Pharmacometric Modeling of Naloxegol Efficacy and Safety: Impact on Dose and Label

Clin Pharmacol Ther. 2017 Nov;102(5):741-744. doi: 10.1002/cpt.719. Epub 2017 May 26.

Abstract

Naloxegol is a peripherally acting μ-opioid receptor antagonist that was developed for the treatment of opioid-induced constipation. Modeling and simulation of naloxegol efficacy and tolerability informed selection of doses for phase III studies and provided comprehensive dosage recommendations for the naloxegol US package insert.

Publication types

  • Review

MeSH terms

  • Analgesics, Opioid / adverse effects
  • Animals
  • Constipation / chemically induced
  • Constipation / drug therapy
  • Constipation / metabolism
  • Dose-Response Relationship, Drug
  • Drug Labeling / legislation & jurisprudence
  • Drug Labeling / methods*
  • Drug Labeling / standards
  • Humans
  • Models, Biological*
  • Morphinans / pharmacokinetics*
  • Morphinans / standards
  • Morphinans / therapeutic use
  • Narcotic Antagonists / pharmacokinetics*
  • Narcotic Antagonists / standards
  • Narcotic Antagonists / therapeutic use
  • Polyethylene Glycols / pharmacokinetics*
  • Polyethylene Glycols / standards
  • Polyethylene Glycols / therapeutic use
  • Treatment Outcome

Substances

  • Analgesics, Opioid
  • Morphinans
  • Narcotic Antagonists
  • Polyethylene Glycols
  • naloxegol