Gastrointestinal (GI) adverse events in renal transplant patients are a common cause of mycophenolate mofetil (MMF) dose reductions, which result in an increased risk of graft rejection because of a low immunosuppression. This study investigated whether conversion from MMF to enteric-coated mycophenolate sodium (EC-MPS) in renal transplant patients with serious GI side-effects, alleviated these symptoms and allowed administration of higher doses of EC-MPS. Nineteen renal transplant patients with severe MMF-related GI side-effects underwent a progressive reduction in MMF dose until symptoms disappeared. At this point, 12-h AUC(MMF) was evaluated and patients were shifted to an equimolar dose of EC-MPS. The EC-MPS dose was then progressively increased until the highest recommended dose was reached or GI symptoms re-appeared. Four weeks post-conversion, AUC(EC-MPS) was determined. Conversion led to a mean increase in EC-MPS dose of 68% (P < 0.0001), with a corresponding rise in AUC(0-12) (60.5%, P < 0.0006) associated with significant benefits in terms of both quality of life (Kidney Transplant Questionnaire, P < 0.01) and GI symptoms (Gastrointestinal Symptom Rating Scale, P < 0.0001), using validated questionnaires. In five of 19 patients, the EC-MPS dose could not be increased because of the prompt insurgence of GI symptoms. Renal function and biochemical parameters remained stable post-conversion and no rejection episodes occurred. These findings suggest that, in selected patients, EC-MPS may be better tolerated than MMF when GI symptoms are particularly important and permits higher mycophenolic acid exposure, when required.