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 KRASG12D inhibitors are available. The current Patent Highlight presents compounds that directly bind to KRASG12D, selectively inhibiting its activity. These compounds possess a favorable therapeutic index, stability, bioavailability, and toxicity profile, suggesting potential utility in cancer therapeutics.