Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

@article{Weiss2022DiscoveryPC,
  title={Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C},
  author={Andreas Weiss and Edwige Lorthiois and Louise Barys and Kim S. Beyer and Claudio Bomio-Confaglia and Heather E Burks and Xueying Chen and Xiaoming Cui and Ruben de Kanter and Lekshmi Dharmarajan and Carmine Fedele and Marc Gerspacher and Daniel A Guthy and Victoria Head and Ashley C. Jaeger and Eloisa Jimenez Nunez and Jeffrey D. Kearns and Catherine Leblanc and Sauveur Michel Maira and Jason Murphy and Helen Oakman and Nils Ostermann and Johannes Ottl and Pascal Rigollier and Danielle Roman and Christian Schnell and Richard C Sedrani and Toshio Shimizu and Rowan Stringer and Andrea Vaupel and Hans Voshol and P. J. J. Wessels and Toni Widmer and Rainer Wilcken and Kun Xu and Fr{\'e}d{\'e}ric J. Z{\'e}cri and Anna F Farago and Simona Cotesta and Saskia M Brachmann},
  journal={Cancer Discovery},
  year={2022},
  volume={12},
  pages={1500 - 1517}
}
The structurally unique KRASG12C inhibitor JDQ443 shows potent, mutant-selective antitumor activity in preclinical models as well as in patients, both alone and in combination with the SHP2 inhibitor TNO155. 

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