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Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
07:42

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays

Published on: September 19, 2018

Tyrosine kinase inhibitors

C Natoli1, B Perrucci, F Perrotti

  • 1Department of Oncology and Neurosciences, Foundation University G. d'Annunzio Medical School, Chieti-Pescara, Italy. natoli@unich.it

Current Cancer Drug Targets
|April 14, 2010
PubMed

Insights

First and second-generation tyrosine kinase inhibitors (TKIs) offer oral cancer treatments. This review examines their mechanisms, clinical activity, and resistance development, a key challenge in cancer research.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Tyrosine kinase inhibitors (TKIs) represent a significant advancement in cancer therapy.
  • These orally available drugs target critical signaling pathways in various neoplasms.
  • TKIs have gained worldwide approval for treating lung, breast, kidney, pancreatic cancers, GIST, and CML.

Purpose of the Study:

  • To review the most relevant first and second-generation TKIs.
  • To explore their molecular mechanisms of action against receptor and nonreceptor tyrosine kinases.
  • To discuss clinical activity and the challenge of acquired resistance.

Main Methods:

  • Comprehensive literature review of TKIs.
  • Analysis of molecular mechanisms in in vitro and in vivo models.
  • Evaluation of clinical data on efficacy and resistance.

Main Results:

  • First and second-generation TKIs demonstrate significant clinical efficacy across multiple cancer types.
  • Understanding molecular mechanisms is crucial for optimizing TKI therapy.
  • Drug resistance remains a major hurdle, necessitating further research.

Conclusions:

  • TKIs are vital, well-tolerated oral agents for treating diverse cancers.
  • Further research into TKI mechanisms and resistance is essential for improving patient outcomes.

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