Products
Mycophenolate mofetil is commercially available in the form of film-coated tablets, capsules, as an injectable, and as a suspension (CellCept, generics). It has been approved in many countries since 1995.
Structure and properties
Mycophenolate mofetil (C23H31NO7, Mr = 433.5 g/mol) exists as a white crystalline powder and is practically insoluble in water. It is the 2-morpholinoethyl ester of mycophenolic acid (MPA). Mycophenolate mofetil is an ester prodrug that is rapidly converted in the body to the active mycophenolic acid. The active ingredient was designed to increase the bioavailability of the acid. The sodium salt of mycophenolic acid, mycophenolate sodium, is also commercially available (Myfortic, Novartis). The active ingredient is of natural origin and was originally isolated from fungus in the late 19th century.
Effects
Mycophenolate mofetil (ATC L04AA06) has immunosuppressive properties. The effects are due to selective, noncompetitive, and reversible inhibition of the enzyme inosine monophosphate dehydrogenase (IMPDH), which is important for the biosynthesis of guanosine. This inhibits DNA synthesis and proliferation of B and T lymphocytes. While active B and T lymphocytes are dependent on this biosynthetic pathway, other cells may use alternative biochemical pathways. This results in a certain selectivity of the substance. Unlike other immunosuppressants, mycophenolic acid is not incorporated into DNA.
Indications
In combination with ciclosporin and glucocorticoids to prevent graft rejection after renal, cardiac, or liver transplantation. Mycophenolate mofetil is also used for other indications but is not officially approved by the authorities for this purpose (off-label).
Dosage
According to the SmPC. Therapy should be started as soon as possible after transplantation. Oral dosage forms are taken twice daily and preferably on an empty stomach.
Contraindications
- Hypersensitivity
- Pregnancy and lactation
- Mycophenolate mofetil is a known teratogen and appropriate precautions must be considered.
Full details can be found in the drug label.
Interactions
Drug-drug interactions have been described with tubular-secreted agents such as aciclovir and ganciclovir, antacids, sevelamer, proton pump inhibitors, colestyramine, rifampicin, antibiotics, and live vaccines. Mycophenolate mofetil undergoes enterohepatic circulation.
Adverse effects
Because of immunosuppression, the risk for infectious disease is increased and frequent infections are observed. Other common adverse effects include diarrhea and vomiting. Mycophenolate mofetil can interfere with blood formation in the bone marrow and cause blood count abnormalities such as anemia. As with other immunosuppressants, there is a risk of developing skin cancer. Therefore, the skin should be well protected from UV radiation.
