Aidan Tomlinson

Oncogenic RAS mutations are among the most common drivers of human cancers, with the KRASQ61H mutation accounting for approximately 10,000 new patients each year in the US alone.  Structure-based drug design efforts focused on interactions with KRASQ61H specific residues and led to the discovery of RMC-0708, an orally bioavailable, bis-macrocyclic, RAS(ON) Q61H-selective, noncovalent, tri-complex inhibitor. The discovery of RMC-0708 further underscores the potential of the TCI platform to identify potent and selective noncovalent inhibitors of mutant RAS(ON) with demonstrated selectivity over wild-type Ras