JAK selectivity: more precision less troubles

Expert Rev Gastroenterol Hepatol. 2020 Sep;14(9):789-796. doi: 10.1080/17474124.2020.1780120. Epub 2020 Jun 16.

Abstract

Introduction: Janus kinases inhibitors (JAKi) are new small molecules recently introduced in the armamentarium of treatments for Inflammatory Bowel Disease (IBD). Janus Kinases (JAK) are tyrosine kinases that act by linkage with different intracellular receptors, regulating cytokines gene transcription implicated in the inflammatory burden seen in IBD patients.

Areas covered: A comprehensive literature search was performed to retrieve studies on JAKi and IBD to discuss the latest developments and how the selectivity of these drugs is changing the natural course of IBD.

Expert opinion: Available data on efficacy and safety of JAKi in IBD are highly encouraging and because of their selectivity, these drugs might become among the foremost options in the treatment algorithm.

Keywords: Janus Kinase; Key-words: inflammatory bowel disease; efficacy; safety; selectivity.

Publication types

  • Review

MeSH terms

  • Colitis, Ulcerative / drug therapy*
  • Crohn Disease / drug therapy*
  • Heterocyclic Compounds, 3-Ring / therapeutic use
  • Humans
  • Janus Kinase 1 / antagonists & inhibitors
  • Janus Kinase 2 / antagonists & inhibitors
  • Janus Kinase 3 / antagonists & inhibitors
  • Janus Kinase Inhibitors / therapeutic use*
  • Naphthyridines / therapeutic use
  • Nitriles / therapeutic use
  • Piperidines / therapeutic use*
  • Pyridines / therapeutic use
  • Pyrimidines / therapeutic use*
  • Signal Transduction
  • TYK2 Kinase / antagonists & inhibitors
  • Triazoles / therapeutic use

Substances

  • GLPG0634
  • Heterocyclic Compounds, 3-Ring
  • Janus Kinase Inhibitors
  • Naphthyridines
  • Nitriles
  • Piperidines
  • Pyridines
  • Pyrimidines
  • Triazoles
  • izencitinib
  • upadacitinib
  • tofacitinib
  • JAK1 protein, human
  • JAK2 protein, human
  • JAK3 protein, human
  • Janus Kinase 1
  • Janus Kinase 2
  • Janus Kinase 3
  • TYK2 Kinase
  • TYK2 protein, human