Everolimus

Definition

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. (NCI05)

Also known as 42-O-(2-Hydroxy)ethyl Rapamycin, Afinitor, Certican, EVEROLIMUS, RAD 001, RAD-001, RAD001, Votubia, Zortress — per NCIT

Also identified as

• ATC L01EG02 per RXNORM
• ATC L04AH02 per RXNORM
• NCIT NCIT:C48387 per NCIT
• SCTID 428127005 per RXNORM
• SCTID 428698007 per RXNORM
• UNII 9HW64Q8G6G per RXNORM

Indications