Cyclosporin B, EvoPure is a dihydroxylated metabolite of cyclosporin A (CsA). Cyclosporin B (M-26) and other cyclosporin metabolites have been found to have lower (<10%) immunosuppressant activity than cyclosporin A (CsA). Cyclosporin B and other metabolites have been isolated and characterized but do not appear to have been extensively studied.
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Cyclosporin B (and other cyclosporin A (CsA) metabolites) have lower immunosuppressant activity but most likely operate under the same mechanism as cyclosporin A (CsA) described below.
Cyclosporin A (CsA) immunosuppressant activity stems from its ability to prevent T-cell activation by blocking specific cytokine transcription genes. After entering a T-cell, cyclosporin A (CsA) associates with ubiquitous cytosolic proteins called cyclophilins which aid in protein folding. Cyclosporin A (CsA) : cyclophilin complexes together bind calcineurin, (another cytosolic protein) effectively blocking the pathway to IL-2 gene transcription and T-cell activation.
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Crabtree, G. R., J. Nourse, and L. Timmermann. "The Mechanism of Action of Cyclosporin A and FK506." Clinical Immunology and Immunotherapy (1996): 40-45.www.ncbi.gov. Web. 27 Aug. 2012.
Wang, Paul C. et. al. "Isolation of 10 Cyclosporine Metabolites from Human Bile." Drug Metabolism and Disposition 17.3 (1989): 292-96. Nih.gov. Web. 28 Oct. 2013.
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