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KRAS is one of the most important oncology proteins, which can activate multiple downstream signaling pathways. Despite the prevalence of KRAS mutations in approximately 30% of human cancers, it has long been considered to be ‘undruggable’ due to the lack of recognizable binding pockets. This review covers the recent patents (2019–2021) on KRAS G12C  inhibitors, which are mostly highlighted in terms of chemical structures, molecular mechanisms of action, pharmacokinetic properties, and potential clinical applications. The last 3 years have seen a significant breakthrough in the development of KRAS inhibitors. So far, ten compounds entered the clinical trials with  AMG510  being approved by FDA in May 2021 for the treatment of lung cancer. Moreover,  MRTX849  also holds the promise of becoming the next approved drug targeting KRAS G12C . However, it is noteworthy that acquired resistance is expected to arise inevitably. With a potentially effective treatment on the horizon, combination strategies could further enhance the efficacy of KRAS-targeted inhibition. Whatever their strengths or limitations, emerging KRAS G12C  inhibitors will undoubtedly enrich our understanding of KRAS biology and KRAS-targeted therapy, which will shed light on the development of inhibitors targeting other KRAS mutations.

Inhibitors of the GTPase KRAS G12C in cancer: a patent review (2019-2021)