Rapamune

Sirolimus is a potent non-calcineurin inhibiting immunosuppressant. Sirolimus is given after kidney transplant to keep body from rejecting the new kidney. It can cause hyperlipidemias. It has been shown to possess antifungal and antineoplastic properties. Sirolimus is often given in conjunction with cyclosporin. Everolimus A derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties. In cells, everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production. Check for active clinical trials or closed clinical trials using this agent.