Cyclosporine Formulations

Abstract

Borel et al in 1972 discovered the immunosuppressive properties of cyclosporine (CyA) and since then this fungal metabolite extracted from Tolypocladium inflatum, has revolutionized the field of clinical transplantation. Approved in 1983 by Food and Drug Administration (FDA) for widespread clinical use, this drug has improved the graft survival and has been the cornerstone in most immunosuppression protocols. The more selective inhibition of T lymphocyte immunity by CyA was unique when it was discovered compared to its predecessor drugs like steroids and azathioprine. Since its use in clinical practice, marked improvements in outcome have been accomplished in one year and in chronic renal allograft survival and routinely successful heart, liver, pancreas, and lung transplants are possible. Cyclosporine is a cyclic polypeptide consisting of 11 aminoacids and molecular weight of approximately 1200 (C₆₂ H₁₁₁ N₁₁ 0₁₂) The cyclic structure is necessary for its immunosuppressive effect.