Pharmacology sirolimus

Pharmacology Sirolimus, a macrolide immunosuppressive agent, inhibits both T-lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (interleukin-2, -4, and -15) stimulation and also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK binding protein-12 (FKBP-12), to generate an immunosuppressive complex. 

Paine, M.F., Leung, L.Y., Lim, H.K., Liao, K., Oganesian, A. et al. (2002) Identification of a novel route of extraction of sirolimus in human small intestine roles of metabolism and secretion. The Journal of Pharmacology and Experimental Therapeutics, 301, 174—186. 

Christians, U. and Benet, L.Z. (2004) CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers studies with sirolimus and midazolam. The Journal of Pharmacology and Experimental Therapeutics, 308, 143-155. 

Le Meur, Y., and Marquet, P. (2006) A comparison of the efiect of cyclosporine and sirolimus on the pharmacokinetics of mycophenolate in renal transplant patients. British Journal of Clinical Pharmacology, 62, 477-484. 

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