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

H. Hofmann, Marco; Gmachl, Michael; Ramharter, Jürgen; Savarese, Fabio; Gerlach, Daniel; R. Marszalek, Joseph; P. Sanderson, Michael; Kessler, Dirk; Trapani, Francesca; Arnhof, Heribert; Rumpel, Klaus; Botesteanu, Dana‐Adriana; Ettmayer, Peter; Gerstberger, Thomas; Kofink, Christiane; Wunberg, Tobias; Zoephel, Andreas; Fu, Szu-Chin; L.F. Teh, Jessica; Böttcher, Jark; Pototschnig, Nikolai; Schachinger, Franziska; Schipany, Katharina; Lieb, Simone; P. Vellano, Christopher; C. O’Connell, Jonathan; L. Mendes, Rachel; Moll, Jürgen; Petronczki, Mark; P. Heffernan, Timothy; Pearson, Mark; B. McConnell, Darryl; Kraut, Norbert

doi:10.1158/2159-8290.cd-20-0142

Public

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

Published in Cancer Discovery • Aug 19, 2020

Authors:

Marco H. Hofmann

Michael Gmachl

Jürgen Ramharter

Abstract

Abstract KRAS is the most frequently mutated driver of pancreatic, colorectal, and non–small cell lung cancers. Direct KRAS blockade has proved challenging, and inhibition of a key downstream effector pathway, the RAF–MEK–ERK cascade, has shown limited success because of activation of feedback netwo...

Subject

KRAS

Cancer research

MEK inhibitor

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