Naloxegol , a new drug for the treatment of opioid-induced constipation.

Abstract

INTRODUCTION:

With increasing chronic opioid use, opioid-induced constipation (OIC) is becoming a relevant clinical challenge. Presently, only few treatments have been demonstrated to be more effective than placebo in treating OIC but most of them have a restricted clinical application because of side effects. Naloxegol , an orally administered, peripherally acting, μ-opioid receptor antagonist (PAMORA), was developed for the treatment of OIC.

AREA COVERED:

This review summarizes published information and presentations at meetings on the effects of naloxegol in OIC. Pharmacodynamic studies have demonstrated that naloxegol inhibits gastrointestinal opioid effects while preserving central analgesic actions. Phase II and Phase III studies in patients with non-cancer OIC have confirmed the efficacy of naloxegol to inhibit OIC, and the most consistent efficacy was seen with the 25 mg dose once daily. Adverse events were mainly gastrointestinal in origin and usually transient and mild. There were no signs of opioid withdrawal in the studies. Safety and tolerability were also shown in a long-term safety study. Regulatory authorities have recently approved the use of naloxegol in OIC.

EXPERT OPINION:

Naloxegol is the first approved, orally available PAMORA. The drug has the potential to substantially improve management of OIC patients.

• Authors: Maura Corsetti, Jan Tack
• Journal: Expert opinion on pharmacotherapy (Expert Opin Pharmacother) Vol. 16 Issue 3 Pg. 399-406 (Feb 2015) ISSN: 1744-7666 [Electronic] England
• PMID: 25496063 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Analgesics, Opioid
• Morphinans
• Polyethylene Glycols
• naloxegol

Topics

• Analgesics, Opioid (adverse effects)
• Animals
• Clinical Trials, Phase II as Topic
• Clinical Trials, Phase III as Topic
• Constipation (chemically induced, drug therapy)
• Humans
• Morphinans (pharmacology, therapeutic use)
• Polyethylene Glycols (pharmacology, therapeutic use)