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Current progress in the field of KRAS drug discovery is a testament to the power of perseverance and innovation in pharmaceutical research. With ongoing clinical trials and the FDA approval of the first targeted KRAS G12C inhibitor, the landscape of cancer treatment is undergoing a significant transformation. Looking forward, the focus is not only on discovering more selective drugs that target different KRAS mutations but also on understanding the complex biology of KRAS inhibition to circumvent resistance mechanisms and improve patient outcomes. The era of direct KRAS targeting has just begun, and the potential for developing more effective cancer treatments is vast and inspiring.