Janus kinase inhibitors for the treatment of myeloproliferative neoplasias and beyond

Nat Rev Drug Discov. 2011 Feb;10(2):127-40. doi: 10.1038/nrd3264.

Abstract

Recent advances in our understanding of the pathogenesis of the Philadelphia chromosome-negative myeloproliferative neoplasms, polycythaemia vera, essential thrombocythaemia and myelofibrosis have led to the identification of the mutation V617F in Janus kinase (JAK) as a potential therapeutic target. This information has prompted the development of ATP-competitive JAK2 inhibitors. Therapy with JAK2 inhibitors may induce rapid and marked reductions in spleen size and can lead to remarkable improvements in constitutional symptoms and overall quality of life. Because JAKs are involved in the pathogenesis of inflammatory and immune-mediated disorders, JAK inhibitors are also being tested in clinical trials in patients with rheumatoid arthritis and psoriasis, as well as for the treatment of other autoimmune diseases and for the prevention of allograft rejection. Preliminary results indicate that these agents hold great promise for the treatment of JAK-driven disorders.

Publication types

  • Review

MeSH terms

  • Animals
  • Humans
  • Janus Kinases / antagonists & inhibitors*
  • Janus Kinases / pharmacokinetics
  • Myeloproliferative Disorders / drug therapy*
  • Myeloproliferative Disorders / enzymology*
  • Protein Kinase Inhibitors / pharmacokinetics
  • Protein Kinase Inhibitors / therapeutic use*
  • Treatment Outcome

Substances

  • Protein Kinase Inhibitors
  • Janus Kinases