[Novel therapeutics in myeloproliferative neoplasms: beyond JAK inhibitors]

Rinsho Ketsueki. 2023;64(9):970-980. doi: 10.11406/rinketsu.64.970.
[Article in Japanese]

Abstract

The discovery of driver genes such as JAK2 in myeloproliferative neoplasms (MPN) led to a better understanding of MPN pathogenesis as a constitutive activation of the JAK/STAT signal. Following these findings, several types of JAK inhibitors have been developed. Ruxolitinib, a JAK1/2 inhibitor licensed for polycythemia vera and myelofibrosis, demonstrated efficacy in regulating hematocrit levels, lowering spleen volume, and relieving MPN-related symptoms. However, some patients with myelofibrosis are refractory to JAK inhibitors, and some are intolerant due to cytopenia. Furthermore, JAK inhibitors did not slow the progression of acute leukemia, indicating the need for new therapeutic methods for myelofibrosis. Novel medicines, including BCL inhibitor, MDM2 inhibitor, LSD1 inhibitor, PI3K inhibitor, BET inhibitor and telomerase inhibitor, are presently being evaluated in clinical studies for myelofibrosis with the potential to enhance clinical outcomes.

Keywords: JAK inhibitor; Myelofibrosis; Myeloproliferative neoplasms; Novel agents.

Publication types

  • English Abstract

MeSH terms

  • Antineoplastic Agents* / therapeutic use
  • Humans
  • Janus Kinase 2 / genetics
  • Janus Kinase Inhibitors* / therapeutic use
  • Myeloproliferative Disorders* / genetics
  • Phosphatidylinositol 3-Kinases / therapeutic use
  • Polycythemia Vera* / drug therapy
  • Primary Myelofibrosis* / drug therapy
  • Protein Kinase Inhibitors / therapeutic use

Substances

  • Janus Kinase Inhibitors
  • Phosphatidylinositol 3-Kinases
  • Protein Kinase Inhibitors
  • Janus Kinase 2
  • Antineoplastic Agents