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The Sound of Evolution
Everolimus
Mechanism of action:
Everolimus is an mTOR inhibitor and a derivative of rapamycin. Everolimus first binds to intracellular FKBP-12 (FK506-binding protein 12), forming an Everolimus-FKBP-12 complex. This complex inhibits the kinase activity of mTORC1, blocks phosphorylation of downstream signaling molecules, causes cell cycle arrest at the G1 phase, and suppresses cell proliferation.
Reference(s):
1. Kuhn B et al. (2001). Metabolism of sirolimus and its derivative everolimus by cytochrome P450 3A4: insights from docking, molecular dynamics, and quantum chemical calculations. J Med Chem.
2. Krueger DA et al. (2010). Everolimus for subependymal giant-cell astrocytomas in tuberous sclerosis. N Engl J Med.
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