The article provides an updated review of FDA-approved small-molecule kinase inhibitors, highlighting their binding mechanisms and structural features. It discusses the progress in kinase research over the past fifteen years, noting that kinases have become one of the most sought-after targets in pharmacological research, especially for cancer treatment. The review covers 28 approved kinase inhibitors, with a focus on tyrosine kinases, serine/threonine kinases, and lipid kinases. It details the binding modes of these inhibitors, such as reversible and irreversible inhibitors, and their structural interactions with target kinases. The authors also address current challenges in kinase inhibitor development, including the need to explore a broader range of kinases, diversify scaffold structures, and improve selectivity. Future directions include the development of lipid kinase inhibitors, the exploration of novel mechanisms of action, and the potential of irreversible inhibitors. The review concludes by emphasizing the interdisciplinary nature of kinase inhibitor development and the importance of clinical data in guiding future research.The article provides an updated review of FDA-approved small-molecule kinase inhibitors, highlighting their binding mechanisms and structural features. It discusses the progress in kinase research over the past fifteen years, noting that kinases have become one of the most sought-after targets in pharmacological research, especially for cancer treatment. The review covers 28 approved kinase inhibitors, with a focus on tyrosine kinases, serine/threonine kinases, and lipid kinases. It details the binding modes of these inhibitors, such as reversible and irreversible inhibitors, and their structural interactions with target kinases. The authors also address current challenges in kinase inhibitor development, including the need to explore a broader range of kinases, diversify scaffold structures, and improve selectivity. Future directions include the development of lipid kinase inhibitors, the exploration of novel mechanisms of action, and the potential of irreversible inhibitors. The review concludes by emphasizing the interdisciplinary nature of kinase inhibitor development and the importance of clinical data in guiding future research.