eluxadoline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
analgesics 5001 864821-90-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • truberzi
  • eluxadoline
  • viberzi
  • JNJ-27018966
  • JNJ 27018966
  • MuDelta
Eluxadoline is a mu-opioid receptor agonist; eluxadoline is also a delta opioid receptor antagonist and a kappa opioid receptor agonist. The binding affinities (Ki) of eluxadoline for the human mu and delta opioid receptors are 1.8 nM and 430 nM, respectively. The binding affinity (Ki) of eluxadoline for the human kappa opioid receptor has not been determined; however, the Ki for guinea pig cerebellum kappa opioid receptor is 55 nM. In animals, eluxadoline interacts with opioid receptors in the gut.
  • Molecular weight: 569.66
  • Formula: C32H35N5O5
  • CLOGP: 0.72
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 4
  • TPSA: 164.63
  • ALOGS: -5.33
  • ROTB: 11
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 19, 2016 EMA Allergan Pharmaceuticals International Limited
May 27, 2015 FDA FURIEX PHARMA INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pancreatitis 116.32 33.46 39 860 42575 50561650
Abdominal pain 76.76 33.46 49 850 236179 50368046
Sphincter of Oddi dysfunction 63.34 33.46 10 889 360 50603865
Abdominal pain upper 56.44 33.46 35 864 159274 50444951
Contraindicated product prescribed 49.15 33.46 9 890 788 50603437
Constipation 42.18 33.46 31 868 185677 50418548
Pancreatitis acute 39.07 33.46 15 884 23797 50580428

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pancreatitis 122.69 32.23 40 734 59567 64438391
Sphincter of Oddi dysfunction 66.31 32.23 10 764 397 64497561
Abdominal pain 61.74 32.23 41 733 312334 64185624
Abdominal pain upper 47.06 32.23 28 746 175002 64322956
Pancreatitis acute 36.25 32.23 15 759 42840 64455118
Constipation 33.24 32.23 25 749 229312 64268646

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A07DA06 ALIMENTARY TRACT AND METABOLISM
ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
ANTIPROPULSIVES
Antipropulsives
MeSH PA D005765 Gastrointestinal Agents
FDA MoA N0000191866 Opioid mu-Receptor Agonists
FDA EPC N0000191867 mu-Opioid Receptor Agonist
CHEBI has role CHEBI:55322 mu-opioid agonists
CHEBI has role CHEBI:55324 gastrointestinal drugs
CHEBI has role CHEBI:59282 kappa-opioid receptor agonists
CHEBI has role CHEBI:59283 delta-opioid antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Irritable bowel syndrome with diarrhea indication 197125005




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.68 acidic
pKa2 12.56 acidic
pKa3 13.17 acidic
pKa4 8.27 Basic
pKa5 5.63 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 10213415 March 14, 2025 TREATMENT OF PAIN ASSOCIATED WITH IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE)
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 8344011 March 14, 2025 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 8772325 March 14, 2025 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9205076 March 14, 2025 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 10213415 March 14, 2025 TREATMENT OF PAIN ASSOCIATED WITH IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE)
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 8344011 March 14, 2025 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 8772325 March 14, 2025 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9205076 March 14, 2025 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 8691860 July 7, 2028 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9115091 July 7, 2028 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE)
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9364489 July 7, 2028 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9789125 July 7, 2028 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
100MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9789125 July 7, 2028 TREATMENT OF PAIN ASSOCIATED WITH IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE)
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 8691860 July 7, 2028 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9115091 July 7, 2028 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE)
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9364489 July 7, 2028 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9789125 July 7, 2028 TREATMENT OF IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE).
75MG VIBERZI ALLERGAN HOLDINGS N206940 May 27, 2015 RX TABLET ORAL 9789125 July 7, 2028 TREATMENT OF PAIN ASSOCIATED WITH IRRITABLE BOWEL SYNDROME WITH DIARRHEA (IBS-D) WITH VIBERZI (ELUXADOLINE)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Mu-type opioid receptor GPCR AGONIST Ki 8.77 SCIENTIFIC LITERATURE DRUG LABEL
Delta-type opioid receptor GPCR ANTAGONIST Ki 8.89 SCIENTIFIC LITERATURE DRUG LABEL
Kappa-type opioid receptor GPCR AGONIST Ki 7.26 SCIENTIFIC LITERATURE
Mu-type opioid receptor GPCR Ki 9.05 CHEMBL
Delta-type opioid receptor GPCR Ki 8.89 CHEMBL
Kappa-type opioid receptor GPCR AGONIST Ki 7.26 DRUG LABEL

External reference:

IDSource
D10403 KEGG_DRUG
4035123 VANDF
CHEBI:85980 CHEBI
CHEMBL2159122 ChEMBL_ID
C583636 MESH_SUPPLEMENTAL_RECORD_UI
7691 IUPHAR_LIGAND_ID
9749 INN_ID
864825-13-8 SECONDARY_CAS_RN
DB09272 DRUGBANK_ID
45TPJ4MBQ1 UNII
11250029 PUBCHEM_CID
1653781 RXNORM
237230 MMSL
31303 MMSL
d08401 MMSL
716119001 SNOMEDCT_US
763582003 SNOMEDCT_US
C3712232 UMLSCUI
016415 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Viberzi HUMAN PRESCRIPTION DRUG LABEL 1 61874-075 TABLET, FILM COATED 75 mg ORAL NDA 33 sections
Viberzi HUMAN PRESCRIPTION DRUG LABEL 1 61874-100 TABLET, FILM COATED 100 mg ORAL NDA 33 sections