Imatinib mesilate for the treatment of gastrointestinal stromal tumour

Expert Opin Pharmacother. 2008 May;9(7):1211-22. doi: 10.1517/14656566.9.7.1211.


Background: The molecular hallmark of gastrointestinal stromal tumours (GISTs), the mutation of the KIT gene, was discovered 10 years ago. GISTs have since been recognized as separate pathological entities among sarcomas, and have become a model for targeted treatment of solid tumours. Imatinib mesilate, which was approved in 2002 for the treatment of patients with advanced GIST, has dramatically changed the course of the disease.

Objective: This article will focus on the development of imatinib mesilate in the treatment of patients with GIST.

Methods: A Pubmed search was performed using the keywords 'imatinib', 'gastrointestinal stromal', 'GIST', 'KIT' and 'PDGFR'. Websites of the American Society of Clinical Oncology and the European Society of Medical Oncology were searched for data reported in abstract form at recent symposiums. Personal communications from opinion leaders were sought for additional information that might be relevant.

Results: Imatinib has changed the clinical course of patients with advanced GISTs and further development in the adjuvant setting as well as prospective assessment of predictive factors are the current focus of ongoing research.

Publication types

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

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Benzamides
  • Controlled Clinical Trials as Topic
  • Drug Delivery Systems
  • Drug Resistance, Neoplasm
  • Gastrointestinal Stromal Tumors / drug therapy*
  • Gastrointestinal Stromal Tumors / epidemiology
  • Gastrointestinal Stromal Tumors / physiopathology
  • Humans
  • Imatinib Mesylate
  • Mutation
  • Piperazines / pharmacology
  • Piperazines / therapeutic use*
  • Proto-Oncogene Proteins c-kit
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use*


  • Antineoplastic Agents
  • Benzamides
  • Piperazines
  • Pyrimidines
  • Imatinib Mesylate
  • Proto-Oncogene Proteins c-kit