Clinical Information

Mycophenolate mofetil (CellCept) is an immunosuppressive agent useful in organ transplantation. It is approved for use in renal, hepatic, and cardiac transplants. When mycophenolate mofetil enters the blood, it is immediately metabolized to the active drug, mycophenolic acid (MPA), which inhibits inosine monophosphate dehydrogenase and interferes with the de novo pathway of guanosine nucleotide synthesis selectively in lymphocytes. MPA inhibits proliferative responses of T and B lymphocytes to both mitogenic and allo-specific stimulation. MPA acts in the same fashion as azathioprine, and MPA is suggested as replacement therapy for azathioprine. The drug is deactivated by the hepatic enzyme, uridine diphosphate glucuronosyltransferase to form MPA glucuronide (MPA-G).

The principle clinical problem encountered in MPA therapy is excessive immunosuppression, which predisposes the patient to systemic infection. Measurement of the blood level of MPA and MPA-G can be useful to guide therapy.

Monitoring is recommended before and after making any changes to immunosuppressive therapy or when initiating or discontinuing concomitant medications. Additional monitoring is indicated if the MPA level is not in the therapeutic range or if a major change in health status occurs.