Article
Preclinical Characterization and Clinical Activity of RNK08954, a Highly Selective and Orally Bioavailable KRASG12D Inhibitor.
Cancer discovery - 1 May 2026
Xie Ling, Xu Chunwei, Si Han, Fu Xiaoshuang, Yang Xiangcai, Jin Jianan, Yu Xiaoqing, Shao Zhiying, Wang Yanling, Chu Tianqing, Zhang Jun, Liang Rong, Meng Rui, Fei Yuchen, Song Haolin, Ying Chenghao, Dai Yan, Wang Yaya, Ei-Hariry Iman, Wang Guoqiang, Ying Weiwen, Song Zhengbo
Abstract excerpt
KRAS G12D is the most prevalent subtype of KRAS mutation across solid tumors, but no drug is available in the clinic. RNK08954 is a potent and selective KRASG12D inhibitor that inhibits proliferation of KRASG12D-mutant cells and demonstrates significant tumor regressions in mouse xenograft models while inhibiting KRAS-mediated signaling. The in vivo effects of RNK08954 are explained by its unique pharmacokinetic...
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