Eluxadoline 864821-90-9

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Eluxadoline Basic information
Overview and History Indication and applications Mode of action Adverse reactions Warning and Precaution References
Product Name: Eluxadoline
Synonyms: Eluxadoline (Viberzi);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;API-Diarrhea;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-;EOS-61916
CAS: 864821-90-9
MF: C32H35N5O5
MW: 569.6508
EINECS: 1592732-453-0
Product Categories: API
Mol File: 864821-90-9.mol

Eluxadoline Chemical Properties
Boiling point  834.2±65.0 °C(Predicted)
density  1.284±0.06 g/cm3(Predicted)
pka 4.01±0.10(Predicted)
CAS DataBase Reference 864821-90-9

Indication and applications Eluxadoline is indicated for the treatment of diarrhea-predominant irritable bowel syndrome(IBS-D). It can work directly in the intestines to slow the movement of food during digestion. Eluxadoline also makes the nerves in the intestines less sensitive to stimulation[1, 6].
Mode of action Eluxadoline takes effect through acting as the antagonist of mu-opioid receptor agonis, kappa opioid receptor agonist and a delta opioid receptor[7,8]. Eluxadoline can be used for diarrhea predominant IBS because it reduces intestinal contractility and normalizes stress-induced acceleration of upper GI transit[9]. Antagonistic activity at the delta receptor minimizes the constipating effect usually seen by mu-opioid receptor agonists alone. Because of it's limited systemic bioavailability, there may be less side effects associated with the use of eluxadoline in comparison with other therapies used to treat diarrhea predominant IBS[10].
Adverse reactions Common adverse reaction associated with Eluxadoline include constipation, nausea, abdominal pain, upper respiratory tract infection, pancreatitis, sphincter of Oddi spasm, hypersensitivity reactions, vomiting, nasopharyngitis, abdominal distention, bronchitis, dizziness, flatulence, rash, increased ALT, fatigue, viral gastroenteritis and stomach pain[4, 6, 11]. Less common adverse reactions also include gastroesophageal reflux disease, sedation, somnolence, and euphoric mood, respiration disorders such as asthma, bronchospasm, respiration failure and wheezing. Constipation was the most commonly reported adverse reaction in during the treatment by Eluxadoline. Approximately 50% of constipation events occurred within the first 2 weeks of treatment while the majority occurred within the first 3 months of therapy. Similar rates of constipation occurred between the active and placebo arms beyond 3 months of treatment. In severe cases, constipation can even lead to permanent discontinuation of drugs[11].