Literature DB >> 20179227

Everolimus.

Peter J Houghton1.   

Abstract

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.

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Year:  2010        PMID: 20179227      PMCID: PMC3003868          DOI: 10.1158/1078-0432.CCR-09-1314

Source DB:  PubMed          Journal:  Clin Cancer Res        ISSN: 1078-0432            Impact factor:   12.531


  23 in total

Review 1.  The TOR pathway: a target for cancer therapy.

Authors:  Mary-Ann Bjornsti; Peter J Houghton
Journal:  Nat Rev Cancer       Date:  2004-05       Impact factor: 60.716

Review 2.  TOR signaling in growth and metabolism.

Authors:  Stephan Wullschleger; Robbie Loewith; Michael N Hall
Journal:  Cell       Date:  2006-02-10       Impact factor: 41.582

3.  4E-binding proteins, the suppressors of eukaryotic initiation factor 4E, are down-regulated in cells with acquired or intrinsic resistance to rapamycin.

Authors:  Michael B Dilling; Glen S Germain; Lorina Dudkin; Arun L Jayaraman; Xiongwen Zhang; Franklin C Harwood; Peter J Houghton
Journal:  J Biol Chem       Date:  2002-02-14       Impact factor: 5.157

Review 4.  Growing roles for the mTOR pathway.

Authors:  Dos D Sarbassov; Siraj M Ali; David M Sabatini
Journal:  Curr Opin Cell Biol       Date:  2005-10-13       Impact factor: 8.382

Review 5.  IRS-1: auditing the effectiveness of mTOR inhibitors.

Authors:  John B Easton; Raushan T Kurmasheva; Peter J Houghton
Journal:  Cancer Cell       Date:  2006-03       Impact factor: 31.743

6.  A novel hypoxia-inducible factor-independent hypoxic response regulating mammalian target of rapamycin and its targets.

Authors:  Andrew M Arsham; Jessica J Howell; M Celeste Simon
Journal:  J Biol Chem       Date:  2003-05-30       Impact factor: 5.157

Review 7.  Exploring mammalian target of rapamycin (mTOR) inhibition for treatment of mantle cell lymphoma and other hematologic malignancies.

Authors:  Bertrand Coiffier; Vincent Ribrag
Journal:  Leuk Lymphoma       Date:  2009-12

8.  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.

Authors:  Josep Tabernero; Federico Rojo; Emiliano Calvo; Howard Burris; Ian Judson; Katharine Hazell; Erika Martinelli; Santiago Ramon y Cajal; Suzanne Jones; Laura Vidal; Nicholas Shand; Teresa Macarulla; Francisco Javier Ramos; Sasa Dimitrijevic; Ulrike Zoellner; Pui Tang; Michael Stumm; Heidi A Lane; David Lebwohl; José Baselga
Journal:  J Clin Oncol       Date:  2008-03-10       Impact factor: 44.544

9.  Akt and hypoxia-inducible factor-1 independently enhance tumor growth and angiogenesis.

Authors:  Andrew M Arsham; David R Plas; Craig B Thompson; M Celeste Simon
Journal:  Cancer Res       Date:  2004-05-15       Impact factor: 12.701

10.  Hypoxia regulates TSC1/2-mTOR signaling and tumor suppression through REDD1-mediated 14-3-3 shuttling.

Authors:  Maurice Phillip DeYoung; Peter Horak; Avi Sofer; Dennis Sgroi; Leif W Ellisen
Journal:  Genes Dev       Date:  2008-01-15       Impact factor: 11.361

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  74 in total

1.  High-dose rapamycin induces apoptosis in human cancer cells by dissociating mTOR complex 1 and suppressing phosphorylation of 4E-BP1.

Authors:  Paige Yellen; Mahesh Saqcena; Darin Salloum; Jiangnan Feng; Angela Preda; Limei Xu; Vanessa Rodrik-Outmezguine; David A Foster
Journal:  Cell Cycle       Date:  2011-11-15       Impact factor: 4.534

2.  Rapamycin inhibits cell proliferation in type I and type II endometrial carcinomas: a search for biomarkers of sensitivity to treatment.

Authors:  Victoria L Bae-Jump; Chunxiao Zhou; John F Boggess; Young E Whang; Lisa Barroilhet; Paola A Gehrig
Journal:  Gynecol Oncol       Date:  2010-09-21       Impact factor: 5.482

3.  Targeting of mTORC2 may have advantages over selective targeting of mTORC1 in the treatment of malignant pheochromocytoma.

Authors:  Xiaohua Zhang; Xianjin Wang; Tianyuan Xu; Shan Zhong; Zhoujun Shen
Journal:  Tumour Biol       Date:  2015-02-11

Review 4.  The Enigma of Rapamycin Dosage.

Authors:  Suman Mukhopadhyay; Maria A Frias; Amrita Chatterjee; Paige Yellen; David A Foster
Journal:  Mol Cancer Ther       Date:  2016-02-25       Impact factor: 6.261

Review 5.  Pre-S2 Mutant-Induced Mammalian Target of Rapamycin Signal Pathways as Potential Therapeutic Targets for Hepatitis B Virus-Associated Hepatocellular Carcinoma.

Authors:  Chiao-Fang Teng; Han-Chieh Wu; Woei-Cherng Shyu; Long-Bin Jeng; Ih-Jen Su
Journal:  Cell Transplant       Date:  2017-02-14       Impact factor: 4.064

6.  Everolimus in the treatment of neuroendocrine tumors: efficacy, side-effects, resistance, and factors affecting its place in the treatment sequence.

Authors:  Lingaku Lee; Tetsuhide Ito; Robert T Jensen
Journal:  Expert Opin Pharmacother       Date:  2018-05-24       Impact factor: 3.889

7.  Efficacy of rapamycin against glioblastoma cancer stem cells.

Authors:  M Mendiburu-Eliçabe; J Gil-Ranedo; M Izquierdo
Journal:  Clin Transl Oncol       Date:  2013-09-17       Impact factor: 3.405

8.  A phase I trial of everolimus in combination with 5-FU/LV, mFOLFOX6 and mFOLFOX6 plus panitumumab in patients with refractory solid tumors.

Authors:  Autumn J McRee; Janine M Davies; Hanna G Sanoff; Richard M Goldberg; Stephen Bernard; E Claire Dees; Kimberly Keller; Anastasia Ivanova; Bert H O'Neil
Journal:  Cancer Chemother Pharmacol       Date:  2014-05-13       Impact factor: 3.333

9.  Targeting angiogenesis in metastatic breast cancer.

Authors:  Sangeetha Reddy; Michael Raffin; Virginia Kaklamani
Journal:  Oncologist       Date:  2012-07-27

10.  Targeting TOR dependence in cancer.

Authors:  Matthew R Janes; David A Fruman
Journal:  Oncotarget       Date:  2010-05
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