Crohn's disease (CD) is a chronic inflammatory condition of the gastrointestinal tract, characterized by overactive T-helper (Th)1-mediated responses towards resident bacterial flora in genetically susceptible individuals. Biotechnological methodology has allowed the development of therapeutic compounds that specifically target single, well-defined pathways, thereby inhibiting abnormal Th1 polarization. These therapies include antibody-based, as well as nucleic-acid related approaches that target various pro-inflammatory cytokines, as well as intracellular signaling pathways. This review summarizes treatments already in clinical use and discusses novel targets that offer additional therapeutic opportunities in the management of CD.