Chemical Property of Eluxadoline
Chemical Property:
- Boiling Point:834.2±65.0 °C(Predicted)
- PKA:4.01±0.10(Predicted)
- PSA：164.63000
- Density:1.284±0.06 g/cm3(Predicted)
- LogP:5.55960
- Storage Temp.:Refrigerator
- Solubility.:DMSO (Slightly), Methanol (Slightly)
- XLogP3:0.9
- Hydrogen Bond Donor Count:4
- Hydrogen Bond Acceptor Count:7
- Rotatable Bond Count:11
- Exact Mass:569.26381923
- Heavy Atom Count:42
- Complexity:917
- Purity/Quality:
-
99% *data from raw suppliers
Eluxadoline *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Drug Classes:Gastrointestinal Agents
- Canonical SMILES:CC1=CC(=CC(=C1CC(C(=O)N(CC2=CC(=C(C=C2)OC)C(=O)O)C(C)C3=NC=C(N3)C4=CC=CC=C4)N)C)C(=O)N
- Isomeric SMILES:CC1=CC(=CC(=C1C[C@@H](C(=O)N(CC2=CC(=C(C=C2)OC)C(=O)O)[C@@H](C)C3=NC=C(N3)C4=CC=CC=C4)N)C)C(=O)N
- Recent ClinicalTrials:Study to Explore the Therapeutic Effect of Eluxadoline in Treating Irritable Bowel Syndrome With Diarrhea in Children
- Recent EU Clinical Trials:A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Dose-Ranging Study to Evaluate the Safety and Efficacy of Eluxadoline in Pediatric Patients (Age 12 to 17 Years) with Irritable Bowel Syndrome with Diarrhea (IBS-D)
-
Description
Eluxadoline, originally developed
by Janssen and currently marketed by Allergan (formerly
Actavis), was approved in May 2015 by the FDA for the
treatment of diarrhea-predominant irritable bowel syndrome
(IBS-D). Eluxadoline, an orally dosed agent, employs a
unique mechanism for IBS-D treatment, as it functions
simultaneously as a μ- and κ-opioid receptor agonist and a δ-
opioid receptor antagonist, leading to a first-in-class therapy
for treatment of IBS-D. Specifically, in animal studies,
eluxadoline was found to interact with opioid receptors in the
gut, inhibiting neurogenically mediated secretion and reducing
intestinal contractility. Additionally, the treatment led to a
decrease in stress-induced acceleration of upper GI transit
without causing rebound constipation, earning its mark as
a first-line therapeutic treatment for IBS-D. In two phase III
clinical trials of over 2400 patients with IBS-D, patients taking
eluxadoline showed a greater improvement toward the end
point (≥30% improvement from their baseline IBS-D score on
at least 50% of days treated with eluxadoline) compared to
patients treated with placebo.
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Uses
Eluxadoline is an orally-active drug used to reduce symptoms of irritable bowel syndrome such as diarrhea and abdominal pain.
-
Clinical Use
Mixed mu-opioid receptor agonist, kappa-opioid receptor
agonist, and a-delta opioid receptor antagonist:
Treatment of irritable bowel syndrome with
diarrhoea
-
Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: concentration possibly increased by
rifampicin - avoid.
Antivirals: concentration possibly increased by
atazanavir, lopinavir, ritonavir, saquinavir and
tipranavir - avoid.
Ciclosporin: concentration of eluxadoline increased
- avoid.
Lipid-lowering agents: concentration possibly
increased by gemfibrozil - avoid.
