Generic Name |
Temsirolimus | |
---|---|---|
IND |
CCI-779 | |
Brand Name (US) |
Torisel | |
Manufacturer |
Wheth Pharmaceuticals | |
Drug Type |
mTOR inhibitor | |
Delivery |
Intravenous | |
Approval Status |
Approved for a non-GIST cancer | |
Indications |
Kidney cancer | |
Overall Strategy |
Oncogenic Signal Path Based | |
Strategy |
Block KIT Signal Path | |
Drug Category |
mTOR inhibitor |
Temsirolimus is an Intravenous drug approved for use in renal cell carcinoma (kidney cancer). It is not approved for GIST.
mTOR inhibitors interfer with the synthesis of proteins that regulate proliferation, growth and survival of tumor cells. They also inhibit tumor angiogenesis by reducing VEGF.
Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor