Eluxadoline

Base Information

• Chemical Name: Eluxadoline
• CAS No.: 864821-90-9
• Molecular Formula: C32H35N5O5
• Molecular Weight: 569.65
• Mol file: 864821-90-9.mol

Synonyms:Eluxadoline;JNJ 27018966;5-(((S)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-N-((S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl)propanamido)methyl)-2-methoxybenzoic acid;Eluxadolin

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)

Purity/Quality:

99.0% ^*data from raw suppliers

Eluxadoline ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

• 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.
• 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.