The Story of Imatinib in GIST - A Journey through the Development of a Targeted Therapy

Abstract

The introduction of the tyrosine kinase inhibitor (TKI) imatinib 15 years ago has radically changed the treatment of advanced/metastatic gastrointestinal stroma tumours (GIST). This review describes and discusses the development of this successful targeted therapy. It shows the evolution of imatinib to become the standard first-line treatment for advanced/metastatic GIST, starting from the first dose-finding trials to the pivotal trials. Other themes discussed are the detection of predictive factors, the results of discontinuing treatment and how long the treatment should last. The discoveries described in the development and research of imatinib now serve as models for treating many other cancers. However, there are still unanswered questions, so research into treating GIST with TKI or other compounds continues.