everolimus

Everolimus is a small molecule inhibitor of the mammalian target of rapamycin (mTOR), specifically targeting the mTORC1 complex. It is a derivative of rapamycin (sirolimus) and acts by binding to FKBP-12 to form a complex that inhibits mTORC1 activity. This inhibition leads to reduced cell proliferation, angiogenesis, and glucose uptake by blocking downstream signaling pathways involved in cell cycle progression and survival. Everolimus is used as an antineoplastic agent for various cancers—including advanced hormone receptor-positive breast cancer (in combination with exemestane), neuroendocrine tumors of pancreatic or gastrointestinal/lung origin, advanced renal cell carcinoma after failure of other treatments, subependymal giant cell astrocytoma associated with tuberous sclerosis complex—and as an immunosuppressant to prevent organ transplant rejection (kidney and liver). It was developed by Novartis and approved by the FDA in 2009[1][3][4][5][7].

Brand names

AfinitorAfinitor DisperzZortressVotubiaTorpenz

Other names

40-O-(2-hydroxyethyl)-rapamycin