Recent studies have shown that fatty acid binding protein (FABP) not only participates in lipid metabolism, but also has many other biological functions, including regulating the generation and development of pain. The mechanism of FABP regulating pain is very complex. The structure and function of FABP, its influence on pain and underlying mechanism, as well as the application and effect of FABP inhibitors are summarized here. Different subtypes of FABP have different structures and different mechanisms for pain regulating. They mainly activate pain‑related receptors, regulate the metabolism of cannabinoid and other pain‑related molecules, affect inflammatory signaling pathways, and then affect the generation and development of pain. The inhibition of FABP has also become a new target for the development of analgesic drugs. FABP inhibitors emerged and achieved certain analgesic effects in animal models, providing a new direction for the development of potential analgesic targets.