_ACT_16885780

Target pathways

Aggregated over 1 target gene(s): PTGDR.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Prostanoid ligand receptors	1	PTGDR
G alpha (s) signalling events	1	PTGDR

Dominant GO biological processes

GO term	Targets
inflammatory response	1
G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
male sex determination	1
sleep	1
mast cell degranulation	1
adenosine metabolic process	1
cellular response to prostaglandin D stimulus	1
signal transduction	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
seasonal allergic rhinitis	2	MONDO:0005324	EFO:0003956
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01651871	PHASE2	COMPLETED	Combination Study Of S-555739/Cetirizine HCl In Adult Patients With Seasonal Allergic Rhinitis
NCT04705597	PHASE2	TERMINATED	Study to Evaluate the Safety, Tolerability, and Efficacy of BGE-175 in Hospitalized Adults With Coronavirus Disease 2019 (COVID-19) That Are Not in Respiratory Failure

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.

16 molecules share ≥1 primary target. Top 16 by shared-target count:

Molecule	Source	Status	Shared targets
DINOPROST	ChEMBL + PubChem	Phase 4 (approved)	PTGDR
ILOPROST	ChEMBL + PubChem	Phase 4 (approved)	PTGDR
LAROPIPRANT	ChEMBL	Phase 4 (approved)	PTGDR
RAMATROBAN	ChEMBL	Phase 4 (approved)	PTGDR
SELEXIPAG	ChEMBL	Phase 4 (approved)	PTGDR
TREPROSTINIL	ChEMBL	Phase 4 (approved)	PTGDR
RALINEPAG	ChEMBL	Phase 3	PTGDR
SETIPIPRANT	ChEMBL	Phase 3	PTGDR
TIMAPIPRANT	ChEMBL	Phase 3	PTGDR
BI-671800	ChEMBL	Phase 2	PTGDR
LASELIPAG	ChEMBL	Phase 2	PTGDR
VIDUPIPRANT	ChEMBL	Phase 2	PTGDR
Alprostadil	PubChem	Approved	PTGDR
Belzutifan	PubChem	Approved	PTGDR
Cloprostenol	PubChem	Approved	PTGDR
dinoprostone	PubChem	Approved	PTGDR