The development of new, safe, and effective anti-inflammatory drugs represents a major challenge for the pharmaceutical industry, as well as a significant opportunity. The increasing prevalence of chronic inflammatory and autoimmune diseases associated with an aging population has led to an intense effort to discover new anti-inflammatory drug targets and drugs acting against them. This review highlights the recent progress made in developing therapies directed against an endothelial cell adhesion molecule called vascular adhesion protein (VAP)-1 for the treatment of chronic inflammatory disease as well as highlighting other therapeutic opportunities offered by this vascular target.