KRAS is the most common mutated oncogene in human cancers and the incidence of KRAS mutation-positive cancers has been on the rise.The lack of a classical drug binding site for KRAS has led to the fact that inhibitor drugs targeting KRAS have been challenging.With the advent of K-RasG12C inhibitors,the myth that KRAS is undruggable has been dispelled.The two K-RasG12C inhibitors currently marketed globally are AMG-510 and MRTX849,which still face a huge demand for use.Understanding successful marketed drugs facilitates better development of new drugs.This review summarises and discusses the research on the two marketed K-RasG12C inhibitors and the resistance mechanism studies faced by this target,and summarises the ways in which K-RasG12C inhibitors can be used in combination with other therapies to overcome drug resistance.
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