eluxadoline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,PDK1,PDK2,PDK4,PRKDC 15
kinase-selectivity-class AXL,BRAF,EIF2AK3,GRK2,STK33 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 110.02 28.56 39 1114 69787 90557507
Abdominal pain 77.81 28.56 53 1100 395668 90231626
Sphincter of Oddi dysfunction 64.57 28.56 10 1143 446 90626848
Constipation 48.93 28.56 35 1118 280360 90346934
Contraindicated product prescribed 45.76 28.56 9 1144 1613 90625681
Abdominal pain upper 45.74 28.56 36 1117 332638 90294656
Pancreatitis acute 39.55 28.56 15 1138 32100 90595194
Diarrhoea 35.64 28.56 51 1102 939139 89688155

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 116.07 28.62 41 1054 93492 110494712
Sphincter of Oddi dysfunction 64.54 28.62 10 1085 578 110587626
Abdominal pain 58.99 28.62 45 1050 512944 110075260
Abdominal pain upper 36.44 28.62 29 1066 349082 110239122
Constipation 35.81 28.62 29 1066 357757 110230447
Pancreatitis acute 34.06 28.62 15 1080 60259 110527945

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:53784 antispasmodic drug
CHEBI has role CHEBI:55322 μ-opioid receptor agonist
CHEBI has role CHEBI:55324 gastrointestinal drug
CHEBI has role CHEBI:59282 κ-opioid receptor agonist
CHEBI has role CHEBI:59283 δ-opioid receptor antagonist

Related Drugs by ATC class:

A07DA Antipropulsives 5 drugs
difenoxindiphenoxylateloperamideloperamide oxidemorphine

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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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)
100MG VIBERZI ABBVIE N206940 May 27, 2015 RX TABLET ORAL 11484527 March 14, 2033 REDUCTION OF THE FREQUENCY OF ABDOMINAL PAIN AND DIARRHEA, IN AN INFLAMMATORY BOWEL DISEASE WITH DIARRHEA (IBS-D) PATIENT, WITH ELUXADOLINE TWICE DAILY WITH FOOD
75MG VIBERZI ABBVIE N206940 May 27, 2015 RX TABLET ORAL 12097187 March 14, 2033 REDUCTION OF THE FREQUENCY OF ABDOMINAL PAIN AND DIARRHEA, IN AN INFLAMMATORY BOWEL DISEASE WITH DIARRHEA (IBS-D) PATIENT, WITH ELUXADOLINE TWICE DAILY WITH FOOD

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
Kappa-type opioid receptor GPCR AGONIST Ki 7.26 DRUG LABEL
Mu-type opioid receptor GPCR Ki 9.05 CHEMBL
Delta-type opioid receptor GPCR Ki 8.89 CHEMBL

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Viberzi HUMAN PRESCRIPTION DRUG LABEL 1 61874-075 TABLET, FILM COATED 75 mg ORAL NDA 34 sections
Viberzi HUMAN PRESCRIPTION DRUG LABEL 1 61874-100 TABLET, FILM COATED 100 mg ORAL NDA 34 sections