FAK, a nonreceptor tyrosine kinase, has been recognized as a novel target class for the development of
targeted anticancer agents. Overexpression of FAK is a common occurrence in several solid tumors, in
which the kinase has been implicated in promoting metastases. Consequently, designing and developing
potent FAK inhibitors is becoming an attractive goal, and FAK inhibitors are being recognized as
a promising tool in our armamentarium for treating diverse cancers. This review comprehensively
summarizes the different classes of synthetically derived compounds that have been reported as potent
FAK inhibitors in the last three decades. Finally, the future of FAK-targeting smart drugs that are designed
to slow down the emergence of drug resistance is discussed.