Everolimus (RAD001): an mTOR inhibitor for the treatment of metastatic renal cell carcinoma

References

• Parkin DM, Bray F, Ferlay J, Pisani P. Global cancer statistics, 2002. CA Cancer J. Clin.55(2), 74–108 (2005).
   PubMed Web of Science ®Google Scholar
• Levi F, Ferlay J, Galeone C et al. The changing pattern of kidney cancer incidence and mortality in Europe. BJU Int.101(8), 949–958 (2008).
   PubMed Web of Science ®Google Scholar
• Motzer RJ, Bacik J, Murphy BA, Russo P, Mazumdar M. Interferon-α as a comparative treatment for clinical trials of new therapies against advanced renal cell carcinoma. J. Clin. Oncol.20(1), 289–296 (2002).
   PubMed Web of Science ®Google Scholar
• Choueiri TK, Garcia JA, Elson P et al. Clinical factors associated with outcome in patients with metastatic clear-cell renal cell carcinoma treated with vascular endothelial growth factor-targeted therapy. Cancer110(3), 543–550 (2007).
   PubMed Web of Science ®Google Scholar
• Motzer RJ, Bukowski RM, Figlin RA et al. Prognostic nomogram for sunitinib in patients with metastatic renal cell carcinoma. Cancer113, 1552–1558 (2008).
   PubMed Web of Science ®Google Scholar
• Motzer RJ, Bander NH, Nanus DM. Renal-cell carcinoma. N. Engl. J. Med.335(12), 865–875 ( 1996).
   PubMed Web of Science ®Google Scholar
• Chan DY, Marshall FF. Surgery in advanced and metastatic renal cell carcinoma. Curr. Opin. Urol.8(5), 369–373 (1998).
   PubMedGoogle Scholar
• Coppin C, Le L, Porzsolt F, Wilt T. Targeted therapy for advanced renal cell carcinoma. Cochrane Database Syst Rev.16(2), CD006017 (2008).
   Google Scholar
• Flanagan RC, Mickisch G, Sylvester R et al. Cytoreductive nephrectomy in patients with metastatic renal cancer: a combined analysis. J. Urol.171, 1071–1076 (2004).
   PubMedGoogle Scholar
• Pantuck AJ, Belldegrun AS, Figlin RA. Cytoreductive nephrectomy for metastatic renal cell carcinoma: is it still imperative in the era of targeted therapy? Clin. Cancer Res.13(2 Suppl.), 693S–669S (2007).
   Google Scholar
• Wood CG. Multimodal approaches in the management of locally advanced and metastatic renal cell carcinoma: combining surgery and systemic therapies to improve patient outcome. Clin. Cancer Res.13, 697–702 (2007).
   Google Scholar
• Oudard S, George D, Medioni J, Motzer R. Treatment options in renal cell carcinoma: past, present and future. Ann. Oncol.18(Suppl. 10), X25–X31 (2007).
   PubMed Web of Science ®Google Scholar
• Hutson TE, Figlin RA. Experimental therapy for advanced renal cell carcinoma. Expert Opin. Investig. Drugs17(11), 1693–1702 (2008).
   PubMed Web of Science ®Google Scholar
• Ravaud A, Wallerand H, Culine S et al. Update on the medical treatment of metastatic renal cell carcinoma. Eur. Urol.54(2), 315–325 (2008).
   PubMed Web of Science ®Google Scholar
• Escudier B, Eisen T, Stadler WM et al. Sorafenib in advanced clear-cell renal-cell carcinoma. N. Engl. J. Med.356(2), 125–134 (2007).
   PubMed Web of Science ®Google Scholar
• Motzer RJ, Hutson TE, Tomczak P et al. Sunitinib versus interferon a in metastatic renal-cell carcinoma. N. Engl. J. Med.356(2), 115–124 (2007).
   PubMed Web of Science ®Google Scholar
• Figlin RA, Hutson TE, Tomczak P et al. Overall survival with sunitinib vs. interferon (IFN)-α as first-line treatment of metastatic renal-cell carcinoma (mRCC). J. Clin. Oncol.26(Suppl.), 5024 (2008).
   Web of Science ®Google Scholar
• Hutson TE. Sunitinib (SUTENT®) for the treatment of metastatic renal cell carcinoma. Expert Rev. Anticancer Ther.8(11), 1723–1731 (2008).
   PubMed Web of Science ®Google Scholar
• Hudes G, Carducci M, Tomczak P et al. Temsirolimus, interferon a, or both for advanced renal-cell carcinoma. N. Engl. J. Med.356(22), 2271–2281 (2007).
   PubMed Web of Science ®Google Scholar
• Escudier B, Pluzanska A, Koralewski P et al. Bevacizumab plus interferon α-2a for treatment of metastatic renal cell carcinoma: a randomised, double-blind Phase III trial. Lancet370(9605), 2103–2111 (2007).
   PubMed Web of Science ®Google Scholar
• Rini BI, Halabi S, Rosenberg JE et al. Bevacizumab plus interferon a compared with interferon α monotherapy in patients with metastatic renal cell carcinoma: CALGB 90206. J. Clin. Oncol.26(33), 5422–5428 (2008).
   PubMed Web of Science ®Google Scholar
• Bhojani N, Jeldres C, Patard JJ et al. Toxicities associated with the administration of sorafenib, sunitinib, and temsirolimus and their management in patients with metastatic renal cell carcinoma. Eur. Urol.53(5), 917–930 (2008).
   PubMed Web of Science ®Google Scholar
• Hutson TE, Figlin RA, Kuhn JG, Motzer RJ. Targeted therapies for metastatic renal cell carcinoma: an overview of toxicity and dosing strategies. Oncologist13(10), 1084–1096 (2008).
   PubMed Web of Science ®Google Scholar
• Gollob JA, Rathmell WK, Richmond TM et al. Phase II trial of sorafenib plus interferon α-2b as first- or second-line therapy in patients with metastatic renal cell cancer. J. Clin. Oncol.25, 3288–3295 (2007).
   PubMed Web of Science ®Google Scholar
• Escudier B, Szczylik C, Hutson TE et al. Randomized Phase II trial of first-line treatment with sorafenib versus interferon α-2a in patients with metastatic renal cell carcinoma. J. Clin. Oncol.27(8), 1280–1289 (2009).
   PubMed Web of Science ®Google Scholar
• Motzer RJ, Michaelson MD, Redman BG et al. Activity of SU11248, a multitargeted inhibitor of vascular endothelial growth factor receptor and platelet-derived growth factor receptor, in patients with metastatic renal cell carcinoma. J. Clin. Oncol.24, 16–24 (2006).
   PubMed Web of Science ®Google Scholar
• Motzer RJ, Rini BI, Bukowski RM et al. Sunitinib in patients with renal cell carcinoma. JAMA295(21), 2156–2124 (2006).
   Google Scholar
• Sonpavde G, Hutson TE. Recent advances in the therapy of renal cancer. Expert Opin. Biol. Ther.7(2), 233–242 (2007).
   PubMed Web of Science ®Google Scholar
• Ravaud A, Hawkins R, Gardner JP et al. Lapatinib versus hormone therapy in patients with advanced renal cell carcinoma: a randomized Phase III clinical trial. J. Clin. Oncol.26(14), 2285–2291 (2008).
   PubMed Web of Science ®Google Scholar
• Pascual J. Everolimus in clinical practice – renal transplantation. Nephrol. Dial. Transplant.21(Suppl. 3), iii18–iii23 (2006).
   PubMedGoogle Scholar
• Sánchez-Fructuoso AI. Everolimus: an update on the mechanism of action, pharmacokinetics and recent clinical trials. Expert Opin. Drug Metab. Toxicol.4(6), 807–819 (2008).
   PubMed Web of Science ®Google Scholar
• Yao JC, Phan AT, Chang DZ et al. Efficacy of RAD001 (everolimus) and octreotide LAR in advanced low- to intermediate-grade neuroendocrine tumors: results of a Phase II study. J. Clin. Oncol.26(26), 4311–4318 (2008).
   PubMed Web of Science ®Google Scholar
• Yao JC, Lombard-Bohas C, Baudin E et al. A Phase II trial of daily oral RAD001 (everolimus) in patients with metastatic pancreatic neuroendocrine tumors (NET) after failure of cytotoxic chemotherapy. Ann. Oncol.19(Suppl. 8), viii167 (2008) (Abstract 508PD).
   Google Scholar
• Seeliger H, Guba M, Kleespies A, Jauch KW, Bruns CJ. Role of mTOR in solid tumor systems: a therapeutical target against primary tumor growth, metastases, and angiogenesis. Cancer Metastasis Rev.26(3–4), 611–621 (2007).
   PubMed Web of Science ®Google Scholar
• Cho D, Signoretti S, Regan M, Mier JW, Atkins MB. The role of mammalian target of rapamycin inhibitors in the treatment of advanced renal cancer. Clin. Cancer Res.13(2 Suppl.), 758S–763S (2007).
   PubMed Web of Science ®Google Scholar
• Pantuck AJ, Seligson DB, Klatte T et al. Prognostic relevance of the mTOR pathway in renal cell carcinoma. Implications for molecular patient selection for targeted therapy. Cancer109, 2257–2267 (2007).
   PubMed Web of Science ®Google Scholar
• Boulay A, Zumstein-Mecker S, Stephan C et al. Anti-tumor efficacy of intermittent treatment schedules with the rapamycin derivative RAD001 correlates with prolonged inactivation of ribosomal protein S6 kinase 1 in peripheral blood mononuclear cells. Cancer Res.64(1), 252–261 (2004).
   PubMed Web of Science ®Google Scholar
• Keller K, Daniel C, Schöcklmann H et al. Everolimus inhibits glomerular endothelial cell proliferation and VEGF, but not long-term recovery in experimental thrombotic microangiopathy. Nephrol. Dial. Transplant.21(10), 2724–2735 (2006).
   PubMed Web of Science ®Google Scholar
• Tanaka C, O’Reilly T, Kovarik JM et al. Identifying optimal biologic doses of everolimus (RAD001) in patients with cancer based on the modeling of preclinical and clinical pharmacokinetic and pharmacodynamic data. J. Clin. Oncol.26(10), 1596–1602 (2008).
   PubMedGoogle Scholar
• Tabernero J, Rojo F, Calvo E et al. Dose- and schedule-dependent inhibition of the mammalian target of rapamycin pathway with everolimus: a Phase I tumor pharmacodynamic study in patients with advanced solid tumors. J. Clin. Oncol.26(10), 1603–1610 (2008).
   PubMed Web of Science ®Google Scholar
• Cho D, Signoretti S, Dabora S et al. Potential histologic and molecular predictors of response to temsirolimus in patients with advanced renal cell carcinoma. Clin. Genitourin. Cancer5(6), 379–385 (2007).
   PubMed Web of Science ®Google Scholar
• O’Donnell A, Faivre S, Burris HA 3rd et al. Phase I pharmacokinetic and pharmacodynamic study of the oral mammalian target of rapamycin inhibitor everolimus in patients with advanced solid tumors. J. Clin. Oncol.26(10), 1588–1595 (2008).
   PubMed Web of Science ®Google Scholar
• Strom T, Haschke M, Zhang YL et al. Identification of everolimus metabolite patterns in trough blood samples of kidney transplant patients. Ther. Drug Monit.29(5), 592–599 (2007).
   PubMed Web of Science ®Google Scholar
• Jac J, Amato RJ, Giessinger S, Saxena S, Willis JP. A Phase II study with a daily regimen of the oral mTOR inhibitor RAD001 (everolimus) in patients with metastatic renal cell carcinoma which has progressed on tyrosine kinase inhibition therapy. J. Clin. Oncol.26(15 Suppl.), 5113 (2008).
   PubMedGoogle Scholar
• Whorf RC, Hainsworth JD, Spigel DR et al. Phase II study of bevacizumab and everolimus (RAD001) in the treatment of advanced renal cell carcinoma (RCC). J. Clin. Oncol.26(Suppl.), (2008) (Abstract 5010).
   Google Scholar
• Motzer RJ, Escudier B, Oudard S et al. Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled Phase III trial. Lancet372(9637), 449–456 (2008).
   PubMed Web of Science ®Google Scholar
• Escudier B, Ravaud A, Oudard S et al. Phase-3 randomised trial of everolimus (RAD001) vs placebo in metastatic renal cell carcinoma. Ann. Oncol. (2008) (Epub ahead of print).
   Google Scholar
• Chhajed PN, Dickenmann M, Bubendorf L, Mayr M, Steiger J, Tamm M. Patterns of pulmonary complications associated with sirolimus. Respiration73, 367–374 (2008).
   Google Scholar
• Bellmunt J, Szczylik C, Feingold J, Strahs A, Berkenblit A. Temsirolimus safety profile and management of toxic effects in patients with advanced renal cell carcinoma and poor prognostic features. Ann. Oncol.19(8), 1387–1392 (2008).
   PubMed Web of Science ®Google Scholar
• Zafar Y, Bendell J, Lager J et al. Preliminary results of a Phase 1 study of bevacizumab (BV) in combination with everolimus (E) in patients with advanced solid tumors. J. Clin. Oncol.24(18 Suppl.), 18S (2006) (Abstract 3097).
   Google Scholar
• Manegold PC, Paringer C, Kulka U et al. Antiangiogenic therapy with mammalian target of rapamycin inhibitor RAD001 (everolimus) increases radiosensitivity in solid cancer. Clin. Cancer Res.14(3), 892–900 (2008).
   PubMedGoogle Scholar