Description

Everolimus is a derivative of the natural macrocyclic lactone sirolimus (https://pubchem.ncbi.nlm.nih.gov/compound/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 (https://pubchem.ncbi.nlm.nih.gov/compound/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.