Mast cell leukemia: identification of a new c-Kit mutation, dup(501-502), and response to masitinib, a c-Kit tyrosine kinase inhibitor

Eur J Haematol. 2012 Jul;89(1):47-52. doi: 10.1111/j.1600-0609.2012.01761.x. Epub 2012 Apr 28.

Abstract

Objective: Most patients with systemic mastocytosis bear mutations in the tyrosine kinase receptor gene c-Kit. Limited treatment options exist for mast cell leukemia, a rare form of systemic mastocytosis associated with a dire prognosis. Our aim was to investigate c-Kit mutations associated with mast cell leukemia and find new treatment for this severe form of mastocytosis.

Patient and methods: We describe here a patient with mast cell leukemia characterized by 42% of circulating mast cells associated with a previously unidentified c-Kit mutation in adult mastocytosis: dup(501-502).

Main findings: This patient was treated with masitinib, a novel c-Kit tyrosine kinase inhibitor, with a dramatic response observed following 3 months of treatment, including clinical improvement, disappearance of circulating mast cells, and decrease in both serum histamine and tryptase levels. In vitro and ex vivo research was performed on the patient's cells and revealed constitutive c-Kit phosphorylation in mast cell leukemia.

Conclusions: This case highlights the importance of sequencing all c-Kit exons when the classical D816V c-Kit mutation is not found, even in adults with SM. It also indicates that masitinib may be safe and effective for the treatment for some mast cell leukemia.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Base Sequence
  • Benzamides
  • COS Cells
  • Chlorocebus aethiops
  • Female
  • Humans
  • Immunophenotyping
  • Leukemia, Mast-Cell / drug therapy*
  • Leukemia, Mast-Cell / genetics*
  • Mast Cells / metabolism
  • Mast Cells / pathology
  • Mutation*
  • Neoplastic Cells, Circulating / metabolism
  • Neoplastic Cells, Circulating / pathology
  • Piperidines
  • Protein Kinase Inhibitors / therapeutic use*
  • Proto-Oncogene Proteins c-kit / genetics*
  • Pyridines
  • Thiazoles / therapeutic use
  • Tryptases / blood

Substances

  • Antineoplastic Agents
  • Benzamides
  • Piperidines
  • Protein Kinase Inhibitors
  • Pyridines
  • Thiazoles
  • Proto-Oncogene Proteins c-kit
  • Tryptases
  • masitinib