GIST Treatment – Tyrosine Kinase Inhibitors

FOR US RESIDENTS ONLY

SEND TO A COLLEAGUE |

PRINT PAGE | A A A

Tyrosine Kinase
Inhibitors

GIST Patient Registry

Connect with other healthcare professionals who treat Kit+ GIST

Tyrosine Kinase Inhibitors

KIT mutations and the expanding role
of targeted treatment

In early 1998, Hirota et al¹ and Kindblom et al² independently published their observations of KIT tyrosine kinase mutations in GIST- a ground breaking discovery that defined the biology of the neoplasms. KIT is the most common tumor marker for GIST, with 95% of GISTs staining positive for KIT.³

Tyrosine kinase inhibitors (TKIs) are now accepted as effective systemic treatments for KIT+ GIST.⁴ They are used as adjuvant therapy after surgical resection and for the treatment of unresectable and/or metastatic disease.

TKIs inhibit the phosphorylation (activation) of KIT kinase, thus blocking oncogenic signaling related to KIT mutations.³

The most recent practice guidelines issued by the National Comprehensive Cancer Network (NCCN) support the use of certain TKIs as:

Neoadjuvant treatment, to reduce the size of potentially resectable GISTs
Adjuvant treatment, to reduce the risk of recurrence after resection
Systemic treatment to slow the progression of unresectable and/or metastatic disease⁴

The figure below summarizes the NCCN guidelines for the use of TKIs in the management of KIT+ GIST.

View Chart

Hirota S, Isozaki K, Moriyama Y, et al. Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors. Science. 1998;279(5350):577-580.
Kindblom LG, Remotti HE, Aldenborg F, Meis-Kindblom JM. Gastrointestinal pacemaker cell tumor (GIPACT): Gastrointestinal stromal tumors show phenotypic characteristics of the interstitial cells of Cajal. Am J Pathol. 1998;152(5):1259-1269.
Corless CL, Heinrich MC. Molecular pathobiology of gastrointestinal stromal sarcomas. Annu Rev Pathol Mech Dis. 2008;3:557-586.
National Comprehensive Cancer Network. NCCN Clinical Practice Guidelines in Oncology: soft tissue sarcoma. V.2.2007.

Enroll in the
GIST Registry, an
observational database
designed to collect data
on patients on GIST.

Learn More About
GIST Registry

Related Information