Resatorvid

Summary

Resatorvid (CHEMBL225157) is a phase-3 clinical-stage small molecule targeting TLR4; indicated across 2 conditions.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (TLR4)
• Indications: 2 conditions
• Clinical trials: 4
• Chemistry: 361.8 Da · C15H17ClFNO4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL225157
Name	Resatorvid
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	11703255
Molecular formula	C15H17ClFNO4S
Molecular weight	361.8
InChIKey	LEEIJTHMHDMWLJ-CQSZACIVSA-N

SMILES: CCOC(=O)C1=CCCC[C@H]1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl

IUPAC name: ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate

Also known as: Cli-095, Resatorvid, Tak-242, RESATORVID, TAK-242 S enantiomer

Parent form; salt/anhydrous children: CHEMBL3527013

Patent coverage: 215 distinct patent families (420 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 412 (98%) 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
TLR4	TLR4	Antagonist		0%	O00206

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Toll-like receptor 4, Toll-like receptor 4.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q9QUK6	8.89	IC50	1.3	nM	CHEMBL_ACT_25535230
Q9QUK6	8.74	IC50	1.8	nM	CHEMBL_ACT_25535228
Q9QUK6	8.72	IC50	1.9	nM	CHEMBL_ACT_25535229
Q9QUK6	8.24	IC50	5.7	nM	CHEMBL_ACT_16519811
TLR4	7.33	IC50	47	nM	CHEMBL_ACT_29127063
TLR4	7.22	IC50	60	nM	CHEMBL_ACT_29127085
TLR4	6.17	IC50	680	nM	CHEMBL_ACT_18571503

Target pathways

Aggregated over 1 target gene(s): TLR4.

Top Reactome pathways

18 total, by targets touching each:

Pathway	Targets	Genes
ER-Phagosome pathway	1	TLR4
Caspase activation via Death Receptors in the presence of ligand	1	TLR4
Toll Like Receptor 4 (TLR4) Cascade	1	TLR4
MyD88:MAL(TIRAP) cascade initiated on plasma membrane	1	TLR4
MyD88-independent TLR4 cascade	1	TLR4
TRIF-mediated programmed cell death	1	TLR4
MyD88 deficiency (TLR2/4)	1	TLR4
IRAK4 deficiency (TLR2/4)	1	TLR4
Regulation of TLR by endogenous ligand	1	TLR4
Activation of IRF3, IRF7 mediated by TBK1, IKKε (IKBKE)	1	TLR4
IKK complex recruitment mediated by RIP1	1	TLR4
TRAF6-mediated induction of TAK1 complex within TLR4 complex	1	TLR4
Heme signaling	1	TLR4
IRAK2 mediated activation of TAK1 complex upon TLR7/8 or 9 stimulation	1	TLR4
Respiratory syncytial virus (RSV) attachment and entry	1	TLR4
Regulation of TBK1, IKKε (IKBKE)-mediated activation of IRF3, IRF7	1	TLR4
RSV-host interactions	1	TLR4
Dengue Virus-Host Interactions	1	TLR4

Dominant GO biological processes

GO term	Targets
toll-like receptor signaling pathway	1
wound healing involved in inflammatory response	1
B cell proliferation involved in immune response	1
nitric oxide production involved in inflammatory response	1
regulation of dendritic cell cytokine production	1
MyD88-dependent toll-like receptor signaling pathway	1
growth plate cartilage morphogenesis	1
nitric oxide biosynthetic process	1
phagocytosis	1
inflammatory response	1
immune response	1
JNK cascade	1
gene expression	1
positive regulation of platelet activation	1
positive regulation of gene expression	1

Indications & clinical

Indications

2 indications (0 at ChEMBL trial phase 4).

The 2 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE3	2
PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00143611	PHASE3	COMPLETED	Efficacy & Safety of Resatorvid in Adults With Severe Sepsis
NCT00633477	PHASE3	TERMINATED	Efficacy and Safety of Resatorvid in Patients With Sepsis-induced Cardiovascular and Respiratory Failure
NCT06890039	PHASE2	NOT_YET_RECRUITING	A-TANGO Phase 2 Study
NCT04620148	PHASE2	UNKNOWN	TAK-242 in Patients With Acute Alcoholic Hepatitis

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.

5 molecules share ≥1 primary target. Top 5 by shared-target count:

Molecule	Source	Status	Shared targets
CARVEDILOL	ChEMBL + PubChem	Phase 4 (approved)	TLR4
METHOTREXATE	ChEMBL + PubChem	Phase 4 (approved)	TLR4
POLYMYXIN B	ChEMBL	Phase 4 (approved)	TLR4
ERITORAN	ChEMBL	Phase 3	TLR4
ERITORAN TETRASODIUM	ChEMBL	Phase 3	TLR4