Discovery of Selective and Potent KRAS G12D Inhibitors as Potential Therapy in Cancer.

Recent studies reveal that nearly one in seven human cancers exhibit KRAS alterations, contributing to an estimated 19.3 million new cancer cases worldwide in 2020. To date, no marketed mutant-selective and potent KRAS G12D inhibitors are available. The current Patent Highlight presents compounds that directly bind to KRAS G12D , selectively inhibiting its activity. These compounds possess a favorable therapeutic index, stability, bioavailability, and toxicity profile, suggesting potential utility in cancer therapeutics.