Neoral: a microemulsion cyclosporine.

Abstract

Cyclosporine (Sandimmune), introduced in the 1980s, improved patient and graft survival rates primarily by decreasing the frequency and severity of early, acute rejection. Today, the challenge for coordinators and clinicians is to promote long-term clinical stability in transplant recipients. This requires maintaining the cyclosporine blood level within a relatively narrow therapeutic range to ensure adequate and stable immunosuppression, thus reducing the risk of rejection caused by a suboptimal drug level or drug-related toxicity because of a level above the therapeutic range. However, the clinical use of Sandimmune is complicated by low bioavailability and highly variable pharmacokinetics that provide management challenges and can affect clinical outcomes adversely. Neoral, a new oral microemulsion formulation (in capsules and oral solution) of cyclosporine, improves the bioavailability and pharmacokinetics of cyclosporine and reduces inter- and intraindividual pharmacokinetic variability with a safety profile comparable to that of Sandimmune.