BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition

BI-3406 是一种强效且选择性的 SOS1-KRAS 相互作用抑制剂,可通过联合 MEK 抑制有效治疗 KRAS 驱动的癌症

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作者:Marco H Hofmann #, Michael Gmachl #, Juergen Ramharter #, Fabio Savarese, Daniel Gerlach, Joseph R Marszalek, Michael P Sanderson, Dirk Kessler, Francesca Trapani, Heribert Arnhof, Klaus Rumpel, Dana-Adriana Botesteanu, Peter Ettmayer, Thomas Gerstberger, Christiane Kofink, Tobias Wunberg, Andreas Z

Significance

To date, there are no effective targeted pan-KRAS therapies. In-depth characterization of BI-3406 activity and identification of MEK inhibitors as effective combination partners provide an attractive therapeutic concept for the majority of KRAS-mutant cancers, including those fueled by the most prevalent mutant KRAS oncoproteins, G12D, G12V, G12C, and G13D.See related commentary by Zhao et al., p. 17.This article is highlighted in the In This Issue feature, p. 1.

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