Diffuse large B-cell lymphoma (DLBCL) is the most common type of lymphoma in the western world. Current treatment regimens result in curing approximately 50% to 60% of patients with DLBCL. In 2006, the Food and Drug Administration approved rituximab for use in the first-line treatment of patients with DLBCL in combination with anthracycline-based chemotherapy regimens. Since then, no other agents have been approved for the treatment of DLBCL. This article reviews recent data on the most promising agents in development for the treatment of DLBCL.