Prophylaxis of organ rejection in patients undergoing heart, kidney, and liver transplantation.

Mycophenolate mofetil is an ester prodrug of mycophenolic acid(MPA). MPA inhibits inosine monophosphate dehydrogenase (IMPDH), a vital enzyme in the de novo pathway of purine biosynthesis. T and B-lymphocytes are dependent on this pathway for proliferation.

Oral bioavailability: about 50% in early renal transplant patients(＜40 days post), ＞90% in stable patients. Mycophenolate mofetil is rapidly hydrolyzed to active MPA. MPA undergoes first-pass effect and is primarily metabolized in the liver by glucuronyl transferase to an inactive metabolite, MPA glucuronide. MPA protein binding: 97%. Elimination half-life of MPA: 11.7 hr.

Hypersensitivity to mycophenolic acid or mycophenolate mofetil

D

not recommended

Diarrhea (31%), nausea, vomiting, GI tract hemorrhage, leukopenia, infection related to immunosuppression, lymphoma

1 gm PO BID on an empty stomach