Mycophenolate mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphatedehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively.
Inosine monophosphate dehydrogenase II, IC50:27 nM
描述
Mycophenolate mofetil (MMF) is a relatively new systemic immunosuppressive agent used in the field of dermatologic[3]. It is the morpholinoethylester prodrug of mycophenolic acid, an agent that inhibits the proliferation of B and T lymphocytes through noncompetitive, reversible inhibition of inosine monophosphate dehydrogenase, a key enzyme in the de novo synthetic pathway of guanine nucleotides. Mycophenolate mofetil is approved for the prevention of acute renal allograft rejection when given in combination with cyclosporine and steroids[4]. A phase I clinical trial showed MMF was well tolerated in renal transplant patients at doses up to 3,500 mg/day for up to two years. There was no correlation between the incidence of adverse effects and dose of MMF, and no overt nephrotoxicity, hepatotoxicity, or myelotoxicity was observed. In a large multicenter trial, MMF in combination with cyclosporine and prednisone was superior to a standard immunosuppressive regimen including azathioprine[5].
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