Products
Mycophenolate is commercially available in the form of enteric-coated film-coated tablets (Myfortic). It has been approved in many countries since 2002.
Structure and properties
Mycophenolate is the deprotonated form of mycophenolic acid (C17H20O6, Mr = 320.3 g/mol). It is present in the drug as mycophenolate sodium, a white crystalline powder that is highly soluble in water. Mycophenolic acid is also administered in the form of the prodrug mycophenolate mofetil (CellCept, generic) (see there). Due to its galenics, mycophenolate sodium is absorbed only in the small intestine and was developed for better gastric tolerance. The active ingredient is of natural origin and was originally isolated from an -fungus.
Effects
Mycophenolate (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
For prevention of graft rejection after renal transplantation in combination with ciclosporin and glucocorticoids.
Dosage
According to the SmPC. Treatment is started within two days of transplantation. Tablets are taken twice daily and independently of meals.
Contraindications
- Hypersensitivity
- Pregnancy and lactation
Mycophenolate is a known teratogen. Full precautions can be found in the drug label.
Interactions
Drug-drug interactions have been described with other immunosuppressants, antacids, sevelamer, colestyramine, tubular-secreted agents such as aciclovir, norfloxacin, metronidazole, rifampicin, and oral contraceptives.
Adverse effects
Because of immunosuppression, the risk for infectious diseases is increased and frequent infections are observed. Other common side effects include diarrhea, constipation, vomiting, blood count changes, and sleep disturbances. As with other immunosuppressants, there is a risk of developing skin cancer. Therefore, the skin should be well protected from UV radiation.
