Alvimopan

Alvimopan is a selective antagonist of the cloned human µ-opioid receptor with a Ki of 0.4 nM (0.2 ng/mL) and no measurable opioid-agonist effects in standard pharmacologic assays. The dissociation of [ 3 H]-alvimopan from the human µ-opioid receptor is slower than that of other opioid ligands, consistent with its higher affinity for the receptor.

• Alvimopan capsules are indicated to accelerate the time to upper and lower gastrointestinal recovery following surgeries that include partial bowel resection with primary anastomosis. Alvimopan capsules are an opioid antagonist indicated to accelerate the time to upper and lower gastrointestinal recovery following surgeries that include partial bowel resection with primary anastomosis.

• Alvimopan capsules are contraindicated in patients who have taken therapeutic doses of opioids for more than 7 consecutive days immediately prior to taking alvimopan capsules [see Warnings and Precautions ( 5.3 )] . Patients who have taken therapeutic doses of opioids for more than 7 consecutive days prior to taking alvimopan capsules.contraindicated

For hospital use only. The recommended adult dosage of alvimopan capsules is 12 mg administered 30 minutes to 5 hours prior to surgery followed by 12 mg twice daily beginning the day after surgery until discharge for a maximum of 7 days. Patients should not receive more than 15 doses of alvimopan capsules. Alvimopan capsules can be taken with or without food [see Clinical Pharmacology ( 12.3 )] . For hospital use only. ( 2 ) The recommended dosage is 12 mg administered 30 minutes to 5 hours prior to surgery followed by 12 mg twice daily beginning the day after surgery until discharge for a maximum of 7 days. Patients should not receive more than 15 doses of alvimopan capsules. ( 2 )

Myocardial Infarction : A higher number of myocardial infarctions was reported in patients treated with alvimopan 0.5 mg twice daily compared with placebo in a 12-month study in patients treated with opioids for chronic non-cancer pain, although a causal relationship with long-term use has not been established. ( 5.1 ) Gastrointestinal Adverse Reactions in Opioid Tolerant Patients : Patients recently exposed to opioids may be more sensitive to the effects of alvimopan and experience gastrointestinal adverse reactions (e.g., abdominal pain, nausea and vomiting, and diarrhea). ( 5.3 ) Patients with Severe Hepatic Impairment : Increased risk of serious adverse reactions due to higher plasma concentrations; use is not recommended. ( 5.4 , 8.6 ) Patients with End-Stage Renal Disease : No studies have been conducted; use is not recommended. ( 5.5 , 8.7 ) Patients with Complete Gastrointestinal Obstruction : No studies have been conducted in patients with complete gastrointestinal obstruction or in patients who have surgery for correction of complete bowel obstruction; use is not recommended. ( 5.6 ) Patients with Pancreatic and Gastric Anastomoses : No studies have been conducted; use is not recommended. ( 5.7 ) 5.1 Potential Risk of Myocardial Infarction with Long-Term Use There were more reports of myocardial infarctions in patients treated with alvimopan 0.5 mg twice daily compared with placebo-treated patients in a 12-month study of patients treated with opioids for chronic non-cancer pain (alvimopan 0.5 mg, n = 538; placebo, n = 267).

The following clinically significant adverse reactions are described elsewhere in the labeling: Potential Risk of Myocardial Infarction with Long-Term Use [see Warnings and Precautions ( 5.1 )] Gastrointestinal-Related Adverse Reactions in Opioid-Tolerant Patients [see Warnings and Precautions ( 5.3 )] Risk of Serious Adverse Reactions in Patients with Severe Hepatic Impairment [see Warnings and Precautions ( 5.4 )] Risk of Serious Adverse Reactions in Patients with Complete Gastrointestinal Obstruction [see Warnings and Precautions ( 5.6 )] Risk of Serious Adverse Reactions in Pancreatic and Gastric Anastomoses [see Warnings and Precautions ( 5.7 )] Most common adverse reaction (≥1.5%): dyspepsia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc. at 1-800-962-8364 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be compared directly with rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The adverse event information from clinical trials does, however, provide a basis for identifying the adverse events that appear to be related to drug use and for approximating rates. The data described below reflect exposure to alvimopan 12 mg in 1,793 patients in 10 placebo-controlled studies.

Hepatic Impairment : Monitor patients with mild-to-moderate impairment for gastrointestinal adverse reactions. ( 8.6 ) Renal Impairment : Monitor patients with mild-to-severe impairment for gastrointestinal adverse reactions. ( 8.7 ) Race/Ethnicity : Monitor Japanese patients for gastrointestinal adverse reactions. ( 8.8 ) 8.1 Pregnancy Risk Summary: Available data regarding use of alvimopan in pregnant women are limited, and are insufficient to inform a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. No fetal harm was observed in animal reproduction studies with oral administration of alvimopan during organogenesis to pregnant rats at doses 68 to 136 times the recommended human oral dose, or with intravenous administration during organogenesis to pregnant rats and pregnant rabbits at doses 3.4 to 6.8 times, and 5 to 10 times, respectively, the recommended human oral dose (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

Following oral administration of alvimopan, an amide hydrolysis compound is present in the systemic circulation, which is considered a product exclusively of intestinal flora metabolism. This compound is referred to as the ‘metabolite’.

• Dec 19, 2019ANDAANDA208295Watson Labs Teva
• Jan 24, 2023ANDAANDA216843Ph Health
• Aug 31, 2023ANDAANDA217753Hikma

1. 1Hospitalisation1944%
2. 2Acute Kidney Injury512%
3. 3Acute Myocardial Infarction49.3%
4. 4Ileus37.0%
5. 5Pruritus37.0%
6. 6Urinary Retention37.0%
7. 7Adenocarcinoma Of Colon24.7%
8. 8Cardio-respiratory Arrest24.7%
9. 9Chronic Kidney Disease24.7%
10. 10Dizziness24.7%
11. 11Freezing Phenomenon24.7%
12. 12Haemoglobin Decreased24.7%
13. 13Hyperhidrosis24.7%
14. 14Pain24.7%
15. 15Postoperative Wound Infection24.7%

The 10 most recently updated of 26 ClinicalTrials.gov registrations naming Alvimopan as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Surgical Techniques During Cystectomy
  Recruiting · Phase 3 · Interventional · 530 enrolled · Memorial Sloan Kettering Cancer Center
  NCT06703476updated 2026-01-27
• Alvimopan as a Rescue Treatment of Postoperative Ileus
  Completed · Phase 4 · Interventional · 65 enrolled · Scott Steele
  NCT04405037updated 2025-08-20
• Alvimopan Versus Placebo in Patients Undergoing Radical Cystectomy on an Enhanced Recovery Protocol
  Recruiting · Phase 3 · Interventional · 136 enrolled · Brigham and Women's Hospital
  NCT03216525updated 2023-09-28
• Alvimopan as Rescue in Post op Ileus
  Terminated · Phase 3 · Interventional · 14 enrolled · Sharon Stein
  NCT02742181updated 2022-11-18
• Phase 2 RCT of Alvimopan vs. Placebo After CRS/HIPEC
  Terminated · Phase 2 · Interventional · 84 enrolled · University of California, San Diego
  NCT03352414updated 2021-08-18
• Trial of Alvimopan in Major Spine Surgery
  Completed · Phase 4 · Interventional · 49 enrolled · University of Virginia
  NCT02789111updated 2020-12-01
• Conventional VS Enhanced Recovery After Surgery Protocols in Emergency GIT Surgery
  Unknown · Observational · 60 enrolled · Assiut University
  NCT04584060updated 2020-10-12
• Alvimopan Use in Polytraumatized Patients
  Terminated · Phase 4 · Interventional · 3 enrolled · University of Puerto Rico
  NCT03068975updated 2020-02-05
• Gastrointestinal Tract Recovery in Patients Undergoing Open Ventral Hernia Repair
  Terminated · Interventional · 10 enrolled · Medical College of Wisconsin
  NCT02379858updated 2019-11-14
• Alvimopan and Ileus in PSF
  Completed · Interventional · 31 enrolled · Washington University School of Medicine
  NCT02218190updated 2019-05-17

Frequently asked questions

How does Alvimopan work?

Alvimopan is a selective antagonist of the cloned human µ-opioid receptor with a Ki of 0.4 nM (0.2 ng/mL) and no measurable opioid-agonist effects in standard pharmacologic assays. The dissociation of [ 3 H]-alvimopan from the human µ-opioid receptor is slower than that of other opioid ligands, consistent with its higher affinity for the receptor.

What is Alvimopan used for?

According to FDA labeling, Alvimopan carries indications including: Alvimopan capsules are indicated to accelerate the time to upper and lower gastrointestinal recovery following surgeries that include partial bowel resection with primary anastomosis. Alvimopan capsules are an opioid antagonist indicated to accelerate the time to upper and lower gastrointestinal recovery following surgeries that include partial bowel resection with primary anastomosis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Alvimopan?

Alvimopan is classified as Peripheral opioid receptor antagonists, Competitive Opioid Antagonists, Increased Gastric Motility.

What are the brand names for Alvimopan?

Alvimopan is marketed under brand names including Entereg.

What are the contraindications for Alvimopan?

Alvimopan labeling lists contraindications including: Alvimopan capsules are contraindicated in patients who have taken therapeutic doses of opioids for more than 7 consecutive days immediately prior to taking alvimopan capsules [see Warnings and Precautions ( 5.3 )] . Patients who have taken therapeutic doses of opioids for more than 7 consecutive days prior to taking alvimopan capsules.. Always consult the full prescribing information and a clinician.