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

Stem definition	Drug id	CAS RN
analgesics	5001	864821-90-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.20	g	O

ADMET properties:

None

Approvals:

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Date	Agency	Company	Orphan
May 27, 2015	FDA	FURIEX PHARMA INC
Sept. 19, 2016	EMA	Allergan Pharmaceuticals International Limited

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Male)

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A07DA06	ALIMENTARY TRACT AND METABOLISM ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS ANTIPROPULSIVES Antipropulsives
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
FDA EPC	N0000191867	mu-Opioid Receptor Agonist
FDA MoA	N0000191866	Opioid mu-Receptor Agonists
MeSH PA	D005765	Gastrointestinal Agents

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

Disease	Relation	SNOMED_ID	DOID
Irritable bowel syndrome with diarrhea	indication	197125005

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.68	acidic
pKa2	12.56	acidic
pKa3	13.17	acidic
pKa4	8.27	Basic
pKa5	5.63	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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).
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)
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

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	Ki	8.77	SCIENTIFIC LITERATURE	DRUG LABEL
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN	ANTAGONIST	Ki	8.89	SCIENTIFIC LITERATURE	DRUG LABEL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN	AGONIST	Ki	7.26	SCIENTIFIC LITERATURE
Mu-type opioid receptor	GPCR		OPRM_RAT		Ki	9.05	CHEMBL
Delta-type opioid receptor	GPCR		OPRD_RAT		Ki	8.89	CHEMBL
Kappa-type opioid receptor	GPCR		OPRK_CAVPO	AGONIST	Ki	7.26	DRUG LABEL

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External reference:

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ID	Source
016415	NDDF
11250029	PUBCHEM_CID
1653781	RXNORM
237230	MMSL
31303	MMSL
4035123	VANDF
45TPJ4MBQ1	UNII
716119001	SNOMEDCT_US
763582003	SNOMEDCT_US
7691	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

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