Varespladib Methyl

Summary

Varespladib Methyl (CHEMBL2105659) is a phase-3 clinical-stage small-molecule prodrug; indicated across 3 conditions including acute coronary syndrome and coronary artery disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 3 conditions
• Clinical trials: 7
• Chemistry: 394.4 Da · C22H22N2O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2105659
Name	Varespladib Methyl
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9886917
ChEBI	CHEBI:192805
Molecular formula	C22H22N2O5
Molecular weight	394.4
InChIKey	VJYDOJXJUCJUHL-UHFFFAOYSA-N

SMILES: CCC1=C(C2=C(N1CC3=CC=CC=C3)C=CC=C2OCC(=O)OC)C(=O)C(=O)N

IUPAC name: methyl 2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetate

ChEBI definition: A methyl ester resulting from the formal condensation of the carboxy group of varespladib with methanol. It is a potential therapy for the treatment of snakebite envenomings in which toxicity depends on the action of PLA2s.

Pharmacological roles (ChEBI): prodrug, anti-inflammatory drug, antidote, EC 3.1.1.4 (phospholipase A2) inhibitor.

Also known as: A-002, LY-333013, LY333013, S-3013, Varespladib methyl, Varespladib methyl ester, VARESPLADIB METHYL

Patent coverage: 126 distinct patent families (316 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

No target linkage available.

Bioactivity

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

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 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
acute coronary syndrome	3	MONDO:0005542	EFO:0005672
coronary artery disorder	2	MONDO:0005010	EFO:0001645
kidney disorder	1	MONDO:0005240	EFO:0003086

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE2	4
PHASE1	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01130246	PHASE3	TERMINATED	VISTA-16 Trial: Evaluation of Safety and Efficacy of Short-term A-002 Treatment in Subjects With Acute Coronary Syndrome
NCT00455546	PHASE2	COMPLETED	PLASMA Trial: A Dose-Response Study of A-002 In Subjects With Stable Coronary Artery Disease
NCT00525954	PHASE2	COMPLETED	PLASMA 2 Trial: Examination of Once Daily (QD) Dosing of A-002 In Subjects With Stable Coronary Artery Disease
NCT00743925	PHASE2	COMPLETED	FRANCIS-ACS Trial: A Study of the Safety and Efficacy of A 002 in Subjects With Acute Coronary Syndromes
NCT04996264	PHASE2	COMPLETED	Broad-spectrum Rapid Antidote: Varespladib Oral for Snakebite
NCT01359579	PHASE1	TERMINATED	A Study of the Pharmacokinetics and Safety of Varespladib in Subjects With Normal or Impaired Renal Function
NCT01359605	PHASE1	COMPLETED	Study to Assess the Metabolism and Elimination of [14C]-Labeled Varespladib Methyl in Healthy Male 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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).