Enteric-coated mycophenolate sodium for transplant immunosuppression

Abstract

Purpose: The pharmacology, pharmacokinetics, drug interactions, clinical efficacy, adverse effects, monitoring, and dosage and administration of enteric-coated (EC) mycophenolate sodium are reviewed.

Summary: EC mycophenolate sodium is the EC salt form of mycophenolic acid (MPA), the active component of the pro-drug, mycophenolate mofetil. EC mycophenolate sodium was developed to reduce the upper-gastrointestinal (GI) effects of mycophenolate mofetil. Unlike oral mycophenolate mofetil, which releases MPA in the stomach, EC mycophenolate sodium releases MPA in the small intestine. The absolute bioavailability of EC mycophenolate sodium is 72%. MPA undergoes hepatic metabolism by glucuronyl transferase to the inactive mycophenolic acid glucuronide (MPAG), the predominant metabolite. The majority of an administered dose of EC mycophenolate sodium is found as MPAG in the urine. The mean terminal half-life of MPA ranges from 8 to 16 hours. EC mycophenolate sodium and mycophenolate mofetil have equivalent mechanisms of action and drug interaction profiles. Thus far, EC mycophenolate sodium has demonstrated similar efficacy and safety to mycophenolate mofetil in two Phase III clinical trials of adult renal transplant recipients. One study demonstrated improved health-related quality of life in patients switched from mycophenolate mofetil to EC mycophenolate sodium. Ongoing Phase IV studies are trying to further determine advantages of the EC product.

Conclusion: EC mycophenolate sodium is a safe and effective immunosuppressive agent approved for use in the prevention of acute rejection after renal transplantation. It offers an excellent addition to the current armamentarium of immunosuppressive drugs for transplant immunosuppression.