Oral naloxegol (Movantik™, Moventig(®)), a peripherally acting μ-opioid receptor antagonist, inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract. This article reviews the pharmacological properties of naloxegol and its clinical efficacy and tolerability in patients with opioid-induced constipation. It demonstrated clinical efficacy and was well tolerated in placebo-controlled trials in patients with non-cancer pain and opioid-induced constipation, including those with an inadequate response to laxatives, and was well tolerated in a long-term safety study. As a PEGylated naloxone derivative, naloxegol is associated with significant improvements in spontaneous bowel movements, while maintaining levels of opioid-related analgesia (a result of its reduced ability to cross the blood-brain barrier). Naloxegol is a useful option in the treatment of opioid-induced constipation.