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Mycophenolate mofetil

Mycophenolate mofetil is a salt form of the immunosuppressive drug mycophenolic acid. The salt form is much better tolerated and allows good and rapid absorption by the body before it is converted to the active agent mycophenolic acid.

Mycophenolic acid acts by inhibiting lymphocyte proliferation and antibody production; hence it is used primarily in immunosuppressive regimens in solid organ transplantations. More recently, mycophenolic mofetil has been used to treat various non-transplant-related conditions, including the following autoimmune skin disorders:

Mycophenolic mofetil is available in both oral and intravenous preparations. The trade name in New Zealand is CellCept® and is currently registered for the prophylaxis of acute organ rejection in patients receiving allogeneic transplants.

• Cutaneous lupus erythematosus
• Psoriasis
• Atopic dermatitis
• Pyoderma gangrenosum
• Sarcoidosis
• Cutaneous vasculitis
• Necrobiosis lipoidica
• Blistering diseases including:
  • Pemphigus vulgaris
  • Pemphigus foliaceus
  • Paraneoplastic pemphigus
  • Bullous pemphigoid
  • Linear IgA bullous dermatosis
  • Epidermolysis bullosa acquisita

How to use mycophenolic mofetil

For the treatment of skin diseases, mycophenolic mofetil is used either alone or in combination with other immunosuppressive agents such as ciclosporin and corticosteroids.

Because it is absorbed well, it is commonly given orally, usually in divided doses. Doses range from 1 to 1.5 g twice daily for the treatment of psoriasis and most other skin diseases (up to maximum dose of 3g daily). When the psoriasis or skin condition begins to improve, the dose can be decreased to 1g daily in divided doses.

Mycophenolic mofetil may affect blood count, particularly if doses are greater than 3 g daily. It is important to measure complete blood count (CBC) after the first week or two of therapy. If results of several measurements are satisfactory and the patient is on a stable dosage, monthly monitoring should be continued.

Side Effects

Mycophenolic mofetil appears to be well tolerated and to have fewer side effects than other immunosuppressive agents. Most side effect studies have been carried out in large groups of transplant patients. Considering the doses used in transplantation are greater than those used for skin disease, mycophenolic mofetil is usually very well tolerated in patients being treated for skin disease.

The most common side effects experienced are gastrointestinal symptoms such as nausea, vomiting and diarrhoea. These are more common with dosages greater than 3 g daily but have been reported in 20% or more of patients receiving 2 g daily. Lowering the daily dose or dividing the daily dose to give smaller but more frequent doses can often minimize these side effects.

Another side effect is the slightly increased risk of viral infections including uncomplicated herpes simplex and herpes zoster. However, this appears to be more common in transplant recipients receiving mycophenolic mofetil as part of a combination immunosuppressive regimen.

Drug Interactions

Mycophenolic mofetil does not seem to interact with other immunosuppressive agents. Drugs that do interact with mycophenolic mofetil are colestyramine and antacids. These drugs decrease the blood levels of mycophenolic mofetil. The coadministration of mycophenolic mofetil with aciclovir increases the blood levels of aciclovir.

Drugs such as probenecid that interfere with renal tubular secretion and glomerular filtration can increase the blood levels of mycophenolic mofetil as these mechanisms are used for the renal removal of the drug.