Mycophenolate mofetil is an immunosuppressive prodrug of mycophenolic acid used to prevent organ transplant rejection in combination regimens. It carries boxed warnings for embryofetal toxicity, malignancies, and serious infections, and its absorption can be reduced by magnesium/aluminum antacids and some binders.
Steroid- and calcineurin-inhibitor-sparing component of transplant regimens
What to watch for
Diarrhea
Nausea
Vomiting
Known hypersensitivity to mycophenolate mofetil, mycophenolic acid, or formulation components1,3
Pregnancy unless no suitable alternatives and benefits outweigh risks under REMS requirements3
The bottom line
Evidence rating strong. Most-documented uses: prevention of kidney transplant rejection, prevention of heart transplant rejection, prevention of liver transplant rejection. 3 sources indexed (1996–2026), with 2 interaction records on file.
The science
How it works, mechanistically.
Core mechanism
Mycophenolate mofetil is hydrolyzed to mycophenolic acid, a selective, reversible inhibitor of inosine monophosphate dehydrogenase. This blocks de novo guanosine nucleotide synthesis, which T and B lymphocytes rely on heavily for proliferation. Enterohepatic recirculation contributes to exposure, and antacid or binder effects can reduce absorption.1,3
Class
Antiproliferative immunosuppressant
Absorption
Best on an empty stomach
Dosing
Dosing & protocol.
Common range
Kidney transplant adults: commonly 1 g orally twice daily. Heart or liver transplant adults: commonly 1.5 g orally twice daily. Dosing varies by transplant protocol, tolerability, cytopenias, infection, and kidney function.
Recommended form
Oral capsule, tablet, suspension, or supervised intravenous formulation; do not crush tablets or open capsules unnecessarily because of teratogenic handling concerns
Often taken on an empty stomach for consistency, but may be taken with food if needed for gastrointestinal tolerability if the transplant team agrees. Separate from magnesium/aluminum antacids and binders that can reduce absorption.
Safety
Full safety detail.
Side effects
Diarrhea
Nausea
Vomiting
Abdominal pain
Leukopenia
Anemia
Thrombocytopenia
Serious infections
Lymphoma and skin cancers
Pregnancy loss and congenital malformations
Gastrointestinal bleeding or ulceration
Progressive multifocal leukoencephalopathy rarely
Contraindications
Known hypersensitivity to mycophenolate mofetil, mycophenolic acid, or formulation components1,3
Pregnancy unless no suitable alternatives and benefits outweigh risks under REMS requirements3
Avoid live vaccines during significant immunosuppression
Use caution with active serious infection, severe cytopenias, gastrointestinal ulcer disease, or hypoxanthine-guanine phosphoribosyltransferase deficiency3,2
Magnesium/aluminum antacids can reduce mycophenolate absorption and lower mycophenolic acid exposure; ordinary magnesium supplements are less directly studied but should not be taken simultaneously without transplant-team instructions.
Recommendation: Separate magnesium-containing products from mycophenolate by at least 2 hours unless the transplant team gives different instructions.
Numbered references. Citations throughout the page link here.
Randomized controlled trials
1
1A blinded, randomized clinical trial of mycophenolate mofetil for the prevention of acute rejection in cadaveric renal transplantationNeeds reviewNo linkThe Tricontinental Mycophenolate Mofetil Renal Transplantation Study Group · Transplantation · 1996
Pivotal transplant trials established efficacy for rejection prophylaxis.
Reviews & position papers
1
2KDIGO Clinical Practice Guideline for the Care of Kidney Transplant RecipientsNeeds reviewNo linkKidney Disease: Improving Global Outcomes · American Journal of Transplantation · 2009
Guideline supports monitoring blood counts, infections, malignancy prevention, and drug interactions in transplant care.
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