Increased understanding of the immunopathology of inflammatory bowel disease (IBD) has led to the development of targeted therapies and has unlocked a new era in IBD treatment. The development of treatment options aimed at a variety of pathological mechanisms offers new hope for customized therapies. Beyond anti-tumor necrosis factor agents, selective lymphocyte trafficking inhibitors have been proposed as potent drugs for IBD. Among these, vedolizumab has recently been approved for both Crohn’s disease and ulcerative colitis. Numerous other agents for IBD treatment are currently under investigation, including Janus kinase inhibitors, anti-mucosal vascular addressin cell adhesion molecule-1 agents, an anti-SMAD7 antisense oligonucleotide, an anti-interleukin-12/23 monoclonal antibody, and a sphingosine-1-phosphate receptor-1 selective agonist. These agents will likely expand the treatment options available for the management of IBD patients in the future. In this review, we discuss the efficacy and safety of novel agents currently under investigation in IBD clinical trials.