Eluxadoline

Eluxadoline is a mu-opioid receptor agonist; eluxadoline is also a delta opioid receptor antagonist and a kappa opioid receptor agonist. The binding affinities (Ki) of eluxadoline for the human mu and delta opioid receptors are 1.8 nM and 430 nM, respectively.

• VIBERZI is indicated in adults for the treatment of irritable bowel syndrome with diarrhea (IBS-D). VIBERZI is a mu-opioid receptor agonist, indicated in adults for the treatment of irritable bowel syndrome with diarrhea (IBS-D).ICD-10: K58.9

• VIBERZI is contraindicated in patients: Without a gallbladder. These patients are at increased risk of developing serious adverse reactions of pancreatitis and/or sphincter of Oddi spasm [see Warnings and Precautions ( 5.1 , 5.2 )] With known or suspected biliary duct obstruction; or sphincter of Oddi disease or dysfunction.contraindicated

The recommended dosage of VIBERZI is 100 mg taken orally twice daily with food. The recommended dosage of VIBERZI is 75 mg taken orally twice daily with food in patients: unable to tolerate the 100 mg dose of VIBERZI [see Adverse Reactions ( 6.1 ) ]. receiving concomitant OATP1B1 inhibitors [see Drug Interactions ( 7 )] . with mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) hepatic impairment [see Use in Specific Population s ( 8.6 ) ] . with moderate or severe renal impairment (eGFR less than 60 mL/min/1.73 m 2 ); and in patients with end stage renal disease (ESRD) not yet on dialysis (eGFR less than 15 mL/min/1.73 m 2 ) [see Use in Specific Populations ( 8.7 )]. Discontinue VIBERZI in patients who develop severe constipation [see Warnings and Precautions ( 5.4 )] . Instruct patients if they miss a dose, take the next dose at the regular time and not to take 2 doses at the same time to make up for a missed dose. The recommended dosage in adults is 100 mg twice daily taken with food. ( 2 ) The recommended dosage is 75 mg twice daily taken with food in patients: unable to tolerate the 100 mg dose. ( 2 , 6.1 ) receiving concomitant OATP1B1 inhibitors. ( 2 , 7 ) with mild or moderate hepatic impairment. ( 2 , 8.6 ) with moderate or severe renal impairment; and in patients with end stage renal disease not yet on dialysis. ( 2 , 8.7 ) Discontinue VIBERZI in patients who develop severe constipation. ( 2 ) If a dose is missed, take the next dose at the regular time; do not take 2 doses at once. ( 2 )

Pancreatitis and Sphincter of Oddi Spasm : Monitor patients for new or worsening abdominal pain, with or without nausea and vomiting, or acute biliary pain with liver or pancreatic enzyme elevations; immediately discontinue VIBERZI and seek medical attention if symptoms develop. ( 5.1 , 5.2 ) Hypersensitivity Reactions, including anaphylaxis : Immediately discontinue VIBERZI and seek medical attention if symptoms develop. ( 4 , 5.3 ) Constipation: Instruct patients to stop VIBERZI and immediately contact their healthcare provider if they develop severe constipation. Avoid use with other drugs that may cause constipation ( 5.4 , 7 ) 5.1 Pancreatitis Pancreatitis, with or without sphincter of Oddi spasm [ see Warnings and Precautions ( 5.1 ) ] , has been reported in patients taking either the 75 mg or 100 mg dosage of VIBERZI, including serious cases resulting in hospitalization, primarily in patients without a gallbladder. Fatal cases have also been reported in patients without a gallbladder. VIBERZI is contraindicated in patients without a gallbladder [ see Contraindications ( 4 ) ] . Most of the reported cases of serious pancreatitis occurred within a week of starting treatment with VIBERZI and some developed symptoms after one to two doses. In patients with a gallbladder, evaluate a patient’s alcohol intake prior to starting VIBERZI. Instruct patients to avoid chronic or acute excessive alcohol use while taking VIBERZI. Monitor for new or worsening abdominal pain that may radiate to the back or shoulder, with or without nausea and vomiting.

The following adverse reactions described below and elsewhere in the labeling include: Pancreatitis [see Warnings and Precautions ( 5.1 )] Sphincter of Oddi Spasm [ see Warnings and Precautions ( 5.2 )] Hypersensitivity Reactions [see Warnings and Precautions ( 5.3 )] Constipation [see Warnings and Precautions ( 5.4 )] Most common adverse reactions (>5%) are constipation, nausea and abdominal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact AbbVie at 1- 800-678-1605 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial s Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Over 1700 patients with IBS-D have been treated with 75 or 100 mg of VIBERZI twice daily in controlled trials. Exposures from placebo-controlled clinical trials in adult patients with IBS-D included 1391 exposed for 3 months, 1001 exposed for 6 months and 488 exposed for one year. Demographic characteristics were comparable between the treatment groups [see Clinical Studies ( 14 )] . Data described below represent pooled data compared to placebo across the randomized trials. Pancreatitis Cases of pancreatitis, not associated with sphincter of Oddi spasm, were reported in 2/807 (0.2%) of patients receiving 75 mg and 3/1032 (0.3%) of patients receiving 100 mg VIBERZI twice daily in clinical trials.

8.1 Pregnancy Risk Summary There are no studies with VIBERZI in pregnant women that inform any drug-associated risks. The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4% and of miscarriage is 15 to 20% of clinically recognized pregnancies. In animal reproduction studies, oral and subcutaneous administration of eluxadoline to rats and rabbits during organogenesis at doses approximately 51 and 115 times the human exposure after a single oral dose of 100 mg, respectively, demonstrated no teratogenic effects. In a pre- and postnatal development study in rats, no adverse effects were observed in offspring with oral administration of eluxadoline at doses approximately 10 times the human exposure ( see Data ) . Data Animal Data Eluxadoline administered as combined oral (1000 mg/kg/day) and subcutaneous (5 mg/kg/day) doses during the period of organogenesis to rats and rabbits (exposures about 51 and 115 times, respectively, the human AUC of 24 ng.h/mL after a single oral dose of 100 mg) did not cause any adverse effects on embryofetal development.

Metabolism

Following oral administration of 100 mg VIBERZI in healthy subjects, the C max of eluxadoline was approximately 2 to 4 ng/mL and AUC was 12 to 22 ng.h/mL. Eluxadoline has approximately linear pharmacokinetics with no accumulation upon repeated twice daily dosing.

No reports of overdosage with VIBERZI have been reported. In the event of acute overdose, the stomach should be emptied and adequate hydration maintained. The patient should be carefully observed and given standard supportive treatment as required. Given eluxadoline’s action at opioid receptors, administration of a narcotic mu-opioid antagonist, such as naloxone, should be considered. Considering the short half-life of naloxone, repeated administration may be necessary. In the event of naloxone administration, subjects should be monitored closely for the return of overdose symptoms, which may indicate need for repeated naloxone injection.

• May 27, 2015NDANDA206940Abbvie

1. 1Off Label Use36112%
2. 2Abdominal Pain35012%
3. 3Diarrhoea34212%
4. 4Constipation2829.7%
5. 5Pancreatitis2789.6%
6. 6Nausea2187.5%
7. 7Drug Ineffective2177.5%
8. 8Abdominal Pain Upper2097.2%
9. 9Inappropriate Schedule Of Drug Administration1625.6%
10. 10Vomiting1364.7%
11. 11Fatigue1184.1%
12. 12Dizziness1083.7%
13. 13Wrong Technique In Product Usage Process1083.7%
14. 14Pain1053.6%
15. 15Incorrect Dose Administered893.1%

The 10 most recently updated of 10 ClinicalTrials.gov registrations naming Eluxadoline as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Efficacy of Pregabalin for Patients With Irritable Bowel Syndrome
  Recruiting · Interventional · 258 enrolled · Beijing Tiantan Hospital
  NCT07635394updated 2026-06-09
• Study to Explore the Therapeutic Effect of Eluxadoline in Treating Irritable Bowel Syndrome With Diarrhea in Children
  Recruiting · Phase 2 · Interventional · 95 enrolled · AbbVie
  NCT03339128updated 2025-09-19
• A Study Evaluating Oral Eluxadoline Administered to Pediatric Participants With Irritable Bowel Syndrome With Diarrhea (IBS-D)
  Enrolling by invitation · Phase 3 · Interventional · 124 enrolled · AbbVie
  NCT04880876updated 2025-07-17
• Investigation of Eluxadoline for Diabetic Diarrhea
  Withdrawn · Phase 2 · Phase 3 · Interventional · 0 enrolled · Temple University
  NCT04313088updated 2023-05-06
• Eluxadoline Bile Acid Malabsorption (BAM) Study
  Completed · Phase 4 · Interventional · 24 enrolled · Allergan
  NCT03441581updated 2021-05-19
• Efficacy, Safety, and Tolerability of JNJ-27018966 (Eluxadoline) in the Treatment of Irritable Bowel Syndrome With Diarrhea
  Completed · Phase 2 · Interventional · 807 enrolled · Furiex Pharmaceuticals, Inc
  NCT01130272updated 2019-10-22
• Effects of Eluxadoline (Viberzi®) 100 mg Twice Daily on Diarrhea-Associated Fecal Incontinence
  Withdrawn · Phase 2 · Interventional · 0 enrolled · University of North Carolina, Chapel Hill
  NCT03489265updated 2019-07-25
• Efficacy of Eluxadoline in the Treatment of Irritable Bowel Syndrome With Diarrhea in Patients With Inadequate Control of Symptoms With Prior Loperamide Use
  Completed · Phase 4 · Interventional · 346 enrolled · Allergan
  NCT02959983updated 2019-02-15
• Efficacy, Safety, and Tolerability of Eluxadoline in the Treatment of Participants With Diarrhea-Predominant Irritable Bowel Syndrome (IBS-d)
  Completed · Phase 3 · Interventional · 1,282 enrolled · Furiex Pharmaceuticals, Inc
  NCT01553591updated 2018-09-04
• Efficacy, Safety, and Tolerability of Eluxadoline in the Treatment of Participants With Diarrhea-Predominant Irritable Bowel Syndrome (IBS-d)
  Completed · Phase 3 · Interventional · 1,146 enrolled · Furiex Pharmaceuticals, Inc
  NCT01553747updated 2018-07-30

Frequently asked questions

How does Eluxadoline work?

Eluxadoline is a mu-opioid receptor agonist; eluxadoline is also a delta opioid receptor antagonist and a kappa opioid receptor agonist. The binding affinities (Ki) of eluxadoline for the human mu and delta opioid receptors are 1.8 nM and 430 nM, respectively.

What is Eluxadoline used for?

According to FDA labeling, Eluxadoline carries indications including: VIBERZI is indicated in adults for the treatment of irritable bowel syndrome with diarrhea (IBS-D). VIBERZI is a mu-opioid receptor agonist, indicated in adults for the treatment of irritable bowel syndrome with diarrhea (IBS-D).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Eluxadoline?

Eluxadoline is classified as Antipropulsives, mu-Opioid Receptor Agonist, Opioid Antagonists, Opioid mu-Receptor Agonists, Decreased Large Intestinal Motility.

What are the brand names for Eluxadoline?

Eluxadoline is marketed under brand names including Viberzi.

What are the contraindications for Eluxadoline?

Eluxadoline labeling lists contraindications including: VIBERZI is contraindicated in patients: Without a gallbladder. These patients are at increased risk of developing serious adverse reactions of pancreatitis and/or sphincter of Oddi spasm [see Warnings and Precautions ( 5.1 , 5.2 )] With known or suspected biliary duct obstruction; or sphincter of Oddi disease or dysfunction.. Always consult the full prescribing information and a clinician.