eluxadoline profile

ID Source	ID
PubMed CID	11250029
CHEMBL ID	2159122
CHEBI ID	85980
SCHEMBL ID	12971682
SCHEMBL ID	17950908
MeSH ID	M0588002

Synonym
chebi:85980 ,
unii-45tpj4mbq1
eluxadoline ,
jnj-27018966
viberzi
dea no. 9725
jnj 27018966
eluxadoline [usan:inn]
864821-90-9
truberzi
benzoic acid, 5-((((2s)-2-amino-3-(4-(aminocarbonyl)-2,6-dimethylphenyl)-1-oxopropyl)((1s)-1-(5-phenyl-1h-imidazol-2-yl)ethyl)amino)methyl)-2-methoxy-
45tpj4mbq1 ,
chembl2159122 ,
eluxadoline (usan)
viberzi (tn)
D10403
eluxadoline [orange book]
5-((2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-n-(1-(5-phenyl-1h-imidazol-2-yl)ethyl)propanamido)methyl)-2-methoxybenzoic acid
5-((((2s)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)propanoyl)((1s)-1-(4-phenyl-1h-imidazol-2-yl)ethyl)amino(methyl)-2-methoxybenzoic acid
eluxadoline [nflis-drug]
eluxadoline [mi]
eluxadoline [who-dd]
eluxadoline [usan]
eluxadoline [inn]
5-[[[(2s)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)propanoyl]-[(1s)-1-(4-phenyl-3h-imidazol-2-yl)ethyl]amino]methyl]-2-methoxybenzoic acid
gtpl7691
CS-3855
DTXSID70235589 ,
5-({(4-carbamoyl-2,6-dimethyl-l-phenylalanyl)[(1s)-1-(4-phenyl-1h-imidazol-2-yl)ethyl]amino}methyl)-2-methoxybenzoic acid
SCHEMBL12971682
HY-12247
AC-30329
DB09272
5-(((s)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-n-((s)-1-(5-phenyl-1h-imidazol-2-yl)ethyl)propanamido)methyl)-2-methoxybenzoic acid
jnj27018966
EX-A1169
SCHEMBL17950908
mfcd28386164
NCGC00485958-01
AKOS030632800
FT-0701295
AS-35135
Q20539232
benzoic acid, 5-[[[(2s)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1s)-1-(5-phenyl-1h-imidazol-2-yl)ethyl]amino]methyl]-2-methoxy-
AMY39829
CCG-270093
864821-90-9 (free base)
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
eluxadolina
a07da06
eluxadoline (nflis-drug)
dtxcid50158080
5-(((4-carbamoyl-2,6-dimethyl-l-phenylalanyl)((1s)-1-(4-phenyl-1h-imidazol-2-yl)ethyl)amino)methyl)-2-methoxybenzoic acid
eluxadolinum
5-{[(2s)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-n-[(1s)-1-(5-phenyl-1h-imidazol-2-yl)ethyl]propanamido]methyl}-2-methoxybenzoic acid

Excerpt	Reference	Relevance
"Eluxadoline is a mixed μ-opioid, κ-opioid receptor agonist, and δ-opioid receptor antagonist, approved in the United States for adults with diarrhea-predominant irritable bowel syndrome. "	( An Open-Label Study to Evaluate the Effect of Eluxadoline on the Single-Dose Pharmacokinetics of Midazolam in Healthy Participants. Boinpally, R; Kaczynski, E; McGeeney, D; Weissman, D, 2022)	2.42
"Eluxadoline is a novel medication that was approved in the USA in 2015 for the treatment of diarrhoea-predominant irritable bowel syndrome. "	( Eluxadoline-induced pancreatitis occurring in an adult man without a prior cholecystectomy. Groff, A; Jain, R; Packard, E; Shahid, Z, 2019)	3.4
"Eluxadoline is a novel, locally acting mixed μ- and κ-opioid receptor agonist and δ-receptor antagonist approved by the Food and Drug Administration (FDA) for treatment of adults with IBS-D."	( Update on Eluxadoline for the Treatment of Irritable Bowel Syndrome with Diarrhea: Patient Selection and Perspectives. Liu, R; Staller, K, 2020)	1.68
"Eluxadoline is a novel drug approved for the management of diarrhea predominant irritable bowel syndrome (IBS-D). "	( Eluxadoline in the treatment of diarrhea-predominant irritable bowel syndrome. Özdener, AE; Rivkin, A, 2017)	3.34
"Eluxadoline is a gut-targeting μ and κ opioid receptor agonist and a δ opioid receptor antagonist."	( Update on the Management of Diarrhea-Predominant Irritable Bowel Syndrome: Focus on Rifaximin and Eluxadoline. Rivkin, A; Rybalov, S, 2016)	1.37
"Eluxadoline is a mixed μ-opioid receptor (OR) and κ-OR agonist and δ-OR antagonist, approved for the treatment of irritable bowel syndrome with diarrhea (IBS-D). "	( Safety of Eluxadoline in Patients with Irritable Bowel Syndrome with Diarrhea. Cash, BD; Covington, PS; Dove, LS; Lacy, BE; Schoenfeld, PS, 2017)	2.3
"Eluxadoline is a locally acting mixed μ-opiod and κ-opioid receptor agonist and δ-opioid receptor antagonist."	( Eluxadoline Demonstrates a Lack of Abuse Potential in Phase 2 and 3 Studies of Patients With Irritable Bowel Syndrome With Diarrhea. Cash, BD; Covington, PS; Dove, LS; Fant, RV; Henningfield, JE, 2017)	2.62

Excerpt	Reference	Relevance
"Eluxadoline has been approved in the US, and submissions to other global authorities are being contemplated or planned."	( Eluxadoline: First Global Approval. Garnock-Jones, KP, 2015)	2.58

Excerpt	Reference	Relevance
" Adverse events (AEs) were assessed, with special focus on opioid-related AEs, including suspected sphincter of Oddi spasm (SOS) events."	( Safety of Eluxadoline in Patients with Irritable Bowel Syndrome with Diarrhea. Cash, BD; Covington, PS; Dove, LS; Lacy, BE; Schoenfeld, PS, 2017)	0.86
" Consistent with the known adverse effects of opioid agonists, clinically apparent SOS events were observed in eluxadoline-treated patients."	( Safety of Eluxadoline in Patients with Irritable Bowel Syndrome with Diarrhea. Cash, BD; Covington, PS; Dove, LS; Lacy, BE; Schoenfeld, PS, 2017)	1.07
" Incidence of adverse events during alosetron use was not remarkable and was similar to that previously reported."	( Alosetron versus traditional pharmacotherapy in clinical practice: effects on resource use, health-related quality of life, safety and symptom improvement in women with severe diarrhea-predominant irritable bowel syndrome. Chey, WD; Chuang, E; Earnest, DL; Olden, KW; Paul Nicandro, J; Shringarpure, R, 2019)	0.51
" Rates of adverse events were comparable in both groups (37."	( Efficacy and Safety of Eluxadoline in Patients With Irritable Bowel Syndrome With Diarrhea Who Report Inadequate Symptom Control With Loperamide: RELIEF Phase 4 Study. Brenner, DM; Cash, BD; Elmes, SJR; Gutman, CR; Jo, E; Liu, LWC; Sayuk, GS, 2019)	0.82
"Eluxadoline appears safe and effective for treating IBS-D symptoms in patients with an intact gallbladder reporting inadequate relief with prior loperamide use."	( Efficacy and Safety of Eluxadoline in Patients With Irritable Bowel Syndrome With Diarrhea Who Report Inadequate Symptom Control With Loperamide: RELIEF Phase 4 Study. Brenner, DM; Cash, BD; Elmes, SJR; Gutman, CR; Jo, E; Liu, LWC; Sayuk, GS, 2019)	2.27
" There were no deaths, serious treatment-emergent adverse events, or discontinuations due to adverse events during the study."	( Safety and Efficacy of Eluxadoline in Patients with Irritable Bowel Syndrome-Diarrhea With or Without Bile Acid Diarrhea: Open-Label Study. Boinpally, R; Breen-Lyles, M; Busciglio, I; Camilleri, M; Carrothers, TJ; Maselli, D; Muslin, A; Nord, SL; Vijayvargiya, P, 2022)	1.03
"Eluxadoline is similarly efficacious in the treatment of IBS-D and BAD, and it appears to be safe and efficacious as documented in large clinical trials."	( Safety and Efficacy of Eluxadoline in Patients with Irritable Bowel Syndrome-Diarrhea With or Without Bile Acid Diarrhea: Open-Label Study. Boinpally, R; Breen-Lyles, M; Busciglio, I; Camilleri, M; Carrothers, TJ; Maselli, D; Muslin, A; Nord, SL; Vijayvargiya, P, 2022)	2.47

Excerpt	Reference	Relevance
" The method was applied successfully to a clinical pharmacokinetic study in six healthy South Indian male subjects under fed conditions and the results were authenticated by incurred sample reanalysis."	( High sensitive LC-MS/MS method for estimation of eluxadoline in human plasma and its application to pharmacokinetic study. Dodda, S; Kandhagatla, RN; Makula, A; Polagani, SR, 2019)	0.77
" Primary outcome measures were pharmacokinetic parameters of midazolam and 1-hydroxy-midazolam."	( An Open-Label Study to Evaluate the Effect of Eluxadoline on the Single-Dose Pharmacokinetics of Midazolam in Healthy Participants. Boinpally, R; Kaczynski, E; McGeeney, D; Weissman, D, 2022)	0.98

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" Furthermore, compared to loperamide, which is used to treat non-specific diarrhea, the effects of eluxadoline on GI transit occur over a wider dosage range."	( Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers. Devi, LA; Dove, LS; Fujita, W; Gomes, I; McIntyre, G; Prohaska, D, 2014)	0.91
" To date only a few opioid receptor modulators are currently in use for the treatment of IBS but with dosage limitations due to the early development of severe constipation."	( Eluxadoline for the treatment of diarrhoea-predominant irritable bowel syndrome. Abenavoli, L; Gasbarrini, A; Ianiro, G; Laterza, L; Scarpellini, E; Tack, J, 2016)	1.88

Role	Description
mu-opioid receptor agonist	A compound that exhibits agonist activity at the mu-opioid receptor.
delta-opioid receptor antagonist	Any compound that exhibits antagonist activity at the delta-opioid receptor.
kappa-opioid receptor agonist	A compound that exhibits agonist activity at the kappa-opioid receptor.
gastrointestinal drug	A drug used for its effects on the gastrointestinal system, e.g. controlling gastric acidity, regulating gastrointestinal motility and water flow, and improving digestion.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
imidazoles	A five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
methoxybenzoic acid	Any benzoic acid carrying one or more methoxy substituents.
benzamides
L-phenylalanine derivative	A proteinogenic amino acid derivative resulting from reaction of L-phenylalanine at the amino group or the carboxy group, or from the replacement of any hydrogen of L-phenylalanine by a heteroatom.
amino acid amide	An amide of an amino acid formed formally by conversion of the carboxy group to a carboxamido group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 3A4	Homo sapiens (human)	Ki	0.0550	0.0001	1.4162	9.9000	AID696092
Delta-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0013	0.0000	0.6068	9.2330	AID696086
Mu-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0009	0.0000	0.3845	8.6000	AID696087
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0550	0.0000	0.2018	6.4240	AID696092
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Mu-type opioid receptor	Homo sapiens (human)	EC50 (µMol)	0.0010	0.0000	0.3263	9.4000	AID696089
Delta-type opioid receptor	Homo sapiens (human)	EC50 (µMol)	10.0000	0.0000	0.4332	8.3000	AID696088
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Mu-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
sensory perception	Mu-type opioid receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Mu-type opioid receptor	Homo sapiens (human)
sensory perception of pain	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
behavioral response to ethanol	Mu-type opioid receptor	Homo sapiens (human)
positive regulation of neurogenesis	Mu-type opioid receptor	Homo sapiens (human)
negative regulation of Wnt protein secretion	Mu-type opioid receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Mu-type opioid receptor	Homo sapiens (human)
calcium ion transmembrane transport	Mu-type opioid receptor	Homo sapiens (human)
cellular response to morphine	Mu-type opioid receptor	Homo sapiens (human)
regulation of cellular response to stress	Mu-type opioid receptor	Homo sapiens (human)
regulation of NMDA receptor activity	Mu-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Mu-type opioid receptor	Homo sapiens (human)
immune response	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Delta-type opioid receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
adult locomotory behavior	Delta-type opioid receptor	Homo sapiens (human)
negative regulation of gene expression	Delta-type opioid receptor	Homo sapiens (human)
negative regulation of protein-containing complex assembly	Delta-type opioid receptor	Homo sapiens (human)
positive regulation of CREB transcription factor activity	Delta-type opioid receptor	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Delta-type opioid receptor	Homo sapiens (human)
response to nicotine	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
eating behavior	Delta-type opioid receptor	Homo sapiens (human)
regulation of mitochondrial membrane potential	Delta-type opioid receptor	Homo sapiens (human)
regulation of calcium ion transport	Delta-type opioid receptor	Homo sapiens (human)
cellular response to growth factor stimulus	Delta-type opioid receptor	Homo sapiens (human)
cellular response to hypoxia	Delta-type opioid receptor	Homo sapiens (human)
cellular response to toxic substance	Delta-type opioid receptor	Homo sapiens (human)
neuropeptide signaling pathway	Delta-type opioid receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
G-protein alpha-subunit binding	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled receptor activity	Mu-type opioid receptor	Homo sapiens (human)
beta-endorphin receptor activity	Mu-type opioid receptor	Homo sapiens (human)
voltage-gated calcium channel activity	Mu-type opioid receptor	Homo sapiens (human)
protein binding	Mu-type opioid receptor	Homo sapiens (human)
morphine receptor activity	Mu-type opioid receptor	Homo sapiens (human)
G-protein beta-subunit binding	Mu-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Mu-type opioid receptor	Homo sapiens (human)
G protein-coupled opioid receptor activity	Delta-type opioid receptor	Homo sapiens (human)
protein binding	Delta-type opioid receptor	Homo sapiens (human)
receptor serine/threonine kinase binding	Delta-type opioid receptor	Homo sapiens (human)
G protein-coupled enkephalin receptor activity	Delta-type opioid receptor	Homo sapiens (human)
neuropeptide binding	Delta-type opioid receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
endosome	Mu-type opioid receptor	Homo sapiens (human)
endoplasmic reticulum	Mu-type opioid receptor	Homo sapiens (human)
Golgi apparatus	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Homo sapiens (human)
axon	Mu-type opioid receptor	Homo sapiens (human)
dendrite	Mu-type opioid receptor	Homo sapiens (human)
perikaryon	Mu-type opioid receptor	Homo sapiens (human)
synapse	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Mu-type opioid receptor	Homo sapiens (human)
neuron projection	Mu-type opioid receptor	Homo sapiens (human)
plasma membrane	Delta-type opioid receptor	Homo sapiens (human)
synaptic vesicle membrane	Delta-type opioid receptor	Homo sapiens (human)
dendrite membrane	Delta-type opioid receptor	Homo sapiens (human)
presynaptic membrane	Delta-type opioid receptor	Homo sapiens (human)
axon terminus	Delta-type opioid receptor	Homo sapiens (human)
spine apparatus	Delta-type opioid receptor	Homo sapiens (human)
postsynaptic density membrane	Delta-type opioid receptor	Homo sapiens (human)
neuronal dense core vesicle	Delta-type opioid receptor	Homo sapiens (human)
plasma membrane	Delta-type opioid receptor	Homo sapiens (human)
neuron projection	Delta-type opioid receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID696092	Binding affinity to guinea pig kappa opioid receptor	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID696086	Binding affinity to rat delta opioid receptor	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID696091	Antagonist activity at delta opioid receptor in hamster vas deferens tissue	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID696093	Agonist activity at kappa opioid receptor guinea pig colon tissue	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID696087	Binding affinity to rat mu opioid receptor	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID696089	Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID696088	Agonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID696090	Antagonist activity at delta opioid receptor expressed in CHO-hg cells assessed as inhibition of SNC-80-induced [35S]-GTPgammaS binding	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID1346364	Human mu receptor (Opioid receptors)	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID1346400	Rat mu receptor (Opioid receptors)	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
AID1346406	Rat delta receptor (Opioid receptors)	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	59 (80.82)	24.3611
2020's	14 (19.18)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	11 (14.67%)	5.53%
Reviews	22 (29.33%)	6.00%
Case Studies	3 (4.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	39 (52.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Double Blind, Placebo Controlled, Cross Over Study to Investigate the Effectiveness and Safety of Eluxadoline in the Treatment of Diabetic Diarrhea [NCT04313088]	Phase 2/Phase 3	0 participants (Actual)	Interventional	2022-07-01	Withdrawn(stopped due to This study did not enroll any subjects)
A Phase 4 Multicenter, Multinational, Prospective, Randomized, Placebo-Controlled, Double-Blinded Parallel Group Study to Assess Efficacy of Eluxadoline in the Treatment of Irritable Bowel Syndrome With Diarrhea (IBS-D) in Patients Who Report Inadequate C [NCT02959983]	Phase 4	346 participants (Actual)	Interventional	2016-10-25	Completed
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Dose-Ranging Study to Evaluate the Safety and Efficacy of Eluxadoline in Pediatric Participants (Age 6 to 17 Years) With Irritable Bowel Syndrome With Diarrhea (IBS-D) [NCT03339128]	Phase 2	95 participants (Anticipated)	Interventional	2017-11-15	Recruiting
A Randomized, Double-blind, Placebo-controlled, Parallel Group, Dose Ranging, Multicenter Study to Evaluate the Efficacy, Safety, and Tolerability of JNJ-27018966 in the Treatment of Patients With Irritable Bowel Syndrome With Diarrhea [NCT01130272]	Phase 2	807 participants (Actual)	Interventional	2010-04-28	Completed
3030-401-002: An Open-Label Pilot Study of Eluxadoline in Participants With Irritable Bowel Syndrome With Diarrhea (IBS-D) Who Have Evidence of Bile Acid Malabsorption (BAM) [NCT03441581]	Phase 4	24 participants (Actual)	Interventional	2018-02-23	Completed
A Randomized, Double-blind, Placebo-controlled, Phase 3 Study to Evaluate the Efficacy, Safety, and Tolerability of JNJ-27018966 in the Treatment of Patients With Diarrhea-Predominant Irritable Bowel Syndrome [NCT01553747]	Phase 3	1,146 participants (Actual)	Interventional	2012-05-29	Completed
A Randomized, Double-blind, Placebo-controlled, Phase 3 Study to Evaluate the Efficacy, Safety, and Tolerability of JNJ-27018966 in the Treatment of Patients With Diarrhea-Predominant Irritable Bowel Syndrome [NCT01553591]	Phase 3	1,282 participants (Actual)	Interventional	2012-05-29	Completed
Treatment of Diarrhea-Associated Fecal Incontinence With Eluxadoline [NCT03489265]	Phase 2	0 participants (Actual)	Interventional	2019-04-30	Withdrawn(stopped due to Difficult to recruit severely affected patients with fecal incontinence)
A Phase 3, Long-term Safety Study of Oral Eluxadoline Administered to Pediatric Participants With Irritable Bowel Syndrome With Diarrhea (IBS-D) [NCT04880876]	Phase 3	124 participants (Anticipated)	Interventional	2021-08-13	Enrolling by invitation
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT01130272 (6) [back to overview]	Change From Baseline in the Weekly Pain Scores
NCT01130272 (6) [back to overview]	Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain and Daily Stool Consistency Scores at Week 12
NCT01130272 (6) [back to overview]	Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain and Daily Stool Consistency Scores at Week 4
NCT01130272 (6) [back to overview]	Change From Baseline in the Number of Daily Bowel Movements
NCT01130272 (6) [back to overview]	Change From Baseline in Weekly BSS Scores
NCT01130272 (6) [back to overview]	Percentage of Participants With Response Based on Participants Achieving Prespecified Improvement in Symptoms for at Least 50% of the Time
NCT01553591 (15) [back to overview]	Number of Bowel Incontinence Episodes
NCT01553591 (15) [back to overview]	Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain And Daily Stool Consistency Scores
NCT01553591 (15) [back to overview]	IBS-QoL Total Scores
NCT01553591 (15) [back to overview]	Number of Bowel Incontinence Free Days
NCT01553591 (15) [back to overview]	Change From Baseline in IBS-QoL Total Scores
NCT01553591 (15) [back to overview]	Change From Baseline in Daily Abdominal Discomfort Scores
NCT01553591 (15) [back to overview]	Change From Baseline in Daily Abdominal Bloating Scores
NCT01553591 (15) [back to overview]	Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain And Daily Stool Consistency Scores
NCT01553591 (15) [back to overview]	Percentage of Participants With Irritable Bowel Syndrome - Adequate Relief (IBS-AR) Scale
NCT01553591 (15) [back to overview]	Percentage of Participants Who Were Responders to the Irritable Bowel Syndrome Quality of Life Measure (IBS-QoL) Scale
NCT01553591 (15) [back to overview]	Percentage of Participants Who Were Responders In Irritable Bowel Syndrome, Diarrhea Predominant (IBS-d) Global Symptom Scale by Intervals
NCT01553591 (15) [back to overview]	Percentage of Participants Who Were Responders In Daily Stool Consistency Scores by Intervals
NCT01553591 (15) [back to overview]	Percentage of Participants Who Were Pain Responders In Daily Worst Abdominal Pain Scores by Intervals
NCT01553591 (15) [back to overview]	Number of Urgency Episodes Per Day
NCT01553591 (15) [back to overview]	Number of Bowel Movements Per Day
NCT01553747 (14) [back to overview]	Number of Bowel Incontinence Free Days
NCT01553747 (14) [back to overview]	Number of Urgency Episodes Per Day
NCT01553747 (14) [back to overview]	Percentage of Participants Who Were Pain Responders In Daily Worst Abdominal Pain Scores by Intervals
NCT01553747 (14) [back to overview]	Percentage of Participants Who Were Responders In Daily Stool Consistency Scores by Intervals
NCT01553747 (14) [back to overview]	Percentage of Participants Who Were Responders In Irritable Bowel Syndrome, Diarrhea Predominant (IBS-d) Global Symptom Scale by Intervals
NCT01553747 (14) [back to overview]	Percentage of Participants Who Were Responders to the Irritable Bowel Syndrome Quality of Life Measure (IBS-QoL) Scale
NCT01553747 (14) [back to overview]	Percentage of Participants With Irritable Bowel Syndrome - Adequate Relief (IBS-AR) Scale
NCT01553747 (14) [back to overview]	Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain and Daily Stool Consistency Scores
NCT01553747 (14) [back to overview]	Number of Bowel Movements Per Day
NCT01553747 (14) [back to overview]	Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain and Daily Stool Consistency Scores
NCT01553747 (14) [back to overview]	Change From Baseline in Daily Abdominal Bloating Scores
NCT01553747 (14) [back to overview]	Change From Baseline in Daily Abdominal Discomfort Scores
NCT01553747 (14) [back to overview]	Change From Baseline in IBS-QoL Total Scores
NCT01553747 (14) [back to overview]	Number of Bowel Incontinence Episodes
NCT02959983 (4) [back to overview]	Percentage of Monthly Composite Responders
NCT02959983 (4) [back to overview]	Percentage of Pain Responders
NCT02959983 (4) [back to overview]	Percentage of Stool Consistency Responders
NCT02959983 (4) [back to overview]	Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain And Daily Stool Consistency Scores
NCT03441581 (19) [back to overview]	AUC: Area Under the Concentration-time Curve During the Dosing Interval for Eluxadoline
NCT03441581 (19) [back to overview]	CL/F: Apparent Total Clearance of the Drug From Plasma After Oral Administration for Eluxadoline
NCT03441581 (19) [back to overview]	Cmax: Maximum Concentration for Eluxadoline
NCT03441581 (19) [back to overview]	Cmin: Minimum Concentration for Eluxadoline
NCT03441581 (19) [back to overview]	Change From Baseline in Average Bristol Stool Form Scale (BSFS) Score Over 4 Weeks of Treatment Period
NCT03441581 (19) [back to overview]	Change From Baseline in the 4-week Average of Daily Worst Abdominal Pain Scores During the Treatment Period
NCT03441581 (19) [back to overview]	Change From Baseline in the 4-week Average of Daily Bowel Movement Frequency During the Treatment Period
NCT03441581 (19) [back to overview]	Change From Baseline in the 4-week Average of Daily Bloating Scores During the Treatment Period
NCT03441581 (19) [back to overview]	Change From Baseline in the 4-week Average Number of Daily Urgent Bowel Movements During the Treatment Period
NCT03441581 (19) [back to overview]	Change From Baseline in Irritable Bowel Syndrome Quality of Life (IBS-QOL) Total Score at the End of the Treatment Period
NCT03441581 (19) [back to overview]	Change From Baseline in Fasting Serum 7α-hydroxy-4-cholesten-3-one (7αC4) Levels at the End of the Treatment Period
NCT03441581 (19) [back to overview]	Vc/F: Apparent Volume of Distribution for Eluxadoline
NCT03441581 (19) [back to overview]	Tmax: Time to Cmax for Eluxadoline
NCT03441581 (19) [back to overview]	t1/2: Half-Life for Eluxadoline
NCT03441581 (19) [back to overview]	Percentage of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT03441581 (19) [back to overview]	Percentage of Participants With Any Fecal Incontinence During the Treatment Period
NCT03441581 (19) [back to overview]	Number of Participants Who Experienced Potentially Clinically Significant Change in Vital Signs
NCT03441581 (19) [back to overview]	Number of Participants Who Experienced Potentially Clinically Significant Change in Laboratory Tests
NCT03441581 (19) [back to overview]	Number of Participants Who Experienced Clinically Significant Change From Baseline in General Physical Condition as Measured Through General Physical Exam

Change From Baseline in the Weekly Pain Scores

The participant recorded their worst daily pain score in a diary using an 11-point scale where: 0=no pain to 10=worst pain imaginable. The daily scores over the previous week were averaged. A negative change from Baseline indicates improvement. (NCT01130272)
Timeframe: Baseline (Week Prior to Randomization) to Weeks 4, 8, and 12

,,,,

Intervention	scores on a scale (Mean)
	Baseline	Change from Baseline to Week 4	Change from Baseline to Week 8	Change from Baseline to Week 12
Eluxadoline 100 mg	6.11	-2.33	-2.81	-3.25
Eluxadoline 200 mg	5.78	-2.20	-2.58	-2.96
Eluxadoline 25 mg	5.91	-2.11	-2.54	-2.57
Eluxadoline 5 mg	5.75	-1.76	-2.35	-2.50
Placebo	5.87	-2.09	-2.54	-2.65

Intervention	percentage of participants (Number)
Eluxadoline 5 mg	8.6
Eluxadoline 25 mg	13.2
Eluxadoline 100 mg	20.2
Eluxadoline 200 mg	15.0
Placebo	11.3

Intervention	percentage of participants (Number)
Eluxadoline 5 mg	12.4
Eluxadoline 25 mg	12.0
Eluxadoline 100 mg	11.0
Eluxadoline 200 mg	13.8
Placebo	5.7

Intervention	percentage of participants (Number)
	Weeks 1-12	Weeks 1-4	Weeks 5-8	Weeks 9-12
Eluxadoline 100 mg	29.7	24.9	43.0	49.1
Eluxadoline 200 mg	30.6	32.7	39.3	50.7
Eluxadoline 25 mg	20.2	21.0	34.4	34.4
Eluxadoline 5 mg	16.5	18.0	29.3	29.7
Placebo	19.0	20.0	30.3	31.0

Intervention	incontinence episodes (Mean)
	Week 4	Week 12	Week 26
Eluxadoline 100 mg	0.72	0.71	0.58
Eluxadoline 75 mg	0.74	0.63	0.46
Placebo	0.93	0.94	0.69

Intervention	score on a scale (Mean)
	Responders at Week 4	Responders at Week 8	Responders at Week 12	Responders at Week 18	Responders at Week 26	Responders at Week 36	Responders at Week 44	Responders at Week 52/EOT
Eluxadoline 100 mg	64.34	67.73	68.93	70.05	71.34	72.37	72.15	71.02
Eluxadoline 75 mg	62.37	66.22	66.80	68.75	70.74	70.53	70.30	68.85
Placebo	57.13	59.46	61.72	63.60	64.83	66.47	65.59	63.93

Intervention	score on a scale (Mean)
	Change at Week 4	Change at Week 8	Change at Week 12	Change at Week 18	Change at Week 26	Change at Week 36	Change at Week 44	Change at Week 52/EOT
Eluxadoline 100 mg	17.86	21.08	22.76	24.18	25.80	27.18	26.64	25.86
Eluxadoline 75 mg	16.49	19.88	20.26	23.09	25.28	25.37	25.13	23.30
Placebo	13.25	15.76	17.76	19.80	20.62	22.64	21.77	20.66

Intervention	percentage of participants (Number)
	Responders during Weeks 1-12	Responders during Weeks 1-26
Eluxadoline 100 mg	54.2	49.5
Eluxadoline 75 mg	52.9	45.7
Placebo	43.8	40.0

Intervention	percentage of participants (Number)
	Responders during Weeks 1-12	Responders during Weeks 1-26	Responders during Weeks 1-4	Responders during Weeks 5-8	Responders during Weeks 9-12	Responders during Weeks 13-16	Responders during Weeks 17-20	Responders during Weeks 21-24
Eluxadoline 100 mg	34.7	37.1	31.9	38.7	36.6	35.9	36.4	35.2
Eluxadoline 75 mg	35.1	36.3	32.6	37.0	35.6	35.8	37.5	36.8
Placebo	28.8	32.3	26.9	32.8	34.0	35.4	33.3	29.5

Intervention	Percentage of Participants (Number)
	Overall Weeks 1 to 12	Weeks 1 to 4	Weeks 5 to 8	Weeks 9 to 12
Eluxadoline	43.6	30.2	45.9	44.8
Placebo	31.0	25.9	31.6	35.1

Intervention	nanogram* hour/milliliter (ng*h/mL) (Mean)
Eluxadoline 100 mg With BAM	9.22
Eluxadoline 100 mg Without BAM	7.75

Intervention	days (Mean)
	Week 4	Week 12	Week 26
Eluxadoline 100 mg	4.95	4.79	4.35
Eluxadoline 75 mg	4.83	4.96	4.39
Placebo	4.63	4.64	4.00

Intervention	liter/hour (L/h) (Mean)
Eluxadoline 100 mg With BAM	20236
Eluxadoline 100 mg Without BAM	21901

Intervention	ng/mL (Mean)
Eluxadoline 100 mg With BAM	1.40
Eluxadoline 100 mg Without BAM	0.91

Intervention	ng/mL (Mean)
Eluxadoline 100 mg With BAM	0.39
Eluxadoline 100 mg Without BAM	0.42

Intervention	score on a scale (Mean)
	Baseline	Change From Baseline at Week 4
Eluxadoline 100 mg With BAM	5.89	-1.25
Eluxadoline 100 mg Without BAM	5.34	-1.09

Intervention	nanogram/milliliter (ng/mL) (Mean)
	Baseline	Change from Baseline at End of Treatment
Eluxadoline 100 mg With BAM	42.95	-5.59
Eluxadoline 100 mg Without BAM	30.58	-8.78

Intervention	L (Mean)
Eluxadoline 100 mg With BAM	29432
Eluxadoline 100 mg Without BAM	39799

Intervention	h (Median)
Eluxadoline 100 mg With BAM	30.5
Eluxadoline 100 mg Without BAM	35.2

Intervention	percentage of participants (Number)
Eluxadoline 100 mg With BAM	91.7
Eluxadoline 100 mg Without BAM	58.3

Substance	Relationship Strength	Studies	Trials	Classes	Roles
alosetron alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.	11.96	8	0	imidazoles; pyridoindole	antiemetic; gastrointestinal drug; serotonergic antagonist
ebastine [no description available]	3.25	1	0	organic molecular entity
loperamide Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.	9.57	12	2	monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol	anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist
midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.	7.41	1	0	imidazobenzodiazepine; monofluorobenzenes; organochlorine compound	anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative
probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.	3.5	1	1	benzoic acids; sulfonamide	uricosuric drug
phenylalanine Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.	16.34	75	14	amino acid zwitterion; erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid; phenylalanine; proteinogenic amino acid	algal metabolite; EC 3.1.3.1 (alkaline phosphatase) inhibitor; Escherichia coli metabolite; human xenobiotic metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	3.25	1	0	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
diphenoxylate Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.. diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin.	4.22	1	0	ethyl ester; nitrile; piperidinecarboxylate ester; tertiary amine	antidiarrhoeal drug
colestipol Colestipol: Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels.. colestipol : A high molecular weight copolymer of diethylenetriamine and epichlorohydrin (hydrochloride), with approximately 1 out of 5 amine nitrogens protonated. Due to the highly cross-linked and insoluble nature of the material, no structural formula has been assigned and no specific molecular weight information is available. A basic anion exchange resin, it is used as its hydrochloride for binding bile acids in the intestine, inhibiting their reabsorption.	2.13	1	0
octylonium octylonium: RN given refers to bromide; structure	3.25	1	0	benzamides
ramosetron [no description available]	3.65	2	0	indoles
moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.	3.56	1	1	aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone	antibacterial drug
lubiprostone [no description available]	2.13	1	0
benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.	2.13	1	0
prucalopride prucalopride: a 5-HT4 agonist enterokinetic compound	2.13	1	0	benzamides
morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.	2.17	1	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
naltrexone Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.	3.68	2	0	cyclopropanes; morphinane-like compound; organic heteropentacyclic compound	antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic
methylnaltrexone methylnaltrexone: RN given refers to parent cpd(5alpha)-isomer	3.68	2	0	phenanthrenes
morphinans Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.	3.27	1	0	isoquinoline alkaloid fundamental parent; morphinane alkaloid
ibodutant 6-methylbenzo(b)thiophene-2-carboxylic acid (1-(2-phenyl-((1-(tetrahydropyran-4-ylmethyl)piperidin-4-ylmethyl)carbamoyl)ethylcarbamoyl)cyclophenyl)amide: a tachykinin NK2 receptor antagonist; structure in first source	3.25	1	0
rifamycins [no description available]	7.22	9	0
piperidines Piperidines: A family of hexahydropyridines.	3.25	1	0
naloxegol naloxegol: A peripherally acting opioid receptor antagonist specific for mu-opioid receptors. Used to decrease the constipating effects of opioids.. naloxegol : An organic heteropentacyclic compound that is naloxone in which the keto group is replaced by a PEG moiety. Used for treatment of opioid-induced constipation.	3.27	1	0	aromatic ether; organic heteropentacyclic compound; phenols; polyether; tertiary alcohol	cathartic; mu-opioid receptor antagonist
plecanatide plecanatide: A uroguanylin analog and guanylate cyclase (GC-C receptor) agonist that activates receptors on gut epithelial cells to maintain barrier function, mucus production, and suppress inflammation. It is used in the treatment of chronic idiopathic constipation and other gastrointestinal disorders.	2.13	1	0
cyclosporine Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).	3.5	1	1
tegaserod tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source	2.13	1	0	carboxamidine; guanidines; hydrazines; indoles	gastrointestinal drug; serotonergic agonist
cholestyramine resin Cholestyramine Resin: A strongly basic anion exchange resin whose main constituent is polystyrene trimethylbenzylammonium Cl(-) anion.	2.13	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Colitis, Mucous [description not available]	0	17.19	78	19
Diarrhea An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.	0	16.99	71	19
Irritable Bowel Syndrome A disorder with chronic or recurrent colonic symptoms without a clearcut etiology. This condition is characterized by chronic or recurrent ABDOMINAL PAIN, bloating, MUCUS in FECES, and an erratic disturbance of DEFECATION.	1	19.19	78	19
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.58	2	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.69	2	0
Acute Edematous Pancreatitis [description not available]	0	11.52	20	10
Colicky Pain [description not available]	0	12.33	17	12
Pancreatitis INFLAMMATION of the PANCREAS. Pancreatitis is classified as acute unless there are computed tomographic or endoscopic retrograde cholangiopancreatographic findings of CHRONIC PANCREATITIS (International Symposium on Acute Pancreatitis, Atlanta, 1992). The two most common forms of acute pancreatitis are ALCOHOLIC PANCREATITIS and gallstone pancreatitis.	0	11.52	20	10
Abdominal Pain Sensation of discomfort, distress, or agony in the abdominal region.	0	17.33	17	12
ANS (Autonomic Nervous System) Diseases [description not available]	0	4.04	1	0
Bacterial Overgrowth Syndrome [description not available]	0	4.04	1	0
Celiac Sprue [description not available]	0	4.92	2	0
Autoimmune Diabetes [description not available]	0	4.04	1	0
Diabetes Mellitus, Adult-Onset [description not available]	0	4.04	1	0
Asymmetric Diabetic Proximal Motor Neuropathy [description not available]	0	4.04	1	0
Innate Inflammatory Response [description not available]	0	4.04	1	0
Pancreatic Insufficiency [description not available]	0	4.92	2	0
Bowel Diseases, Inflammatory [description not available]	0	5.51	3	0
Celiac Disease A malabsorption syndrome that is precipitated by the ingestion of foods containing GLUTEN, such as wheat, rye, and barley. It is characterized by INFLAMMATION of the SMALL INTESTINE, loss of MICROVILLI structure, failed INTESTINAL ABSORPTION, and MALNUTRITION.	0	4.92	2	0
Diabetes Mellitus, Type 1 A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.	0	4.04	1	0
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	0	4.04	1	0
Diabetic Neuropathies Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325)	0	4.04	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	4.04	1	0
Exocrine Pancreatic Insufficiency A malabsorption condition resulting from greater than 10% reduction in the secretion of pancreatic digestive enzymes (LIPASE; PROTEASES; and AMYLASE) by the EXOCRINE PANCREAS into the DUODENUM. This condition is often associated with CYSTIC FIBROSIS and with chronic PANCREATITIS.	0	4.92	2	0
Inflammatory Bowel Diseases Chronic, non-specific inflammation of the GASTROINTESTINAL TRACT. Etiology may be genetic or environmental. This term includes CROHN DISEASE and ULCERATIVE COLITIS.	0	5.51	3	0
Colonic Inertia Symptom characterized by the passage of stool once a week or less.	0	6.98	8	1
Constipation Infrequent or difficult evacuation of FECES. These symptoms are associated with a variety of causes, including low DIETARY FIBER intake, emotional or nervous disturbances, systemic and structural disorders, drug-induced aggravation, and infections.	0	6.98	8	1
Liver Dysfunction [description not available]	0	2.15	1	0
Liver Diseases Pathological processes of the LIVER.	0	2.15	1	0
Adverse Drug Event [description not available]	0	2.17	1	0
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	2.17	1	0
Gall Bladder Diseases [description not available]	0	2.17	1	0
Acute Disease Disease having a short and relatively severe course.	0	2.17	1	0
Chronic Illness [description not available]	0	3.47	2	0
Hospital-Acquired Condition [description not available]	0	3.12	1	0
Steatorrhea A condition that is characterized by chronic fatty DIARRHEA, a result of abnormal DIGESTION and/or INTESTINAL ABSORPTION of FATS.	0	3.12	1	0
Adenocarcinoma, Basal Cell [description not available]	0	3.12	1	0
Adenoma, Basal Cell [description not available]	0	3.12	1	0
Malabsorption Syndromes General term for a group of MALNUTRITION syndromes caused by failure of normal INTESTINAL ABSORPTION of nutrients.	0	3.12	1	0
Colorectal Cancer [description not available]	0	3.12	1	0
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	0	3.12	1	0
Adenoma A benign epithelial tumor with a glandular organization.	0	3.12	1	0
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	0	3.47	2	0
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	0	3.12	1	0
Visceral Pain Pain originating from internal organs (VISCERA) associated with autonomic phenomena (PALLOR; SWEATING; NAUSEA; and VOMITING). It often becomes a REFERRED PAIN.	0	3.46	2	0
Chemical Dependence [description not available]	0	8.95	17	1
Substance-Related Disorders Disorders related to substance use or abuse.	0	8.95	17	1
Sphincter of Oddi Dysfunction Organic or functional motility disorder involving the SPHINCTER OF ODDI and associated with biliary COLIC. Pathological changes are most often seen in the COMMON BILE DUCT sphincter, and less commonly the PANCREATIC DUCT sphincter.	0	3.53	1	1
Muscle Spasm [description not available]	0	3.53	1	1
Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.	0	3.53	1	1
Spasm An involuntary contraction of a muscle or group of muscles. Spasms may involve SKELETAL MUSCLE or SMOOTH MUSCLE.	0	3.53	1	1

eluxadoline

Cross-References

Synonyms (55)

Research Excerpts

Overview

Effects

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Roles (4)

Drug Classes (5)

Protein Targets (6)

Inhibition Measurements

Activation Measurements

Biological Processes (50)

Molecular Functions (33)

Ceullar Components (19)

Bioassays (16)

Research

Studies (73)

Market Indicators

Research Demand Index: 66.40

Study Types

Clinical Trials (9)

Trial Overview

Trial Outcomes

Change From Baseline in the Weekly Pain Scores

Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain and Daily Stool Consistency Scores at Week 12

Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain and Daily Stool Consistency Scores at Week 4

Change From Baseline in the Number of Daily Bowel Movements

Change From Baseline in Weekly BSS Scores

Percentage of Participants With Response Based on Participants Achieving Prespecified Improvement in Symptoms for at Least 50% of the Time

Number of Bowel Incontinence Episodes

Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain And Daily Stool Consistency Scores

IBS-QoL Total Scores

Number of Bowel Incontinence Free Days

Change From Baseline in IBS-QoL Total Scores

Change From Baseline in Daily Abdominal Discomfort Scores

Change From Baseline in Daily Abdominal Bloating Scores

Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain And Daily Stool Consistency Scores

Percentage of Participants With Irritable Bowel Syndrome - Adequate Relief (IBS-AR) Scale

Percentage of Participants Who Were Responders to the Irritable Bowel Syndrome Quality of Life Measure (IBS-QoL) Scale

Percentage of Participants Who Were Responders In Irritable Bowel Syndrome, Diarrhea Predominant (IBS-d) Global Symptom Scale by Intervals

Percentage of Participants Who Were Responders In Daily Stool Consistency Scores by Intervals

Percentage of Participants Who Were Pain Responders In Daily Worst Abdominal Pain Scores by Intervals

Number of Urgency Episodes Per Day

Number of Bowel Movements Per Day

Number of Bowel Incontinence Free Days

Number of Urgency Episodes Per Day

Percentage of Participants Who Were Pain Responders In Daily Worst Abdominal Pain Scores by Intervals

Percentage of Participants Who Were Responders In Daily Stool Consistency Scores by Intervals

Percentage of Participants Who Were Responders In Irritable Bowel Syndrome, Diarrhea Predominant (IBS-d) Global Symptom Scale by Intervals

Percentage of Participants Who Were Responders to the Irritable Bowel Syndrome Quality of Life Measure (IBS-QoL) Scale

Percentage of Participants With Irritable Bowel Syndrome - Adequate Relief (IBS-AR) Scale

Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain and Daily Stool Consistency Scores

Number of Bowel Movements Per Day

Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain and Daily Stool Consistency Scores

Change From Baseline in Daily Abdominal Bloating Scores

Change From Baseline in Daily Abdominal Discomfort Scores

Change From Baseline in IBS-QoL Total Scores

Number of Bowel Incontinence Episodes

Percentage of Monthly Composite Responders

Percentage of Pain Responders

Percentage of Stool Consistency Responders

Percentage of Participants Who Were Composite Responders Based on Improvements From Baseline in Daily Worst Abdominal Pain And Daily Stool Consistency Scores

AUC: Area Under the Concentration-time Curve During the Dosing Interval for Eluxadoline

CL/F: Apparent Total Clearance of the Drug From Plasma After Oral Administration for Eluxadoline

Cmax: Maximum Concentration for Eluxadoline

Cmin: Minimum Concentration for Eluxadoline

Change From Baseline in Average Bristol Stool Form Scale (BSFS) Score Over 4 Weeks of Treatment Period

Change From Baseline in the 4-week Average of Daily Worst Abdominal Pain Scores During the Treatment Period

Change From Baseline in the 4-week Average of Daily Bowel Movement Frequency During the Treatment Period

Change From Baseline in the 4-week Average of Daily Bloating Scores During the Treatment Period

Change From Baseline in the 4-week Average Number of Daily Urgent Bowel Movements During the Treatment Period

Change From Baseline in Irritable Bowel Syndrome Quality of Life (IBS-QOL) Total Score at the End of the Treatment Period

Change From Baseline in Fasting Serum 7α-hydroxy-4-cholesten-3-one (7αC4) Levels at the End of the Treatment Period

Vc/F: Apparent Volume of Distribution for Eluxadoline

Tmax: Time to Cmax for Eluxadoline

t1/2: Half-Life for Eluxadoline