Gastrointestinal Stromal Tumors (GISTs) Medication

Updated: May 24, 2022
  • Author: Michael A Choti, MD, MBA, FACS; Chief Editor: N Joseph Espat, MD, MS, FACS  more...
  • Print

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 inhibitors (TKIs) imatinib or avapritinib are indicated for unresectable GISTs and metastatic malignant GISTs. Evidence of genetic markers for KIT and PDGFRA are essential to determine which therapeutic options are optimal. 


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).

Avapritinib (Ayvakit)

Avapritinib is a tyrosine kinase inhibitor that targets PDGFRA and PDGFRA D842 mutants as well as multiple KIT exon 11, 11/17 and 17 mutants. This results in the inhibition of PDGFRa- and c-Kit-mediated signal transduction pathways and the inhibition of proliferation in tumor cells that express these PDGFRa and c-Kit mutants. It is indicated for adults with unresectable or metastatic GIST harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutations, including PDGFRA D842V mutations.

Ripretinib (Qinlock)

Ripretinib is a broad-spectrum inhibitor or proto-oncogene receptor tyrosine kinase (KIT) and platelet derived growth factor receptor-A (PDGFRA), including wild type, primary, and secondary mutations. It is indicated for advanced GISTs in adults who have received prior treatment with 3 or more kinase inhibitors, including imatinib.