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 114.22 27.80 39 993 49016 63438974
Abdominal pain 75.67 27.80 51 981 293405 63194585
Sphincter of Oddi dysfunction 63.39 27.80 10 1022 392 63487598
Abdominal pain upper 50.91 27.80 35 997 206409 63281581
Contraindicated product prescribed 45.38 27.80 9 1023 1316 63486674
Constipation 43.68 27.80 33 999 224910 63263080
Pancreatitis acute 38.43 27.80 15 1017 27151 63460839
Diarrhoea 30.89 27.80 47 985 715319 62772671

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 120.88 34.59 41 917 68534 79674896
Sphincter of Oddi dysfunction 65.67 34.59 10 948 423 79743007
Abdominal pain 57.83 34.59 43 915 389526 79353904
Abdominal pain upper 40.63 34.59 28 930 223791 79519639
Constipation 34.75 34.59 28 930 283022 79460408

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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 ABBVIE 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 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

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
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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Viberzi HUMAN PRESCRIPTION DRUG LABEL 1 61874-075 TABLET, FILM COATED 75 mg ORAL NDA 35 sections
Viberzi HUMAN PRESCRIPTION DRUG LABEL 1 61874-075 TABLET, FILM COATED 75 mg ORAL NDA 35 sections
Viberzi HUMAN PRESCRIPTION DRUG LABEL 1 61874-100 TABLET, FILM COATED 100 mg ORAL NDA 35 sections
Viberzi HUMAN PRESCRIPTION DRUG LABEL 1 61874-100 TABLET, FILM COATED 100 mg ORAL NDA 35 sections