Tyrosine kinase inhibitors in hematological malignancies

Postepy Hig Med Dosw (Online). 2011 Dec 5;65:819-28. doi: 10.5604/17322693.968778.


Recently novel treatment modalities has focused on targeted therapies. Tyrosine kinases represent a good target for cancer treatment since they are involved in transferring phosphate groups from ATP to tyrosine residues in specific substrate proteins transducing intracellular signals engaged in the many mechanisms, playing an important role in the modulation of growth factors signaling that are strongly related to carcinogenesis. Deregulation of tyrosine kinases activity was also found in hematological malignancies, particularly overexpression of tyrosine kinases was observed in chronic myeloid leukemia or acute lymphoblastic leukemia. Herein we show that tyrosine kinase inhibitors have revolutionized hematology malignancies therapy in a very short period of time and they still remain one of the most interesting anticancer compounds that could give a hope for cure and not only long-lasting complete remission. This manuscript summarizes current view on the first generation tyrosine kinase inhibititor--imatinib, second generation--dasatinib, nilotinib and bosutnib as well as new generation tyrosine kinase inhibititors--ponatinib and danusertib in hematooncology.

Publication types

  • Review

MeSH terms

  • Aniline Compounds / therapeutic use
  • Antineoplastic Agents / therapeutic use*
  • Benzamides
  • Dasatinib
  • Hematologic Neoplasms / drug therapy*
  • Humans
  • Imatinib Mesylate
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy*
  • Nitriles / therapeutic use
  • Piperazines / immunology
  • Piperazines / therapeutic use
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / drug therapy*
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Protein-Tyrosine Kinases / therapeutic use
  • Pyrimidines / immunology
  • Pyrimidines / therapeutic use
  • Quinolines / therapeutic use
  • Thiazoles / therapeutic use


  • 4-methyl-N-(3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-pyridin-3-ylpyrimidin-2-yl)amino)benzamide
  • Aniline Compounds
  • Antineoplastic Agents
  • Benzamides
  • Nitriles
  • Piperazines
  • Pyrimidines
  • Quinolines
  • Thiazoles
  • bosutinib
  • Imatinib Mesylate
  • Protein-Tyrosine Kinases
  • Dasatinib