The article provides a comprehensive review of kinase inhibitors and kinase-targeted cancer therapies, highlighting recent advances and future perspectives. Over 120 small-molecule kinase inhibitors (SMKIs) have been approved worldwide for various diseases, with nearly 70 specifically for cancer treatment, focusing on targets like the epidermal growth factor receptor (EGFR) family. Kinase-targeted strategies include monoclonal antibodies and their derivatives, such as nanobodies and peptides, as well as innovative approaches like kinase degraders and protein kinase interaction inhibitors. These strategies have shown clinical progress and potential in overcoming resistance, but they face significant challenges, including drug resistance and toxicity when combined with immunotherapy. The review covers the mechanisms of action and targets of recently FDA-approved SMKIs, including their classification based on ATP-competitive, allosteric, and covalent inhibition. It also discusses the development of new targets and emerging kinase inhibition strategies, such as nanobodies, kinase degraders, and protein kinase interaction inhibitors. The article outlines current obstacles and future prospects in kinase inhibition, emphasizing the need for further advancements in kinase inhibition to overcome resistance and improve patient outcomes.The article provides a comprehensive review of kinase inhibitors and kinase-targeted cancer therapies, highlighting recent advances and future perspectives. Over 120 small-molecule kinase inhibitors (SMKIs) have been approved worldwide for various diseases, with nearly 70 specifically for cancer treatment, focusing on targets like the epidermal growth factor receptor (EGFR) family. Kinase-targeted strategies include monoclonal antibodies and their derivatives, such as nanobodies and peptides, as well as innovative approaches like kinase degraders and protein kinase interaction inhibitors. These strategies have shown clinical progress and potential in overcoming resistance, but they face significant challenges, including drug resistance and toxicity when combined with immunotherapy. The review covers the mechanisms of action and targets of recently FDA-approved SMKIs, including their classification based on ATP-competitive, allosteric, and covalent inhibition. It also discusses the development of new targets and emerging kinase inhibition strategies, such as nanobodies, kinase degraders, and protein kinase interaction inhibitors. The article outlines current obstacles and future prospects in kinase inhibition, emphasizing the need for further advancements in kinase inhibition to overcome resistance and improve patient outcomes.