everolimus

Summary

Summary: A derivative of sirolimus and an inhibitor of TOR SERINE-THREONINE KINASES. It is used to prevent GRAFT REJECTION in heart and kidney transplant patients by blocking cell proliferation signals. It is also an ANTINEOPLASTIC AGENT.

Top Publications

  1. Massard C, Fizazi K, Gross Goupil M, Escudier B. Reflex sympathetic dystrophy in patients with metastatic renal cell carcinoma treated with everolimus. Invest New Drugs. 2010;28:879-81 pubmed publisher
  2. Amzal B, Fu S, Meng J, Lister J, Karcher H. Cabozantinib versus everolimus, nivolumab, axitinib, sorafenib and best supportive care: A network meta-analysis of progression-free survival and overall survival in second line treatment of advanced renal cell carcinoma. PLoS ONE. 2017;12:e0184423 pubmed publisher
    ..study is to evaluate progression-free survival (PFS) and overall survival (OS) of cabozantinib compared to everolimus, nivolumab, axitinib, sorafenib, and best supportive care (BSC) in aRCC patients who progressed after previous ..
  3. Zaza G, Dalla Gassa A, Felis G, Granata S, Torriani S, Lupo A. Impact of maintenance immunosuppressive therapy on the fecal microbiome of renal transplant recipients: Comparison between an everolimus- and a standard tacrolimus-based regimen. PLoS ONE. 2017;12:e0178228 pubmed publisher
    ..Nine patients were treated with everolimus plus mycophenolate mofetil (EVE+MMF group), and 11 patients were treated with a standard therapy with tacrolimus ..
  4. Biscaglia S, Secco G, Tumscitz C, Di Mario C, Campo G. Optical coherence tomography evaluation of overlapping everolimus-eluting bioresorbable vascular scaffold implantation guided by enhanced stent visualization system. Int J Cardiol. 2015;182:1-3 pubmed publisher
  5. Penttilä P, Donskov F, Rautiola J, Peltola K, Laukka M, Bono P. Everolimus-induced pneumonitis associates with favourable outcome in patients with metastatic renal cell carcinoma. Eur J Cancer. 2017;81:9-16 pubmed publisher
    ..We analysed the association of pneumonitis with outcomes in everolimus treated metastatic renal cell carcinoma (mRCC) patients...
  6. Bundhun P, Janoo G, Yanamala C, Huang F. Adverse cardiovascular events associated with biodegradable polymer drug-eluting stents and durable polymer everolimus-eluting stents: A systematic review and meta-analysis of 10 randomized controlled trials. Medicine (Baltimore). 2017;96:e7510 pubmed publisher
    ..We aimed to compare the adverse cardiovascular events associated with BP-DES and durable polymer everolimus-eluting stents (DP-EES) using a large number of patients obtained from randomized controlled trials (RCTs)...
  7. Ravaud A, Gomez Roca C, Picat M, Digue L, Chevreau C, Gimbert A, et al. Phase I study of axitinib and everolimus in metastatic solid tumours and extension to metastatic renal cell carcinoma: Results of EVAX study. Eur J Cancer. 2017;85:39-48 pubmed publisher
    ..Due to a potential favourable safety profile of axitinib (AX), a phase I study combining everolimus (EV) and AX for solid tumours was explored...
  8. Zabala Letona A, Arruabarrena Aristorena A, Martin Martin N, Fernandez Ruiz S, Sutherland J, Clasquin M, et al. mTORC1-dependent AMD1 regulation sustains polyamine metabolism in prostate cancer. Nature. 2017;547:109-113 pubmed publisher
    ..Conversely, samples from a clinical trial with the mTORC1 inhibitor everolimus exhibit a predominant decrease in AMD1 immunoreactivity that is associated with a decrease in proliferation, in ..
  9. Moscarella E, Spitaleri G, Brugaletta S, Sentí Farrarons S, Pernigotti A, Ortega Paz L, et al. Impact of Body Mass Index on 5-Year Clinical Outcomes in Patients With ST-Segment Elevation Myocardial Infarction After Everolimus-Eluting or Bare-Metal Stent Implantation. Am J Cardiol. 2017;120:1460-1466 pubmed publisher
    ..The EXAMINATION trial randomized 1,498 patients with STEMI to a bare-metal stent or an everolimus-eluting stent...

More Information

Publications62

  1. Singh J, Novik Y, Stein S, Volm M, Meyers M, Smith J, et al. Phase 2 trial of everolimus and carboplatin combination in patients with triple negative metastatic breast cancer. Breast Cancer Res. 2014;16:R32 pubmed publisher
    ..Combination of everolimus also known as RAD001 (oral mammalian target of rapamycin (mTOR) inhibitor) and carboplatin may have activity in ..
  2. Kattan J, Kourie H. The use of everolimus to reverse tamoxifen resistance in men with metastatic breast cancer: a case report. Invest New Drugs. 2014;32:1046-7 pubmed publisher
  3. Sorrentino S, Giustino G, Mehran R, Kini A, Sharma S, Faggioni M, et al. Everolimus-Eluting Bioresorbable Scaffolds Versus Everolimus-Eluting Metallic Stents. J Am Coll Cardiol. 2017;69:3055-3066 pubmed publisher
    ..vascular scaffolds (BVS) are associated with an excess of thrombotic complications compared with metallic everolimus-eluting stents (EES)...
  4. Rogers S, Garcia C, Wu S. Discontinuation of Everolimus Due to Related and Unrelated Adverse Events in Cancer Patients: A Meta-Analysis. Cancer Invest. 2017;35:552-561 pubmed publisher
    A meta-analysis of randomized controlled trials (RCTs) was performed to examine the risk of everolimus discontinuation due to related and unrelated adverse events (AE) in cancer patients...
  5. Pavel M, Singh S, Strosberg J, Bubuteishvili Pacaud L, Degtyarev E, Neary M, et al. Health-related quality of life for everolimus versus placebo in patients with advanced, non-functional, well-differentiated gastrointestinal or lung neuroendocrine tumours (RADIANT-4): a multicentre, randomised, double-blind, placebo-controlled, phas. Lancet Oncol. 2017;18:1411-1422 pubmed publisher
    In the phase 3 RADIANT-4 trial, everolimus increased progression-free survival compared with placebo in patients with advanced, progressive, non-functional, well-differentiated gastrointestinal or lung neuroendocrine tumours (NETs)...
  6. Vicier C, Dieci M, Arnedos M, Delaloge S, Viens P, Andre F. Clinical development of mTOR inhibitors in breast cancer. Breast Cancer Res. 2014;16:203 pubmed publisher
    ..Findings from these studies will provide indispensable tools for the design of future clinical trials and identify new perspectives and challenges for researchers and clinicians. ..
  7. Cochin V, Gross Goupil M, Ravaud A, Godbert Y, Le Moulec S. [Cabozantinib: Mechanism of action, efficacy and indications]. Bull Cancer. 2017;104:393-401 pubmed publisher
    ..Cabozantinib increased overall survival (OS) compared with everolimus in patients with advanced renal cell carcinoma who progressed after previous VEGFR ITK treatment: 21...
  8. Suvannasankha A, Chirgwin J. Role of bone-anabolic agents in the treatment of breast cancer bone metastases. Breast Cancer Res. 2014;16:484 pubmed
    ..Recent results from the Breast cancer trials of Oral Everolimus-2 trial suggest that agents such as the mammalian target of rapamycin inhibitor everolimus may have efficacy ..
  9. Buti S, Bersanelli M. Combination therapy in kidney cancer: the next revolution?. Lancet Oncol. 2015;16:1441-1442 pubmed publisher
  10. Pascual T, Apellaniz Ruiz M, Pernaut C, Cueto Felgueroso C, Villalba P, Alvarez C, et al. Polymorphisms associated with everolimus pharmacokinetics, toxicity and survival in metastatic breast cancer. PLoS ONE. 2017;12:e0180192 pubmed publisher
    ..The BOLERO-2 trial showed that everolimus-exemestane achieves increased progression free survival (PFS) compared with exemestane...
  11. Hede K. Gastric cancer: trastuzumab trial results spur search for other targets. J Natl Cancer Inst. 2009;101:1306-7 pubmed publisher
  12. Valdez B, Hassan M, Andersson B. Development of an assay for cellular efflux of pharmaceutically active agents and its relevance to understanding drug interactions. Exp Hematol. 2017;52:65-71 pubmed publisher
    ..We demonstrated that chlorambucil, 4-hydroperoxycyclophosphamide, ketoconazole, ethacrynic acid, everolimus, and sirolimus strongly inhibited 5-CF efflux in lymphoma and leukemia cell lines...
  13. Moynahan M, Chen D, He W, Sung P, Samoila A, You D, et al. Correlation between PIK3CA mutations in cell-free DNA and everolimus efficacy in HR+, HER2- advanced breast cancer: results from BOLERO-2. Br J Cancer. 2017;116:726-730 pubmed publisher
    The current analysis was performed to evaluate the impact of PIK3CA hotspot mutations on everolimus efficacy in BOLERO-2 participants, using cell-free DNA (cfDNA) from plasma samples collected at the time of patient randomisation...
  14. Abizaid A, Costa J, Gibson C. Bioresorbable vascular scaffolds in daily clinical practice: is the essential really invisible to the eyes?. J Am Coll Cardiol. 2015;65:802-804 pubmed publisher
  15. Sato F, Toi M. [Molecular targeted therapy and genomic evolution of breast cancer]. Nihon Rinsho. 2015;73:1364-72 pubmed
    ..In this article, latest knowledge regarding breast cancer genome, especially in terms of 'evolution', is summarized. ..
  16. Klinghammer K, Otto R, Raguse J, Albers A, Tinhofer I, Fichtner I, et al. Basal subtype is predictive for response to cetuximab treatment in patient-derived xenografts of squamous cell head and neck cancer. Int J Cancer. 2017;141:1215-1221 pubmed publisher
    ..The models were treated in groups of 5-6 animals with docetaxel, cetuximab, everolimus, cis- or carboplatin and 5-fluorouracil...
  17. Liu C, Wu C, Petrossian K, Huang T, Tseng L, Chen S. Treatment for the endocrine resistant breast cancer: Current options and future perspectives. J Steroid Biochem Mol Biol. 2017;172:166-175 pubmed publisher
    ..Last but not the least, we discuss current challenges and future directions for management of endocrine resistant breast cancers. ..
  18. Nanavati A, Patel N, Burke J. Thrombocytosis and coronary occlusion. JACC Cardiovasc Interv. 2012;5:e18-9 pubmed publisher
  19. Watnick T, Germino G. mTOR inhibitors in polycystic kidney disease. N Engl J Med. 2010;363:879-81 pubmed publisher
  20. Gust K, So A. The role of mTOR in bladder cancer. Cancer Biol Ther. 2009;8:2348-50 pubmed
  21. Lee D, Park T, Song Y, Chun W, Choi R, Jeong J, et al. Clinical outcomes of biodegradable polymer biolimus-eluting BioMatrix stents versus durable polymer everolimus-eluting Xience stents. PLoS ONE. 2017;12:e0183079 pubmed publisher
    ..about clinical outcomes of biodegradable polymer biolimus-eluting BioMatrix stents (BP-BES) and durable polymer everolimus-eluting Xience stents (DP-EES) in real world practice...
  22. Bissler J, Kingswood J, Radzikowska E, Zonnenberg B, Belousova E, Frost M, et al. Everolimus long-term use in patients with tuberous sclerosis complex: Four-year update of the EXIST-2 study. PLoS ONE. 2017;12:e0180939 pubmed publisher
    We examined the long-term effects of everolimus in patients with renal angiomyolipoma associated with tuberous sclerosis complex or sporadic lymphangioleiomyomatosis...
  23. Ariaans G, Jalving M, Vries E, Jong S. Anti-tumor effects of everolimus and metformin are complementary and glucose-dependent in breast cancer cells. BMC Cancer. 2017;17:232 pubmed publisher
    Clinical efficacy of the mTOR inhibitor everolimus is limited in breast cancer and regularly leads to side-effects including hyperglycemia...
  24. Suzuki K, Ishikawa T, Mutoh M, Sakamoto H, Mori C, Ogawa T, et al. Propensity-Score Matched Comparison of Midterm Angiographic Outcomes of Sirolimus- Versus Everolimus- and Biolimus-Eluting Stents for De Novo Coronary Stenosis. Int Heart J. 2017;58:320-327 pubmed publisher
    ..conducted propensity-score matched comparisons of midterm angiographic outcomes of sirolimus (SES) versus either everolimus- (EES) or biolimus- (BES) eluting stents after placements for coronary stenosis in a daily practice environment ..
  25. Ormiston J, De Vroey F, Serruys P, Webster M. Bioresorbable polymeric vascular scaffolds: a cautionary tale. Circ Cardiovasc Interv. 2011;4:535-8 pubmed publisher
  26. Xia J, Qu Y, Yin C, Xu D. Optical Coherence Tomography Assessment of Glucose Fluctuation Impact on the Neointimal Proliferation After Stent Implantation in a Diabetic/Hypercholesterolemic Swine Model. Int Heart J. 2017;58:608-614 pubmed publisher
    ..A total of 24 everolimus-eluting stents (EES) were implanted in the right coronary artery (RCA) of the animals using a 20% overstretch ..
  27. Sibaud V, Dalenc F, Mourey L, Chevreau C. Paronychia and pyogenic granuloma induced by new anticancer mTOR inhibitors. Acta Derm Venereol. 2011;91:584-5 pubmed publisher
  28. Janku F. Phosphoinositide 3-kinase (PI3K) pathway inhibitors in solid tumors: From laboratory to patients. Cancer Treat Rev. 2017;59:93-101 pubmed publisher
    ..For the treatment of solid tumors, only allosteric mTOR inhibitors, such as everolimus and temsirolimus, are currently approved for clinical use...
  29. Wahl M, Chang S, Phillips J, Molinaro A, Costello J, Mazor T, et al. Probing the phosphatidylinositol 3-kinase/mammalian target of rapamycin pathway in gliomas: A phase 2 study of everolimus for recurrent adult low-grade gliomas. Cancer. 2017;123:4631-4639 pubmed publisher
  30. Bundhun P, Yanamala C, Huang W. Comparing Stent Thrombosis associated with Zotarolimus Eluting Stents versus Everolimus Eluting Stents at 1 year follow up: a systematic review and meta-analysis of 6 randomized controlled trials. BMC Cardiovasc Disord. 2017;17:84 pubmed publisher
    ..to compare the different types of Stent Thrombosis (ST) associated with Zotarolimus Eluting Stents (ZES) versus Everolimus Eluting Stents (EES) at 1 year follow up. Electronic databases were searched for studies comparing ZES with EES...
  31. Koyama M, Yano T, Kikuchi K, Miura T. Everolimus-responsive dilated cardiomyopathy in tuberous sclerosis. Eur Heart J. 2015;36:2338 pubmed publisher
  32. Schaffrath J, Schmoll H, Voigt W, Müller L, Muller Tidow C, Mueller T. Efficacy of targeted drugs in germ cell cancer cell lines with differential cisplatin sensitivity. PLoS ONE. 2017;12:e0178930 pubmed publisher
    ..However, when combined with cisplatin they did not demonstrate any promising ability to overcome cisplatin resistance in TGCTs. ..
  33. Bernasconi E, Gaudio E, Lejeune P, Tarantelli C, Cascione L, Kwee I, et al. Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma. Br J Haematol. 2017;178:936-948 pubmed publisher
    ..Our data also indicate the use of combination schemes targeting EZH2, mTOR and BTK alongside BET bromodomains. ..
  34. White H. The prequel: defining prognostically important criteria in the periprocedural PCI troponin saga. Circ Cardiovasc Interv. 2012;5:142-5 pubmed publisher
  35. Aristizabal Prada E, Orth M, Nölting S, Spöttl G, Maurer J, Auernhammer C. The MTH1 inhibitor TH588 demonstrates anti-tumoral effects alone and in combination with everolimus, 5-FU and gamma-irradiation in neuroendocrine tumor cells. PLoS ONE. 2017;12:e0178375 pubmed publisher
    ..pathways implicated in the effects of TH588 alone as well as dual-targeting approaches combining TH588 with everolimus, cytotoxic 5-fluorouracil or ?-irradiation...
  36. Daniel C, Weigmann B, von Boehmer H. Reply to "Tolerogenic insulin peptide therapy precipitates type 1 diabetes". J Exp Med. 2017;214:2157-2159 pubmed publisher
    ..Here, we provide a response to these data and suggest that appropriate subimmunogenic conditions are required to induce Foxp3+ regulatory T cell conversion. ..
  37. Dudek D, Rzeszutko Ł, Onuma Y, Sotomi Y, Depukat R, Veldhof S, et al. Vasomotor Response to Nitroglycerine Over 5 Years Follow-Up After Everolimus-Eluting Bioresorbable Scaffold Implantation. JACC Cardiovasc Interv. 2017;10:786-795 pubmed publisher
    ..There are no data regarding long-term vasomotor response after everolimus-eluting bioresorbable vascular scaffold ABSORB implantation...
  38. Nölting S, Rentsch J, Freitag H, Detjen K, Briest F, Möbs M, et al. The selective PI3K? inhibitor BYL719 as a novel therapeutic option for neuroendocrine tumors: Results from multiple cell line models. PLoS ONE. 2017;12:e0182852 pubmed publisher
    ..In BON-1 and QGP-1 cells, the BYL719/everolimus combination was synergistic through simultaneous AKT/mTORC1 inhibition, and significantly increased somatostatin ..
  39. Martin L, Pancholi S, Farmer I, Guest S, Ribas R, Weigel M, et al. Effectiveness and molecular interactions of the clinically active mTORC1 inhibitor everolimus in combination with tamoxifen or letrozole in vitro and in vivo. Breast Cancer Res. 2012;14:R132 pubmed publisher
    ..resistance associated with HER2 overexpression were treated in vitro and as subcutaneous xenografts with everolimus (RAD001-mTORC1 inhibitor), in combination with tamoxifen or letrozole...
  40. Tannir N, Schwab G, Grünwald V. Cabozantinib: an Active Novel Multikinase Inhibitor in Renal Cell Carcinoma. Curr Oncol Rep. 2017;19:14 pubmed publisher
    ..inhibitor nivolumab, the TKI cabozantinib, and the combination of the TKI lenvatinib and the mTOR inhibitor everolimus. Cabozantinib inhibits VEGFRs, MET, and AXL, kinases that promote tumorigenesis, angiogenesis, metastasis, and ..
  41. Parachoniak C, Rankin A, Gaffney B, Hartmaier R, Spritz D, Erlich R, et al. Exceptional durable response to everolimus in a patient with biphenotypic breast cancer harboring an STK11 variant. Cold Spring Harb Mol Case Stud. 2017;3: pubmed publisher
    ..g., the mammalian target of rapamycin [mTOR] inhibitor everolimus) in advanced breast cancer patients have not utilized predictive genomic biomarker-based selection and have ..
  42. Li T, Chen X, Dai X, Wei B, Weng Q, Chen X, et al. Novel Hsp90 inhibitor platycodin D disrupts Hsp90/Cdc37 complex and enhances the anticancer effect of mTOR inhibitor. Toxicol Appl Pharmacol. 2017;330:65-73 pubmed publisher
    ..In different genotypes of non-small cell lung cancer cells, co-treatment with the mTOR inhibitor Everolimus and PD enhanced antiproliferation activity and apoptotic effect...
  43. Jiao Y, Li G, Li Q, Ali R, Qin L, Li W, et al. mTOR (Mechanistic Target of Rapamycin) Inhibition Decreases Mechanosignaling, Collagen Accumulation, and Stiffening of the Thoracic Aorta in Elastin-Deficient Mice. Arterioscler Thromb Vasc Biol. 2017;37:1657-1666 pubmed publisher
    ..Our findings suggest that mTOR-sensitive perturbation of smooth muscle cell mechanosensing contributes to elastin aortopathy. ..
  44. Ruzsa Z, van der Linden M, Van Mieghem N, Regar E, Ligthart J, Serruys P, et al. Culotte stenting with bioabsorbable everolimus-eluting stents. Int J Cardiol. 2013;168:e35-7 pubmed publisher
  45. Northrup H. The mTOR inhibitor revolution rolls on. Lancet Oncol. 2014;15:1418-9 pubmed publisher
  46. Zhang X, Zhu Q, Kang L, Li X, Xu B. Mid- and Long-Term Outcome Comparisons of Everolimus-Eluting Bioresorbable Scaffolds Versus Everolimus-Eluting Metallic Stents: A Systematic Review and Meta-analysis. Ann Intern Med. 2017;167:642-654 pubmed publisher
    ..Percutaneous coronary interventions to implant bioresorbable vascular scaffolds (BVSs) were designed to reduce the late thrombotic events that occur with metallic stents...
  47. TUVESON D, Hanahan D. Translational medicine: Cancer lessons from mice to humans. Nature. 2011;471:316-7 pubmed publisher
  48. Liakakos T, Roukos D. Everolimus and sunitinib: from mouse models to treatment of pancreatic neuroendocrine tumors. Future Oncol. 2011;7:1025-9 pubmed publisher
  49. Montone R, Niccoli G, De Marco F, Minelli S, D Ascenzo F, Testa L, et al. Temporal Trends in Adverse Events After Everolimus-Eluting Bioresorbable Vascular Scaffold Versus Everolimus-Eluting Metallic Stent Implantation: A Meta-Analysis of Randomized Controlled Trials. Circulation. 2017;135:2145-2154 pubmed publisher
    ..The everolimus-eluting bioresorbable vascular scaffold (BVS) is the most studied of these stent platforms; however, recent ..
  50. Şerban R, Scridon A, Dobreanu D, Elkaholut A. Coronary artery aneurysm formation within everolimus-eluting bioresorbable stent. Int J Cardiol. 2014;177:e4-5 pubmed publisher
  51. Cova E, Inghilleri S, Pandolfi L, Morosini M, Magni S, Colombo M, et al. Bioengineered gold nanoparticles targeted to mesenchymal cells from patients with bronchiolitis obliterans syndrome does not rise the inflammatory response and can be safely inhaled by rodents. Nanotoxicology. 2017;11:534-545 pubmed publisher
    ..In a previous work, we engineered GNPs loaded with the mammalian target of rapamycin inhibitor everolimus, specifically decorated with an antibody against CD44, a surface receptor expressed by primary MCs isolated from ..
  52. Toi M, Shao Z, Hurvitz S, Tseng L, Zhang Q, Shen K, et al. Efficacy and safety of everolimus in combination with trastuzumab and paclitaxel in Asian patients with HER2+ advanced breast cancer in BOLERO-1. Breast Cancer Res. 2017;19:47 pubmed publisher
    The current exploratory analysis was performed to evaluate the efficacy and safety of everolimus for treatment of human epidermal growth factor receptor 2-positive (HER2+) advanced breast cancer in the Asian subset of patients in the ..
  53. Chang M, Lee C, Ahn J, Cavalcante R, Sotomi Y, Onuma Y, et al. Comparison of Outcome of Coronary Artery Bypass Grafting Versus Drug-Eluting Stent Implantation for Non-ST-Elevation Acute Coronary Syndrome. Am J Cardiol. 2017;120:380-386 pubmed publisher
    ..Data were pooled from the Randomized Comparison of Coronary Artery Bypass Surgery and Everolimus-Eluting Stent Implantation in the Treatment of Patients with Multivessel Coronary Artery Disease (BEST) trial, ..