Article
Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial.
JAMA oncology - 1 Sept 2021
Wagner Andrew J, Severson Paul L, Shields Anthony F, Patnaik Amita, Chugh Rashmi, Tinoco Gabriel, Wu Guoxian, Nespi Marika, Lin Jack, Zhang Ying, Ewing Todd, Habets Gaston, Burton Elizabeth A, Matusow Bernice, Tsai James, Tsang Garson, Shellooe Rafe, Carias Heidi, Chan Katrina, Rezaei Hamid, Sanftner Laura, Marimuthu Adhirai, Spevak Wayne, Ibrahim Prabha N, Inokuchi Kerry, Alcantar Oscar, Michelson Glenn, Tsiatis Athanasios C, Zhang Chao, Bollag Gideon, Trent Jonathan C, Tap William D
Abstract excerpt
IMPORTANCE: Many cancer subtypes, including KIT-mutant gastrointestinal stromal tumors (GISTs), are driven by activating mutations in tyrosine kinases and may initially respond to kinase inhibitors but frequently relapse owing to outgrowth of heterogeneous subclones with resistance mutations. KIT inhibitors commonly used to treat GIST (eg, imatinib and sunitinib) are inactive-state (type II) inhibitors....
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