MYCOPHENOLATE SODIUM37415-62-6

Mycophenolate sodium, an immunosuppressive agent, was launched in Switzerland as an oral treatment in combination with Neoraland corticosteroids for the prevention of acute transplant rejection in adult patients receiving allogeneic renal transplantation. In contrast to the previously marketed product mycophenolate mofetil (MMF, CellCept), which is a prodrug and must be converted to mycophenolic acid (MPA) in vivo, Myforticcontains MPA itself as the active ingredient. Myforticwas designed to enhance the therapeutic efficacy of MPA through increased tolerability relative to systemic exposure. Unlike MMF, which is absorbed in the stomach, the enteric-coated formulation of MPA sodium is mainly absorbed in the small intestine, thus protecting the upper GI tract from the side effects of MPA. MPA is an inhibitor of inosine monophosphate dehydrogenase (IMDPH), a vital enzyme in the de novo pathway of purine biosynthesis. Proliferating lymphocytes rely principally on this pathway for purine production,thus rendering them succeptible to depletion of purine bases by MPA. Inhibition of IMPDH by MPA results in the inhibition of both T- and B-lymphocyte proliferation upon antigen challenge and facilitates the prevention of acute graft rejection. Following oral administration of MPA sodium, the tmaxof MPA is 1.5–2 h, with a mean absolute bioavailability of 71% and a mean half-life of 11.7 h. MPA is primarily metabolized in the liver by glucuronidation and excreted mainly in the urine as the metabolite. The recommended dosage regimen of MPA sodium is 720 mg twice daily, which provides equimolar amounts of MPA compared with MMF 1000 mg twice daily. In two major clinical trials in 748 patients, Myforticwas demonstrated to be a highly potent and well-tolerated immunosuppressant for new renal transplant patients. A trend was seen towards fewer dose reductions due to GI intolerability and less serious infections relative to other MPA drugs. The most common adverse events associated with MPA treatment are diarrhea and leukopenia.
ChEBI: An organic sodium salt that is the sodium salt of mycophenolic acid. An immunosuppressant, it is widely used to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases.