Mycophenolate mofetil (MMF) has become a popular immunosuppressive agent in pediatric renal transplantation and has helped to address the unique challenges of transplantation in this population. This paper reviews the early studies that proved MMF's efficacy in reducing the risk of acute renal rejection, as well as its safety and tolerability in comparison to azathioprine. Key conclusions about the pharmacokinetics of MMF from studies of MMF alone and in combination with other immunosuppressive therapies are outlined. The importance of therapeutic drug monitoring (TDM) in this population is also explored in this review. Finally, recent studies showing that newer agents used in combination with MMF can further increase efficacy and reduce the risk of adverse events such as posttransplant lymphoproliferative disease are discussed.