The immunosuppressive agent mycophenolate mofetil has been successfully used over the past 10 years to prevent acute allograft rejection after renal transplantation. It has mainly been administered as a fixed dose of mycophenolate mofetil 1000 mg b.i.d. The pharmacokinetics of mycophenolic acid, the active moiety of the prodrug mycophenolate mofetil, show large between-patient variability, and exposure to mycophenolic acid correlates with the risk for acute rejection. This suggests that already excellent clinical results can be further improved by mycophenolate mofetil dose individualization. This review discusses different arguments in favour of individualization of mycophenolate mofetil dose, as well as strategies for managing mycophenolate mofetil therapy individualization, including pharmacokinetic and pharmacodynamic monitoring and dose individualization based on pharmacogenetic information. It is expected that pharmacokinetic monitoring of mycophenolic acid will offer the most effective and feasible tool for mycophenolate mofetil dose individualization.