CellCept (mycophenolate mofetil)

CellCept (mycophenolate mofetil) is the 2-morpholinoethyl ester of mycophenolic acid (MPA), an immunosuppressive agent; inosine monophosphate dehydrogenase (IMPDH) inhibitor.



Mechanism of Action

• prolongs the survival of allogeneic transplants (kidney, heart, liver, intestine, limb, small bowel, pancreatic islets, and bone marrow) in animal models.
• reverses ongoing acute rejection in the canine renal and rat cardiac allograft models. 
• inhibits proliferative arteriopathy in experimental models of aortic and cardiac allografts in rats, as well as in primate cardiac xenografts. 
• used alone or in combination with other immunosuppressive agents in these studies. 
• inhibits immunologically mediated inflammatory responses in animal models
• inhibits tumor development and prolong survival in murine tumor transplant models.
• rapidly absorbed following oral administration
• did not inhibit early events in the activation of human peripheral blood mononuclear cells, such as the production of interleukin-1 (IL-1) and interleukin-2 (IL-2)
• blocks the coupling of these events to DNA synthesis and proliferation.
• hydrolyzed to form MPA
• MPA
• is the active metabolite. 
• is a potent, selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH)
• inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into DNA
• MPA has potent cytostatic effects on lymphocytes (because T- and B-lymphocytes are critically dependent for their proliferation on de novo synthesis of purines, whereas other cell types can utilize salvage pathways)
• inhibits proliferative responses of T- and B-lymphocytes to both mitogenic and allospecific stimulation
• Addition of guanosine or deoxyguanosine reverses the cytostatic effects of MPA on lymphocytes. 
• suppresses antibody formation by B-lymphocytes
• prevents the glycosylation of lymphocyte and monocyte glycoproteins that are involved in intercellular adhesion to endothelial cells and may inhibit recruitment of leukocytes into sites of inflammation and graft rejection

Adverse Reactions

• The principal adverse reactions include diarrhea, leukopenia, sepsis, vomiting
• there is evidence of a higher frequency of certain types of infections eg, opportunistic infection
• The adverse event profile associated with intravenous CellCept is similar to oral CellCept.

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