Mycophenolate

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Information about Mycophenolate[edit source]

Mycophenolate mofetil is an antimetabolite and potent immunosuppressive agent used as adjunctive therapy in prevention of allograft rejection and in the treatment of serious autoimmune diseases.


Liver safety of Mycophenolate[edit source]

Mycophenolate therapy can be associated with mild serum enzyme elevations and it has been linked to rare instances of clinically apparent liver injury.

Mechanism of action of Mycophenolate[edit source]

Mycophenolate (mye" koe fen' o late) mofetil (moe' fe til) is an antimetabolite and immunosuppressive agent that is used widely in the prevention of rejection after organ transplantation as well as in management of patients with serious autoimmune diseases. Mycophenolate blocks de novo purine synthesis via noncompetitive inhibition of inosine monophosphate dehydrogenase (IMPDH). Lymphocytes lack the salvage pathway for purine synthesis and are particularly vulnerable to the inhibitory activity of mycophenolate. The result of the IMPDH inhibition is an inhibition of lymphocyte proliferation and function.

FDA approval information for Mycophenolate[edit source]

Mycophenolate mofetil was approved for use in the United States in 1995 and its current indications are for prevention of organ rejection after transplantation. It is also used off label in therapy of active and recalcitrant forms of autoimmune diseases.

Dosage and administration for Mycophenolate[edit source]

Mycophenolate is available as capsules of 250 mg and tablets of 500 mg in several generic forms and under the brand name CellCept, and as an oral suspension (200 mg/mL) and a powder for injection (500 mg). It is also available as mycophenolic acid in 180 and 360 mg delayed release tablets under the brand name Myfortic. The typical maintenance dose is 1 to 1.5 grams twice daily.

Side effects of Mycophenolate[edit source]

Common side effects include gastrointestinal upset, diarrhea, nausea, headache, fatigue and dizziness. The following drugs used to prevent transplant rejection.

Immunosuppressants

Monoclonal Antibodies

Antithymocyte Globulin

Mycophenolate Resources
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Contributors: Prab R. Tumpati, MD