Pharmacotherapeutic advances for chronic myelogenous leukemia: beyond tyrosine kinase inhibitors

Expert Opin Pharmacother. 2024 Feb;25(2):189-202. doi: 10.1080/14656566.2024.2331778. Epub 2024 Mar 19.

Abstract

Introduction: Despite the notable success of tyrosine kinase inhibitors (TKIs) in treating chronic myeloid leukemia (CML), a subset of patients experiences resistance, or relapse after discontinuation. This challenge is attributed to the Ph+ leukemia stem cells (LSCs) pool not fully involved in the inhibition process due to the current therapeutic approach.

Areas covered: Current pharmacological advancements in CML therapy focus on targeting LSCs, intervening in self-renewal pathways, and exploiting biological vulnerabilities. Beyond BCR::ABL1 inhibition, innovative approaches include immunotherapy, epigenetic modulation, and interference with microenvironmental mechanisms.

Expert opinion: Diverse therapeutic strategies beyond TKIs are under investigation. Immunotherapy with interferon-α (IFN-α) shows some biological effects, although further research is needed for optimal application in enhancing discontinuation rates. Other compounds were able to mobilize Ph+ LSCs from the bone marrow niche (DPP-IV inhibitor vildagliptin or PAI-1 inhibitor TM5614) increasing the LSC clearance or target the CD26, a Ph+ specific surface receptor. It is noteworthy that the majority of these alternative strategies still incorporate TKIs. In conclusion, novel therapeutic perspectives are emerging for CML, holding the potential for substantial advancements in disease treatment.

Keywords: Chronic myeloid leukemia; epigenetic; immunotherapy; leukemia stem cells; mobilization; strategies; treatment-free remission.

Publication types

  • Review

MeSH terms

  • Dipeptidyl-Peptidase IV Inhibitors* / therapeutic use
  • Fusion Proteins, bcr-abl
  • Humans
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / drug therapy
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / metabolism
  • Neoplastic Stem Cells / metabolism
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Tyrosine Kinase Inhibitors
  • Vildagliptin

Substances

  • Tyrosine Kinase Inhibitors
  • Protein Kinase Inhibitors
  • Vildagliptin
  • Dipeptidyl-Peptidase IV Inhibitors
  • Fusion Proteins, bcr-abl