The number of medications used to manage autoimmune disorders has increased dramatically. These agents-the immunomodulators-have resulted in improvements in patient outcomes and, in some cases, slowing of disease progression. Despite these advances, immunomodulators are also associated with substantial medication-safety concerns. The potential for adverse drug reactions, serious drug-related complications, and medication errors is significant. Pharmacists must be acutely aware of immunomodulators' complexity and associated potential for adverse events. Attention to all aspects of the medication-use process-procurement and storage, prescribing, dispensing, administration, and monitoring-is required to assure that these agents are used in the safest and most efficacious manner.