Mechanism of action of rapalogues: The antiangiogenic hypothesis

Expert Opinion on Investigational Drugs

Volumn 17, Issue 11, 2008, Pages 1619-1621

  Faivre, Sandrine ^a   Raymond, Eric ^a  

^a BEAUJON HOSPITAL   (France)

Author keywords

mTOR; Rapalogue; Renal cell carcinoma

Indexed keywords

ALPHA INTERFERON; ANGIOGENESIS INHIBITOR; ANTINEOPLASTIC AGENT; BEVACIZUMAB; CYTOTOXIC AGENT; DEFOROLIMUS; EVEROLIMUS; MAMMALIAN TARGET OF RAPAMYCIN; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; RAPALOGUE DERIVATIVE; SORAFENIB; SUNITINIB; TEMSIROLIMUS; UNCLASSIFIED DRUG;

ANGIOGENESIS; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; CANCER CELL; CANCER SURVIVAL; CELL GROWTH; CELL PROLIFERATION; CLINICAL TRIAL; COMBINATION CHEMOTHERAPY; DISEASE MODEL; DRUG EFFICACY; DRUG MECHANISM; EDITORIAL; ENDOTHELIUM CELL; GENE EXPRESSION; HUMAN; KIDNEY CARCINOMA; MONOTHERAPY; NONHUMAN; PROGNOSIS; PROTEIN INTERACTION; SIGNAL TRANSDUCTION; STROMA CELL;

ANGIOGENESIS INHIBITORS; ANIMALS; HUMANS; KIDNEY NEOPLASMS; SIROLIMUS;

EID: 54949134526     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.17.11.1619     Document Type: Editorial

References (18)

1. Faivre S, Delbaldo C, Vera K, et al. Safety, pharmacokinetic, and antitumor activity of SU11248, a novel oral multitarget tyrosine kinase inhibitor, in patients with cancer. J Clin Oncol 2006;24:25-35
2. Escudier B, Eisen T, Stadler WM, et al. TARGET Study Group. Sorafenib in advanced clear-cell renal-cell carcinoma. N Engl J Med 2007;356:125-34
3. Motzer RJ, Hutson TE, Tomczak P, et al. Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med 2007;356:115-24
4. Faivre S, Demetri G, Sargent W, Raymond E. Molecular basis for sunitinib efficacy and future clinical development. Nat Rev Drug Discov 2007;6:734-45
5. Raymond E, Alexandre J, Faivre S, et al. Safety and pharmacokinetics of escalated doses of weekly intravenous infusion of CCI-779, a novel mTOR inhibitor, in patients with cancer. J Clin Oncol 2004;22:2336-47
6. Hidalgo M, Buckner JC, Erlichman C, et al. A phase I and pharmacokinetic study of temsirolimus (CCI-779) administered intravenously daily for 5 days every 2 weeks to patients with advanced cancer. Clin Cancer Res 2006;12:5755-63
7. Atkins MB, Hidalgo M, Stadler WM, et al. Randomized phase II study of multiple dose levels of CCI-779, a novel mammalian target of rapamycin kinase inhibitor, in patients with advanced refractory renal cell carcinoma. J Clin Oncol 2004;22:909-18
8. Hudes G, Carducci M, Tomczak P, et al. Global ARCC Trial. Temsirolimus, interferon alfa, or both for advanced renal-cell carcinoma. N Engl J Med 2007;356:2271-81
9. Jac J, Giessinger S, Khan M, et al. A phase II trial of RAD001 in patients with metastatic renal cell carcinoma [abstract 5107]. ASCO Annual Meeting Proceedings. J Clin Oncol 2007;25:18S
10. Brenner W, Farber G, Herget T, et al. Loss of tumor suppressor protein PTEN during renal carcinogenesis. Int J Cancer 2002;99:53-7
11. Velickovic M, Delahunt B, McIver B, Grebe SK. Intragenic PTEN/MMACl loss of heterozygosity in conventional (clear-cell) renal cell carcinoma is associated with poor patient prognosis. Mod Pathol 2002;15:479-85
12. Kim HL, Seligson D, Liu X, et al. Using tumor markers to predict the survival of patients with metastatic renal cell carcinoma. J Urol 2005;173:1496-501
13. Hamada K, Sasaki T, Koni PA, et al. The PTEN/PI3K pathway governs normal vascular development and tumor angiogenesis. Genes Dev 2005;19:2054-65
14. Guba M, Von Breitenbuch P, Steinbauer M, et al. Rapamycin inhibits primary and metastatic tumor growth by antiangiogenesis: involvement of vascular endothelial growth factor. Nat Med 2002;8:128-35
15. Arsham AM, Plas DR. Thompson CB, Simon MC. Phosphatidylinositol 3-kinase/ Akt signaling is neither required for hypoxic stabilization of HIF-1 alpha nor sufficient for HIF-1-dependent target gene transcription. J Biol Chem 2002;277:15162-70
16. Le Tourneau C, Raymond E, Faivre S. Sunitinib: a novel tyrosine kinase inhibitor. A brief review of its therapeutic potential in the treatment of renal carcinoma and gastrointestinal stromal tumors (GIST). Ther Clin Risk Man 2007;3:341-8
17. Thomas GV, Tran C, Mellinghoff IK, et al. Hypoxia-inducible factor determines sensitivity to inhibitors of mTOR in kidney cancer. Nat Med 2006;12:122-7
18. Faivre S, Kroemer G, Raymond E. Current development of mTOR inhibitors as anticancer agents. Nat Rev Drug Discov 2006;5:671-88