PMID- 20179227 OWN - NLM STAT- MEDLINE DCOM- 20100520 LR - 20220409 IS - 1557-3265 (Electronic) IS - 1078-0432 (Print) IS - 1078-0432 (Linking) VI - 16 IP - 5 DP - 2010 Mar 1 TI - Everolimus. PG - 1368-72 LID - 10.1158/1078-0432.CCR-09-1314 [doi] AB - Everolimus, an orally administered rapamycin analog, has recently been approved by the U.S. Food and Drug Administration for treatment of renal cell carcinoma (RCC) refractory to inhibitors of vascular endothelial growth factor (VEGF) receptor signaling. Everolimus significantly increased progression-free survival (median PFS for the everolimus treated group was 4.0 months versus 1.9 months for the placebo group), although tumor regressions were observed only infrequently. Although the target for everolimus, [the serine-threonine kinase mammalian target of rapamycin (mTOR)] is well established, the mechanism by which this agent retards tumor growth is not well defined. Further, biomarkers that predict tumor sensitivity are still elusive. The mechanism of action, preclinical antitumor activity, and clinical activity of everolimus against RCC are reviewed. FAU - Houghton, Peter J AU - Houghton PJ AD - Center for Childhood Cancer, The Research Institute, Nationwide Children's Hospital, Columbus, Ohio 43205, USA. Peter.Houghton@nationwidechildrens.org LA - eng GR - R01 CA077776/CA/NCI NIH HHS/United States GR - CA23099/CA/NCI NIH HHS/United States GR - N01 CM042216/CM/NCI NIH HHS/United States GR - P01 CA023099/CA/NCI NIH HHS/United States GR - P01 CA023099-310011/CA/NCI NIH HHS/United States GR - CA77776/CA/NCI NIH HHS/United States GR - R01 CA077776-11/CA/NCI NIH HHS/United States PT - Journal Article PT - Research Support, N.I.H., Extramural PT - Review DEP - 20100223 PL - United States TA - Clin Cancer Res JT - Clinical cancer research : an official journal of the American Association for Cancer Research JID - 9502500 RN - 0 (Antineoplastic Agents) RN - 9HW64Q8G6G (Everolimus) RN - W36ZG6FT64 (Sirolimus) SB - IM MH - Animals MH - Antineoplastic Agents/*pharmacology MH - Carcinoma, Renal Cell/*drug therapy MH - Clinical Trials as Topic MH - Everolimus MH - Humans MH - Kidney Neoplasms/*drug therapy MH - Sirolimus/*analogs & derivatives/pharmacology PMC - PMC3003868 MID - NIHMS167833 EDAT- 2010/02/25 06:00 MHDA- 2010/05/21 06:00 PMCR- 2011/03/01 CRDT- 2010/02/25 06:00 PHST- 2010/02/25 06:00 [entrez] PHST- 2010/02/25 06:00 [pubmed] PHST- 2010/05/21 06:00 [medline] PHST- 2011/03/01 00:00 [pmc-release] AID - 1078-0432.CCR-09-1314 [pii] AID - 10.1158/1078-0432.CCR-09-1314 [doi] PST - ppublish SO - Clin Cancer Res. 2010 Mar 1;16(5):1368-72. doi: 10.1158/1078-0432.CCR-09-1314. Epub 2010 Feb 23.