Eluxadoline

Summary

Eluxadoline (CHEMBL2159122) is an approved small-molecule μ-opioid receptor agonist (ATC A07DA06) targeting OPRD1 and OPRM1; indicated across 2 conditions including irritable bowel syndrome and diarrheal disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A07DA06
• Targets: 2 (OPRD1, OPRM1)
• Indications: 2 conditions
• Clinical trials: 9
• Chemistry: 569.6 Da · C32H35N5O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2159122
Name	Eluxadoline
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	11250029
ChEBI	CHEBI:85980
ATC	A07DA06
Molecular formula	C32H35N5O5
Molecular weight	569.6
InChIKey	QFNHIDANIVGXPE-FNZWTVRRSA-N

SMILES: CC1=CC(=CC(=C1C[C@@H](C(=O)N(CC2=CC(=C(C=C2)OC)C(=O)O)[C@@H](C)C3=NC=C(N3)C4=CC=CC=C4)N)C)C(=O)N

IUPAC name: 5-[[[(2S)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)propanoyl]-[(1S)-1-(5-phenyl-1H-imidazol-2-yl)ethyl]amino]methyl]-2-methoxybenzoic acid

ChEBI definition: An amino acid amide obtained by the formal condensation of the carboxy group of 4-carbamoyl-2,6-dimethyl-L-phenylalanine with the secondary amino group of 2-methoxy-5-({[(1S)-1-(4-phenylimidazol-2-yl)ethyl]amino}methyl)benzoic acid. It has mixed opioid receptor activity and is used for treatment of irritable bowel syndrome with diarrhoea.

Pharmacological roles (ChEBI): μ-opioid receptor agonist, δ-opioid receptor antagonist, κ-opioid receptor agonist, gastrointestinal drug.

Also known as: Eluxadolina, Eluxadoline, JNJ-27018966, Truberzi, Viberzi, ELUXADOLINE

Patent coverage: 191 distinct patent families (416 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 345 (83%) 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
OPRD1	δ receptor	Antagonist	8.89	0.2%	P41143
OPRM1	μ receptor	Agonist	8.77	0%	P35372

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Mu-type opioid receptor, Delta-type opioid receptor, Mu-type opioid receptor, Kappa-type opioid receptor.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 5 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P33535	9.05	Ki	0.9	nM	CHEMBL_ACT_12067008
OPRM1	9	EC50	1	nM	CHEMBL_ACT_12067920
P33533	8.89	Ki	1.3	nM	CHEMBL_ACT_12067941
P41144	7.26	Ki	55	nM	CHEMBL_ACT_12067034
P41144	5.8	EC50	1600	nM	CHEMBL_ACT_12067032

Target pathways

Aggregated over 2 target gene(s): OPRD1, OPRM1.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Peptide ligand-binding receptors	2	OPRD1, OPRM1
G alpha (i) signalling events	2	OPRD1, OPRM1
Interleukin-4 and Interleukin-13 signaling	2	OPRD1, OPRM1
Opioid Signalling	1	OPRM1
G-protein activation	1	OPRM1
MECP2 regulates neuronal receptors and channels	1	OPRM1

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	2
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	2
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	2
phospholipase C-activating G protein-coupled receptor signaling pathway	2
neuropeptide signaling pathway	2
G protein-coupled opioid receptor signaling pathway	2
signal transduction	2
immune response	1
adult locomotory behavior	1
negative regulation of gene expression	1
negative regulation of protein-containing complex assembly	1
response to nicotine	1
eating behavior	1
response to ethanol	1
regulation of mitochondrial membrane potential	1

Indications & clinical

Indications

2 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
irritable bowel syndrome	4	MONDO:0005052	EFO:0000555
diarrheal disease	4	MONDO:0001673	MONDO:0001673

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE3	3
PHASE2	3
PHASE4	2
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02959983	PHASE4	COMPLETED	Efficacy of Eluxadoline in the Treatment of Irritable Bowel Syndrome With Diarrhea in Patients With Inadequate Control of Symptoms With Prior Loperamide Use
NCT03441581	PHASE4	COMPLETED	Eluxadoline Bile Acid Malabsorption (BAM) Study
NCT04880876	PHASE3	ENROLLING_BY_INVITATION	A Study Evaluating Oral Eluxadoline Administered to Pediatric Participants With Irritable Bowel Syndrome With Diarrhea (IBS-D)
NCT01553591	PHASE3	COMPLETED	Efficacy, Safety, and Tolerability of Eluxadoline in the Treatment of Participants With Diarrhea-Predominant Irritable Bowel Syndrome (IBS-d)
NCT01553747	PHASE3	COMPLETED	Efficacy, Safety, and Tolerability of Eluxadoline in the Treatment of Participants With Diarrhea-Predominant Irritable Bowel Syndrome (IBS-d)
NCT04313088	PHASE2/PHASE3	WITHDRAWN	Investigation of Eluxadoline for Diabetic Diarrhea
NCT03339128	PHASE2	RECRUITING	Study to Explore the Therapeutic Effect of Eluxadoline in Treating Irritable Bowel Syndrome With Diarrhea in Children
NCT01130272	PHASE2	COMPLETED	Efficacy, Safety, and Tolerability of JNJ-27018966 (Eluxadoline) in the Treatment of Irritable Bowel Syndrome With Diarrhea
NCT03489265	PHASE2	WITHDRAWN	Effects of Eluxadoline (Viberzi®) 100 mg Twice Daily on Diarrhea-Associated Fecal Incontinence

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.

448 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
PROPOXYPHENE	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
TAFAMIDIS	ChEMBL + PubChem	Phase 4 (approved)	OPRD1, OPRM1
ALFENTANIL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ALVIMOPAN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
AMIODARONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
AMLODIPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
AMOXAPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
BENZTROPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
BUPRENORPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
BUTORPHANOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CANNABIDIOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CINNARIZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
CODEINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ECONAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
FENTANYL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
HYDROCODONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
HYDROMORPHONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
LANSOPRAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
LEVORPHANOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
LOPERAMIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
LOXAPINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
MEPERIDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
METHADONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
METHYLNALTREXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
METHYLNALTREXONE BROMIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
MICONAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
MONTELUKAST	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
MORPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NAFTOPIDIL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALBUPHINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALDEMEDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALFURAFINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALMEFENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALOXEGOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALOXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NALTREXONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
NELFINAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
OLICERIDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
OXICONAZOLE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
OXYCODONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
OXYMORPHONE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PACLITAXEL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PALBOCICLIB	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PAROXETINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PASIREOTIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PENTAZOCINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PERHEXILINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PHENOXYBENZAMINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
PIMOZIDE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
RALOXIFENE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
RIFAMPIN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
RIFAXIMIN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
RITONAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ROTIGOTINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
SAMIDORPHAN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
SAQUINAVIR	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
SUNITINIB	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
TAMOXIFEN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
TELMISARTAN	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
TRAMADOL	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ZIMELDINE	ChEMBL	Phase 4 (approved)	OPRD1, OPRM1
ASIMADOLINE	ChEMBL	Phase 3	OPRD1, OPRM1
ATICAPRANT	ChEMBL	Phase 3	OPRD1, OPRM1
CEBRANOPADOL	ChEMBL	Phase 3	OPRD1, OPRM1
NAVACAPRANT	ChEMBL	Phase 3	OPRD1, OPRM1
TIANEPTINE	ChEMBL	Phase 3	OPRD1, OPRM1
TRIMEBUTINE	ChEMBL	Phase 3	OPRD1, OPRM1
AXELOPRAN	ChEMBL	Phase 2	OPRD1, OPRM1
AZD-7268	ChEMBL	Phase 2	OPRD1, OPRM1
BREMAZOCINE	ChEMBL	Phase 2	OPRD1, OPRM1
CARFENTANIL	ChEMBL	Phase 2	OPRD1, OPRM1
CLINAFLOXACIN	ChEMBL	Phase 2	OPRD1, OPRM1
CLOTHIAPINE	ChEMBL	Phase 2	OPRD1, OPRM1
CP-866087	ChEMBL	Phase 2	OPRD1, OPRM1
CYCLAZOCINE	ChEMBL	Phase 2	OPRD1, OPRM1
DIPRENORPHINE	ChEMBL	Phase 2	OPRD1, OPRM1
ETORPHINE	ChEMBL	Phase 2	OPRD1, OPRM1
FLUNARIZINE	ChEMBL	Phase 2	OPRD1, OPRM1
METAZOCINE	ChEMBL	Phase 2	OPRD1, OPRM1
NALORPHINE	ChEMBL	Phase 2	OPRD1, OPRM1
NIGULDIPINE	ChEMBL	Phase 2	OPRD1, OPRM1
ORGANON	ChEMBL	Phase 2	OPRD1, OPRM1
PENFLURIDOL	ChEMBL	Phase 2	OPRD1, OPRM1
SPIRADOLINE	ChEMBL	Phase 2	OPRD1, OPRM1
THIOPROPERAZINE	ChEMBL	Phase 2	OPRD1, OPRM1
Afatinib	PubChem	Approved	OPRD1, OPRM1
Apixaban	PubChem	Approved	OPRD1, OPRM1
Binimetinib	PubChem	Approved	OPRD1, OPRM1
Bosentan	PubChem	Approved	OPRD1, OPRM1