Mycophenolate mofetil (MMF) inhibits purine synthesis by inhibiting inosine-5′-monophosphate dehydrogenase. Since 1995, it has been approved in the USA for the prevention of allograft rejection in solid organ transplant patients. In the last two decades, it has been frequently used as an immunosuppressive therapy for numerous autoimmune conditions including lupus nephritis. Management of lupus nephritis has been advanced by well-designed randomized clinical trials establishing MMF as a viable alternative to established therapies such as pulse intravenous cyclophosphamide in selected patients. This article outlines the pharmacologic properties of MMF and summarizes recent randomized clinical trials in lupus nephritis.