Everolimus NEW

Everolimus is a derivative of Sirolimus, also known as 40-O-(2-hydroxyethyl) -rapamycin, or 40-O-(2-hydroxyethyl) -Sirolimus, belongs to the kinase class of drugs that interfere with cell communication and prevent tumor cell growth, and is an oral mammalian rapamycin (mTOR) inhibitor. In the past, it was mainly used to prevent rejection after kidney transplantation and heart transplantation. It is also currently available to treat patients with advanced kidney cancer who have been treated with two inhibitors that inhibit vascular endothelial growth factor receptor kinase, Sunitinib (Sutent, Pfizer) and Sorafenib (Nexavar, Bayer), with less toxic side effects.

Sunitinib and sorafenib are inhibitors of multiple kinases (acting on multiple cell targets), while evolimus blocks the mammalian target of rapamycin (mTOR) specific protein, interfering with the growth, differentiation, and metabolism of cancer cells. This mTOR pathway is dysregulated in some human tumors. Evolimus binds to the intracellular protein FKBP-12 to form an inhibitory complex that inhibits mTOR kinase activity while reducing the activity of mTOR's downstream effector S6 ribosomal protein kinase (S6K1) and eukaryotic extension factor 4E-binding protein (4E-BP). In addition, everolimus inhibits the expression of hypoxia-inducing factors (such as HIF-1) and decreases the expression of vascular endothelial growth factor (VEGF), which has been shown to reduce cell proliferation, angiogenesis and glucose uptake in both in vitro and in vivo.

Everolimus macrolide immunosuppressants; Everolimus is a derivative of rapamycin. Everolimus inhibits cytokine-mediated lymphocyte proliferation.