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Apr. 2, 2024

MK-1084: A Macrocyclic KRAS(G12C) Inhibitor from Merck


oral covalent KRAS(G12C) mutant-selective inhibitor Ph. I for solid tumors as monotherapy/combination with pembrolizumab Structure-informed optimization from Amgen’s sotorasib ACS Spring 2024 meeting presentation Merck/Taiho/Astex


MK-1084 is an oral covalent inhibitor of KRAS(G12C) being developed by Merck (as part of a collaboration with Taiho and Astex), which is currently in a Ph. I trial (NCT05067283) for the treatment of solid tumors either as a monotherapy or in combination with their checkpoint inhibitor immunotherapy pembrolizumab (Keytruda™). The medicinal chemistry story was recently presented at the ACS Spring 2024 meeting in New Orleans, following a presentation of the Ph. I interim results by Merck at ESMO in Oct. 2023.



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