eluxadoline

Ligand id: 7691

Name: eluxadoline

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 9
Hydrogen bond donors 4
Rotatable bonds 12
Topological polar surface area 164.63
Molecular weight 569.26
XLogP 5.36
No. Lipinski's rules broken 2

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
In September 2014 the US FDA granted fast-track status to facilitate the development and expedite the review of this comound as a treatment for diarrhea-predominant irritable bowel syndrome (IBS-D). This decision was based on the results of two Phase III clinical studies that met their primary endpoints, showing significant improvement over placebo in both pain and diarrhea. In May 2015 the drug received full FDA marketing authorisation for IBS-D. Click here to view a list of clinical trials involving eluxadoline (using its company research code JNJ-27018966) hosted on the ClinicalTrials.gov website.
Mechanism Of Action and Pharmacodynamic Effects
Eluxadoline acts locally in the gastrointestinal tract. Whilst the μ opioid receptor agonist action treats pain it also reduces gastric propulsion and can lead to opioid induced constipation. The concomittant δ opioid receptor antagonist action should help reduce this constipation and permit the drug to deliver relief from the symptoms of IBS-D.