Article
Characterization of KRASG12C inhibitor olomorasib single-agent and combination with activity in KRASG12C-mutant models.
Nature communications - 4 May 2026
Peng Shengbin, Zhang Youyan, Lin Xi, Si Chong, Van Horn Robert Daniel, Dempsey Jack A, Goetz Eva, Evans Robert J, Farber Andrew, Vandekopple Matthew J, Ming Wenyu, Gao Hong, Yu Chungping, Xu Wei Guo, Brown Nicholas E, Dowless Michele S, Pulliam Nicholas, Barda David A, Guo Deqi, Boulet Serge L, Huber Lysian, Capen Andrew, Jones Bonita, Bogner Sarah, Castanares Mark A, Stephens Jennifer Rachelle, Johnson Megan A, Curtis Carmen L, Strelow John M, Xiao Junpeng, Ballard Josh, Bocchinfuso Wayne P, Chalmers Michael J, Wang Jing, Hendle Jorg, Saflor Melbert D, Lagutan Danalyn Manglicmot, Gheyi Tarun, Sarkar Anita, Kearins Margaret, Tung Frances, Ho Joseph, Rodgers Logan, Benach Jordi, Frommelt Anton Joseph, Zhou Lian, Ackermann Bradley L, McCann Denis, Klippel Anke, Buchanan Sean G, Henry James R, Gong Xueqian
Abstract excerpt
The impact of first-generation covalent KRASG12C inhibitors has been reduced due to the development of drug resistance, tolerability and challenges combining with immunotherapy. We designed olomorasib, a next-generation GDP-binding KRASG12C inhibitor, for nanomolar potency as well as selectivity over wild-type inhibition. In both in vitro and in vivo models of KRASG12C -mutant cancers, olomorasib reduces RAS...
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