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STI571 (imatinib mesylate): the tale of a targeted therapy

Paul Thambi1, Edward A Sausville

  • 1Developmental Therapeutics Program, National Cancer Institute, National Institutes of Health, Rockville, MD 20852, USA. Paul.Thambi@nih.gov

Anti-Cancer Drugs
|March 20, 2002
PubMed

Insights

STI571, or imatinib mesylate, is a targeted therapy for chronic myelogenous leukemia (CML). This review covers its development, clinical success, and discusses resistance mechanisms and future applications.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Chronic myelogenous leukemia (CML) is a hematologic neoplasm driven by the BCR-ABL tyrosine kinase.
  • Targeted therapy represents a paradigm shift in cancer treatment.
  • STI571 (imatinib mesylate) was developed as a specific inhibitor of the BCR-ABL tyrosine kinase.

Purpose of the Study:

  • To review the pre-clinical and clinical development of STI571 (imatinib mesylate).
  • To discuss the mechanisms of resistance to STI571 in CML.
  • To explore potential future directions and applications of STI571.

Main Methods:

  • Review of pre-clinical studies investigating STI571's mechanism of action and efficacy.
  • Analysis of data from early-phase clinical trials of STI571 in CML patients.
  • Discussion of published research on resistance mechanisms and ongoing clinical investigations.

Main Results:

  • STI571 demonstrated remarkable efficacy in early clinical trials for CML.
  • The drug targets the constitutively active p210BCR-ABL tyrosine kinase.
  • Rapid FDA approval was granted based on promising clinical outcomes.

Conclusions:

  • STI571 (imatinib mesylate) exemplifies successful targeted therapy development in oncology.
  • Understanding resistance mechanisms is crucial for optimizing long-term treatment strategies.
  • Further research may expand STI571's therapeutic potential to other targets and diseases.

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