Asciminib as a third line option in chronic myeloid leukemia

Int J Hematol. 2023 Jan;117(1):16-23. doi: 10.1007/s12185-022-03432-7. Epub 2022 Aug 5.

Abstract

Unmet needs remain in the treatment of chronic phase chronic myeloid leukemia (CML) in later lines. Sequential use of tyrosine kinase inhibitors (TKIs) is associated with decreased overall survival and emergence of new mutations, particularly the T315I mutation. Among the new drugs developed to overcome resistance and intolerance, the STAMP inhibitor asciminib (which specifically targets the ABL myristoyl pocket) is the first example of a drug that works by allosteric inhibition. This review focuses on its mechanism of action, pharmacokinetic, efficacy, and toxicity, as well as how this drug will change the therapeutic approach for CML patients not eligible to receive other available drugs.

Keywords: Asciminib; Chronic myeloid leukemia; Later lines.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / adverse effects
  • Drug Resistance, Neoplasm
  • Fusion Proteins, bcr-abl / genetics
  • Humans
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / drug therapy
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / genetics
  • Mutation
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Pyrazoles / therapeutic use

Substances

  • asciminib
  • Fusion Proteins, bcr-abl
  • Pyrazoles
  • Protein Kinase Inhibitors
  • Antineoplastic Agents