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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. (NCI Thesaurus)
| Synonym: | | 42-O-(2-hydroxy)ethyl rapamycin | | | | US brand name: | | Afinitor | | | | Code name: | | RAD001 | | |
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