Article
KIT ATP-Binding Pocket/Activation Loop Mutations in GI Stromal Tumor: Emerging Mechanisms of Kinase Inhibitor Escape.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology - 20 Apr 2024
Mühlenberg Thomas, Falkenhorst Johanna, Schulz Tom, Fletcher Benjamin S, Teuber Alina, Krzeciesa Dawid, Klooster Isabella, Lundberg Meijun, Wilson Lydia, Lategahn Jonas, von Mehren Margaret, Grunewald Susanne, Tüns Alicia Isabell, Wardelmann Eva, Sicklick Jason K, Brahmi Mehdi, Serrano César, Schildhaus Hans-Ulrich, Sievers Sonja, Treckmann Jürgen, Heinrich Michael C, Raut Chandrajit P, Ou Wen-Bin, Marino-Enriquez Adrian, George Suzanne, Rauh Daniel, Fletcher Jonathan A, Bauer Sebastian
Abstract excerpt
PURPOSE: Imatinib resistance in GI stromal tumors (GISTs) is primarily caused by secondary KIT mutations, and clonal heterogeneity of these secondary mutations represents a major treatment obstacle. KIT inhibitors used after imatinib have clinical activity, albeit with limited benefit. Ripretinib is a potent inhibitor of secondary KIT mutations in the activation loop (AL). However, clinical benefit in fourth line...
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