Gorelick AN

TRK xDFG Mutations Trigger a Sensitivity Switch from Type I to II Kinase Inhibitors

In TRK fusion–positive cancers, TRK xDFG substitutions represent a shared liability for type I TRK inhibitors. In contrast, they represent a potential biomarker of type II TRK inhibitor activity. As all currently available type II agents are multikinase inhibitors, rational drug design should focus on selective type II inhibitor creation