Cyclosporine: A Review

Abstract

The discovery and use of cyclosporine since its inception into clinical use in the late 1970s has played a major role in the advancement of transplant medicine. While it has improved rates of acute rejection and early graft survival, data on long-term survival of renal allografts is less convincing. The finding of acute reversible nephrotoxicity and nephrotoxicity in nonrenal transplants has since led to the widely accepted view that there is a chronic more irreversible component to this agent as well. Since that time, there has been intense interest in finding protocols which seek to minimize and even avoid the use of calcineurin inhibitors altogether. We seek to review cyclosporine in terms of its mechanism of action, pathophysiologic, and histologic features associated with acute and chronic nephrotoxicity and recent studies looking to avoid its toxic side effects.

TMBIM6 (transmembrane BAX inhibitor motif containing 6) enhances autophagy and reduces renal dysfunction in a cyclosporine A-induced nephrotoxicity model

“…[52][53][54][55] Significant alterations of autophagy 19,56 have been reported in CsA-associated nephrotoxicity. CsA-induced renal injury is frequently observed in renal tubular structure including proximal tubules.…”

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“…CsA is a potent immune suppressant that induces its biological effects by forming an initial complex with cytosolic proteins termed immunophilins. These drug immunophilin complexes then bind to and inhibit the serine/threonine protein phosphatase calcineurin (CaN) 8 .…”

Development and Validation of a HPLC Method for Dissolution and Stability Assay of Liquid-Filled Cyclosporine Capsule Drug Products

“…It reduces the activity of the immune system by interfering with the activity and growth of T cells (2). Currently, cyclosporine is marketed as liquid-filled capsules and solution for oral administration, solution for injection, and emulsion for ophthalmic administration (3).…”