Gan to kagaku ryoho. Cancer & chemotherapy
-
Gan To Kagaku Ryoho · Jul 2009
Review[Small-molecule inhibitors against KIT and PDGFRs especially in GISTs].
Gastrointestinal stromal tumors (GISTs) are one of the representative diseases for which we now use small-molecule inhibitors against KIT and PDGFRs. Most GISTs have gain-of-function mutations of the c-kit or PDGFRA gene. The mutations result in constitutive receptor activation, and the activated receptor stimulates downstream signaling pathways. ⋯ Although molecular target therapy has been very effective, secondary resistance to imatinib often develops during long-term imatinib administration. Secondary mutations of the c-kit gene in addition to primary c-kit gene mutation are a major cause of secondary resistance to imatinib. Now, we can use sunitinib for patients with imatinib-resistant GIST.