Table 3.

Frequency of clinically relevant gatekeeper resistance mutations found in various kinases targeted by kinase inhibitors

DiseaseTargetMutation% Clinical casesConformation for TKI bindingReferences
CMLABLT315I∼20Inactive(25)
GISTKITT670I∼27Inactive(2628)
NSCLCEGFRT790M∼50ActiveThis study
  • Abbreviations: CML, chronic myelogenous leukemia; GIST, gastrointestinal stromal tumor; NSCLC, non–small-cell lung cancer.