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BBO-8520 + pembrolizumab is a combination therapy consisting of BBO-8520, a first-in-class direct and covalent dual inhibitor of KRAS G12C (ON and OFF forms), and pembrolizumab, an anti-PD-1 monoclonal antibody. BBO-8520 binds in the Switch-II/Helix3 pocket of KRAS G12C, covalently modifies the target cysteine, and disables effector binding to both active and inactive forms of KRAS G12C, providing optimal target coverage. This combination aims to simultaneously target cancer cells directly through KRAS inhibition while activating the immune system against the tumor.
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