Over the last few years, advances in understanding the pathogenesis of inflammatory bowel disease, together with progress in biotechnology, have led to the availability of several biological drugs that have dramatically changed the therapeutic approach to these disorders. Indeed, several molecules targeting crucial inflammatory cytokines, blocking T-cell activation/proliferation or the recruitment of inflammatory cells into the inflamed bowel, have been discovered and commercialized. However, the increasing use of biological agents has raised some concerns regarding their short- and long-term safety. This review offers a critical evaluation of the efficacy and safety of biological agents in the management of both Crohn's disease and ulcerative colitis. In addition, promising therapeutic options are discussed.