Focal adhesion kinase （FAK） as a crucial component of focal adhesions （FAs） plays an important role in intracellular and extracellular signal transduction. FAK is a non-receptor tyrosine kinase and mainly regulated by integrins，growth factors and G-protein-coupled receptors，which mediates various bioactivities，such as cell migration，invasion，proliferation，differentiation and angiogenesis. A wide array of studies have demonstrated that abnormal expression and activation of FAK were critically involved in the pathogenesis of cardiovascular diseases，hepatic and renal injuries，lipometabolism，immunoregulation and cancer，in which were closely related to poor prognosis. In recent years，with the development of FAK animal models and inhibitors，targeting FAK has been recognized as new treatment for diseases. Most FAK inhibitors show promising preclinical effect

without significant adverse effect and several are undergoing clinical trials. This review summarizes the studies on the role of FAK in diseases and related animal models and inhibitors to clarify the underlying mechanism and therapeutic prospect.