Temsirolimus.
Temsirolimus, an ester of sirolimus (rapamycin), selectively inhibits the kinase mammalian target of rapamycin (mTOR) and consequently blocks the translation of cell cycle regulatory proteins and prevents overexpression of angiogenic growth factors. It has been found to have antitumour activity in patients with relapsed or refractory mantle cell lymphoma (MCL). In addition, patients with advanced renal cell carcinoma (RCC) and a poor prognosis who received a once-weekly intravenous (IV) infusion of temsirolimus 25 mg experienced significant survival benefits compared with patients receiving standard interferon-α (IFN-α) therapy in a large phase III clinical study. In this study, median overall survival was 10.9 versus 7.3 months and objective response rates were 8.6% in temsirolimus recipients versus 4.8% IFN-α recipient group. Temsirolimus monotherapy recipients experienced significantly fewer grade 3 or 4 adverse events and had fewer withdrawals for adverse events than patients receiving IFN-α. The role of temsirolimus in sequential and combination therapy is yet to be found.
Department of Urology SLK-Klinikum Heilbronn, Teaching Hospital of the University of Heidelberg, Am Gesundbrunnen 20, 74074, Heidelberg, Germany.
Michael
M
Schulze
Christian
C
Stock
Massimo
M
Zaccagnini
Dogu
D
Teber
Jens J
JJ
Rassweiler
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D020123:Sirolimus / Q000031:analogs & derivatives* / Q000627:therapeutic use; D058570:TOR Serine-Threonine Kinases / Q000037:antagonists & inhibitors
D000970:Antineoplastic Agents; C401859:temsirolimus; C546842:MTOR protein, human; D058570:TOR Serine-Threonine Kinases; D020123:Sirolimus