Article
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
Journal of medicinal chemistry - 22 Dec 2022
Lorthiois Edwige, Gerspacher Marc, Beyer Kim S, Vaupel Andrea, Leblanc Catherine, Stringer Rowan, Weiss Andreas, Wilcken Rainer, Guthy Daniel A, Lingel Andreas, Bomio-Confaglia Claudio, Machauer Rainer, Rigollier Pascal, Ottl Johannes, Arz Dorothee, Bernet Pascal, Desjonqueres Gaëlle, Dussauge Solene, Kazic-Legueux Malika, Lozac'h Marie-Anne, Mura Christophe, Sorge Mickaël, Todorov Milen, Warin Nicolas, Zink Florence, Voshol Hans, Zecri Frederic J, Sedrani Richard C, Ostermann Nils, Brachmann Saskia M, Cotesta Simona
Abstract excerpt
Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from clinical studies of covalent KRASG12C inhibitors. Thus, inhibitors with broad potential for combination treatment and distinct binding modes to overcome resistance mutations may prove beneficial. JDQ443 is an investigational covalent KRASG12C inhibitor derived from structure-based drug design followed by extensive optimization...
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