Enteric-coated mycophenolate sodium (Myfortic®) is a reversible, noncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor that is approved in the EU, the US and in other countries worldwide for immunosuppressive prophylaxis against graft rejection in adult renal transplant patients. Enteric-coated mycophenolate sodium has a delayed absorption from the gastrointestinal (GI) tract in comparison with mycophenolate mofetil, thereby potentially reducing GI adverse events. In randomized, double-blind trials of de novo and maintenance immunosuppressive therapy in renal transplant patients receiving ciclosporin emulsion-based regimens, enteric-coated mycophenolate sodium was as effective as mycophenolate mofetil in preventing renal graft rejection. Enteric-coated mycophenolate sodium provides an alternative to mycophenolate mofetil in the treatment of de novo renal transplant recipients and ongoing research should indicate whether an intensified dosage regimen can further improve clinical outcomes. Renal transplant patients receiving mycophenolate mofetil maintenance immunosuppressive therapy may be switched to enteric-coated mycophenolate sodium without compromising efficacy. The general tolerability profile of enteric-coated mycophenolate sodium was similar to that of mycophenolate mofetil. Patients selected for GI intolerance associated with mycophenolate mofetil treatment showed reductions in GI symptoms when switched to enteric-coated mycophenolate sodium, while in unselected patients in comparative trials, there was no difference between enteric-coated mycophenolate sodium and mycophenolate mofetil in GI tolerability. Enteric-coated mycophenolate sodium provides an alternative to mycophenolate mofetil in renal transplant patients receiving mycophenolate mofetil maintenance immunosuppressive therapy who have GI symptoms that have not responded to other management strategies, because they may experience improvement if switched to enteric-coated mycophenolate sodium. Thus, in association with ciclosporin-based regimens, enteric-coated mycophenolate sodium is a valuable treatment option for immunosuppressive prophylaxis in adult renal transplant recipients. In stable renal transplant patients, the inhibitory effect of enteric-coated mycophenolate sodium on IMPDH, T-cell proliferation, T-cell activation, lymphocyte subsets and cytokine expression was not significantly different from that of mycophenolate mofetil. Mycophenolic acid (MPA) is released from enteric-coated mycophenolate sodium in the small intestine. In renal transplant patients receiving maintenance immunosuppressive therapy, the exposure to MPA with enteric-coated mycophenolate sodium treatment was equivalent to that seen with mycophenolate mofetil treatment, although the time to maximum plasma concentration was longer, as expected with an enteric-coated formulation. As observed with mycophenolate mofetil, in de novo renal transplant recipients, MPA exposure with enteric-coated mycophenolate sodium was generally lower in the immediate post-transplant period than in the maintenance period, although an intensified dosage regimen early after transplantation increased exposure to MPA. There is considerable interindividual and intraindividual variability in MPA pharmacokinetics with enteric-coated mycophenolate sodium and mycophenolate mofetil. In paediatric patents, MPA exposure with a single dose of enteric-coated mycophenolate sodium was slightly higher than that observed in adult patients. In randomized, double-blind, double-dummy, multinational trials, at recommended dosages, enteric-coated mycophenolate sodium had equivalent efficacy to mycophenolate mofetil in de novo renal transplant recipients, and renal transplant patients receiving maintenance immunosuppressive therapy could be switched from mycophenolate mofetil to enteric-coated mycophenolate sodium without affecting efficacy. Extension studies demonstrated that the efficacy of mycophenolate sodium was maintained in the longer term. Large, prospective, noncomparative studies confirm that de novo renal transplant recipients can be effectively treated with enteric-coated mycophenolate sodium, with low rates of renal graft loss and the establishment of stable renal functioning; renal transplant patients receiving maintenance immunosuppressive therapy switched from mycophenolate mofetil to enteric-coated mycophenolate sodium had low treatment failure rates, with no patient experiencing graft loss, and continuing stable renal function. In randomized, double-blind, multinational trials in de novo renal transplant patients and renal transplant patients receiving maintenance immunosuppressive therapy, the most common adverse events associated with mycophenolate sodium treatment were infections and GI symptoms. There were no significant differences between enteric-coated mycophenolate sodium and mycophenolate mofetil treatment groups in the incidence of general or serious adverse events, except that enteric-coated mycophenolate sodium recipients had a lower rate of serious pneumonia in de novo renal transplant patients and serious infections in renal transplant patients receiving maintenance immunosuppressive therapy. The GI tolerability of enteric-coated mycophenolate sodium was no different to that of mycophenolate mofetil in de novo and renal transplant patients receiving maintenance immunosuppressive therapy in randomized, double-blind, multinational trials. In PROGIS and myTIME studies, in patients who had received renal transplants ≥1 month previously and who were experiencing GI symptoms while receiving mycophenolate mofetil, switching to enteric-coated mycophenolate sodium was associated with a significant reduction in GI symptom scores and an improvement in GI health-related quality of life.