Fibroblast activation protein (FAP) is a type II transmembrane protein, which is over-expressed in cancer-associated fibroblasts (CAFs). CAFs are tumor stromal cells that constitute a major component of cancer volume and are reportedly related to tumorigenesis, angiogenesis, metastasis, promotion of drug resistance and induction of tumor immunity. FAP is widely acknowledged as the signature protein of CAFs. At present, FAP inhibitors (FAPI) have achieved ideal results in tumor PET/computed tomography (CT) imaging. Theoretically, FAP-targeted drugs can inhibit tumor progression. Nonetheless, no satisfactory therapeutic effect has been observed so far, which has impeded their implementation in clinical practice. In this review, we describe the characteristics of FAP and its role in the occurrence and development of cancer. We also highlight the potential value of targeting FAP to improve current diagnostic and therapeutic approaches.