The article reviews the roles and inhibitors of focal adhesion kinase (FAK) in cancer, highlighting its significance in tumor growth, invasion, metastasis, and angiogenesis. FAK, a non-receptor tyrosine kinase, is highly expressed in various tumors and is associated with poor prognosis. Its activation promotes tumor progression through both kinase-dependent and kinase-independent pathways, and it plays a crucial role in maintaining the tumor microenvironment (TME). The inhibition of FAK has shown promise in impeding tumorigenesis, metastasis, and drug resistance. Several FAK inhibitors, including IN10018, defactinib, GSK2256098, contelitinib, and APG-2449, have demonstrated positive anti-tumor effects in preclinical studies and are currently undergoing clinical trials for various types of tumors. The review also discusses the benefits of FAK degraders, particularly their scaffold function, which holds potential for future clinical exploration. The article provides a comprehensive overview of the current status and future prospects of FAK-targeted therapy and combination approaches, offering valuable insights for advancing anti-cancer treatment strategies.The article reviews the roles and inhibitors of focal adhesion kinase (FAK) in cancer, highlighting its significance in tumor growth, invasion, metastasis, and angiogenesis. FAK, a non-receptor tyrosine kinase, is highly expressed in various tumors and is associated with poor prognosis. Its activation promotes tumor progression through both kinase-dependent and kinase-independent pathways, and it plays a crucial role in maintaining the tumor microenvironment (TME). The inhibition of FAK has shown promise in impeding tumorigenesis, metastasis, and drug resistance. Several FAK inhibitors, including IN10018, defactinib, GSK2256098, contelitinib, and APG-2449, have demonstrated positive anti-tumor effects in preclinical studies and are currently undergoing clinical trials for various types of tumors. The review also discusses the benefits of FAK degraders, particularly their scaffold function, which holds potential for future clinical exploration. The article provides a comprehensive overview of the current status and future prospects of FAK-targeted therapy and combination approaches, offering valuable insights for advancing anti-cancer treatment strategies.