The article reviews the role of the RAS-MAPK signaling pathway in cancer and the development of small-molecule inhibitors targeting this pathway. The RAS-MAPK pathway, which includes the RAS, RAF, MEK, and ERK components, plays a crucial role in regulating cell growth, differentiation, proliferation, apoptosis, and migration. Abnormal activation of this pathway due to mutations in *RAS* or *RAF* genes is a common feature in human cancers. Several small-molecule inhibitors targeting the RAS-MAPK pathway have been developed and are currently being tested in clinical trials. The article discusses the rationale for targeting this pathway, the application of various inhibitory molecules as anticancer agents, and the results of clinical trials. It highlights the importance of analyzing *RAS* and *BRAF* mutations as markers of response to treatments and to avoid paradoxical effects. Further research is needed to understand the complex regulation of the RAS-MAPK pathway in malignant cells and to develop novel combination therapies to overcome resistance.The article reviews the role of the RAS-MAPK signaling pathway in cancer and the development of small-molecule inhibitors targeting this pathway. The RAS-MAPK pathway, which includes the RAS, RAF, MEK, and ERK components, plays a crucial role in regulating cell growth, differentiation, proliferation, apoptosis, and migration. Abnormal activation of this pathway due to mutations in *RAS* or *RAF* genes is a common feature in human cancers. Several small-molecule inhibitors targeting the RAS-MAPK pathway have been developed and are currently being tested in clinical trials. The article discusses the rationale for targeting this pathway, the application of various inhibitory molecules as anticancer agents, and the results of clinical trials. It highlights the importance of analyzing *RAS* and *BRAF* mutations as markers of response to treatments and to avoid paradoxical effects. Further research is needed to understand the complex regulation of the RAS-MAPK pathway in malignant cells and to develop novel combination therapies to overcome resistance.