Everolimus is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.

The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that, as part of two distinct complexes (mTORC1 and mTORC2), plays pivotal roles in intracellular signaling.Everolimus is a hydroxyethyl ether rapamycin derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.It also acts as an immunosuppressive agent in the context of organ transplantation.