Mycofenolate mofetil (also spelled mycophenolate) is a salt form of the immunosuppressive drug mycofenolic 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 mycofenolic acid.
Mycofenolic acid acts by inhibiting lymphocyte proliferation and antibody production; hence it is used primarily in immunosuppressive regimens in solid organ transplantations. It is rather similar in action to azathioprine, but more specific.
Mycofenolate mofetil is available in both oral and intravenous preparations. The trade name in New Zealand is CellCept® and it is marketed in 250 mg capsules, 500 mg tablets and 5 ml/1 g suspension. It is currently registered and funded on Special Authority application for the prophylaxis of acute organ rejection in patients receiving allogeneic transplants. In April 2011, it was also funded for other indications on specialist application when corticosteroids, azathioprine and cyclosporin have failed or are unsuitable.
Use of mycofenolate for skin diseases
Mycofenolate mofetil has been used to treat various non-transplant-related conditions, including some skin disorders. It is rarely used in New Zealand because of its expense. However, it has been reported to be helpful in the following conditions.
- Connective tissue disorders:
- Blistering diseases:
- Lichen planus
- Pyoderma gangrenosum
- Necrobiosis lipoidica
How to use mycofenolate mofetil
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.
Mycofenolate mofetil may cause anaemia, 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.
Mycofenolate is classified as pregnancy category D, meaning that there is evidence of risk to the fetus. It is best to avoid pregnancy when taking this medicine. However, the drug's potential benefits may outweigh the risks in some women.
Mycofenolate 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, mycofenolate 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, herpes zoster and cytomegalovirus. However, this appears to be more common in transplant recipients receiving mycofenolate mofetil as part of a combination immunosuppressive regimen.
Rarely, fatalities from progressive multifocal leukoencephalopathy have been reported. This is thought due to reactivation of latent John Cunningham polyomavirus.
As with any immunosuppressive treatment, there is concern that longterm treatment might increase the risk of malignancy.
Mycofenolate mofetil does not seem to interact with other immunosuppressive agents. Some drugs decrease the blood levels of mycofenolate mofetil, including rifampicin, colestyramine and antacids. The coadministration of mycofenolate mofetil with aciclovir increases the blood levels of aciclovir.
Drugs such as probenecid and salicylates that interfere with renal tubular secretion and glomerular filtration can increase the blood levels of mycofenolate mofetil as these mechanisms are used for the renal removal of the drug.
Mycofenolate may occasionally reduce the concentration of other drugs including levonorgestrel – the levels of other contraceptive agents appear unchanged.
- Orvis AK, Wesson SK, Breza TS, Church AA, Mitchell CL, Watkins SW. Mycofenolate mofetil in dermatology. J Am Acad Dermatolo 2009;60:183-99.
- Moder KG. Mycofenolate mofetil: new applications for this immunosuppressant. Ann Allergy Asthma Immunol 2003;90:15-20
- Yamauchi PS, Rizk D, Kormeili T, et al. Current systemic therapies for psoriasis: Where are we now? J AM Acad Dermatol 2003;49:S66-77
On DermNet NZ:
- Consumer medicine information – Medsafe
- Medicine data sheets – Medsafe
- Drugs, Herbs and Supplements – MedlinePlus
- Mycofenolate Mofetil – British Association of Dermatologists
- The Emergence of Mycofenolate Mofetilin Dermatology From Its Roots in the World of Organ Transplantation to its Versatile Role in the Dermatology Treatment Room Hyunhee Park, DOJ Clin Aesthet Dermatol. 2011 January; 4(1): 18–27.
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The New Zealand approved datasheet is the official source of information for this prescription medicine, including approved uses and risk information. Check the New Zealand datasheet on the Medsafe website.