Gastrointestinal Stromal Tumors (GISTs) Medication

Updated: Sep 28, 2016
  • Author: Michael A Choti, MD, MBA, FACS; Chief Editor: N Joseph Espat, MD, MS, FACS  more...
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Medication Summary

The goals of pharmacotherapy in patients with gastrointestinal stromal tumors (GISTs) are to induce remission, reduce morbidity, and prevent complications. The tyrosine kinase inhibitor (TKI) imatinib is used in unresectable GISTs and metastatic malignant GISTs, and as adjuvant treatment following complete gross resection of GISTs. The TKIs sunitinib and regorafenib are used for GISTS that become unresponsive to imatinib.


Antineoplastics, Tyrosine Kinase Inhibitor

Class Summary

Agents with strong tyrosine-kinase inhibition activity of the bcr-abl abnormality in all cell-cycle phases of gastric tumor cells.

Imatinib mesylate (Gleevec)

Specifically designed to inhibit tyrosine-kinase activity of the bcr-abl kinase in GI stromal tumors. These tumors are characterized by expression of the product of the proto-oncogene c-kit and often harbor gain-of-function KIT mutations, leading to ligand-independent kinase activation. Gleevec inhibits ABL, KIT, and PDGFR tyrosine kinase.

Sunitinib malate (SU-11248, Sutent)

Multikinase inhibitor that targets several tyrosine-kinase inhibitors implicated in tumor growth, pathologic angiogenesis, and metastatic progression. Inhibits platelet-derived growth factor receptors (ie, PDGFR-alpha, PDGFR-beta), vascular endothelial growth factor receptors (ie, VEGFR1, VEGFR2, VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony-stimulating factor receptor type 1 (CSF-1R), and the glial cell-line–derived neurotrophic factor receptor (RET).

Indicated for persons with GISTs whose disease has progressed or who are unable to tolerate treatment with imatinib (Gleevec). Delays median time to tumor progression.

Regorafenib (Stivarga)

Regorafenib is a tyrosine kinase inhibitor. It is indicated for locally advanced, unresectable gastrointestinal stromal tumors that no longer respond to other treatments (eg, imatinib, sunitinib).