 Abstract cancer is the leading cause of death worldwide, and its treatment and outcomes have been dramatically revolutionized by targeted therapies. As the most frequently mutated oncogene, KRAS has attracted substantial attention. The understanding of KRAS is constantly being updated by numerous studies on KRAS in the initiation and progression of cancer diseases. However, KRAS has been deemed a challenging therapeutic target, even undruggable, after drug-targeting efforts over the past four decades. Recently, there have been surprising advances in directly targeted drugs for KRAS, especially in KRAS, G12C, inhibitors, such as AMG510, Soterasib, and MRTX849, adagrasib, which have obtained encouraging results in clinical trials. Excitingly, AMG510 was the first drug-targeting KRAS, G12C, to be approved for clinical use this year. This review summarizes the most recent understanding of fundamental aspects of KRAS, the relationship between the KRAS mutations and tumor. This article was authored by Lame Huang, Xishenghua, Fang Wang, and others. We are article.tv, links in the description below.