Temsirolimus (also called CCI-779) is an inhibitor of mammalian target of rapamycin (mTOR), a serine/threonine protein kinase. Temsirolimus, the C-42 hydroxyl group ester analog of rapamycin [
R0097], possesses better water solubility. Similarly to rapamycin, temsirolimus forms a complex with FK506-binding protein-12 (FKBP-12), and this complex binds and specifically acts as an allosteric inhibitor of mTOR. Inhibition of mTOR activity interferes with tumor angiogenesis,and resulted in a G1 growth arrest in treated tumor cells.
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