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Drug Evaluation

Everolimus: an update on the mechanism of action, pharmacokinetics and recent clinical trials

Pages 807-819 | Published online: 08 Jul 2008

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (5)

Jacques Dantal. (2012) Everolimus: preventing organ rejection in adult kidney transplant recipients. Expert Opinion on Pharmacotherapy 13:5, pages 767-778.
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Helio Tedesco-Silva Jr, Claudia Rosso Felipe, Tainá Veras de Sandes Freitas, Marina Pontello Cristeli, Carolina Araújo Rodrigues & José Osmar Medina Pestana. (2011) Impact of everolimus: update on immunosuppressive therapy strategies and patient outcomes after renal transplantation. Transplant Research and Risk Management 3, pages 9-29.
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Mareen Matz, Marcel Naik, Mir-Farzin Mashreghi, Petra Glander, Hans-H Neumayer & Klemens Budde. (2011) Evaluation of the novel protein kinase C inhibitor sotrastaurin as immunosuppressive therapy after renal transplantation. Expert Opinion on Drug Metabolism & Toxicology 7:1, pages 103-113.
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S Allan Schaffer & Heather J Ross. (2010) Everolimus: efficacy and safety in cardiac transplantation. Expert Opinion on Drug Safety 9:5, pages 843-854.
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Stéphane Oudard, Jacques Medioni, Jorge Aylllon, Eduardo Barrascourt, Reza-Thierry Elaidi, José Balcaceres & Florian Scotte. (2009) Everolimus (RAD001): an mTOR inhibitor for the treatment of metastatic renal cell carcinoma. Expert Review of Anticancer Therapy 9:6, pages 705-717.
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Articles from other publishers (40)

Jinha Park, Se Hee Kim, Jongsung Hahn, Hoon-Chul Kang, Sang-Guk Lee, Heung Dong Kim & Min Jung Chang. (2023) Population pharmacokinetics of everolimus in patients with seizures associated with focal cortical dysplasia. Frontiers in Pharmacology 14.
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Dae Sung Park, Myung Ho Jeong, Yu Jeong Jin, Mi Hyang Na, Doo Sun Sim, Munki Kim, Kyung Hoon Cho, Dae Young Hyun, Seok Oh, Jeong Ha Kim, Kyung Seob Lim, Jun-Kyu Park, Han Ki Kim, Young Joon Hong, Ju Han Kim, Youngkeun Ahn & Jeong Hun Kim. (2023) Preclinical Evaluation of an Everolimus-Eluting Bioresorbable Vascular Scaffold Via a Long-Term Rabbit Iliac Artery Model. Tissue Engineering and Regenerative Medicine 20:2, pages 239-249.
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Mururul Aisyi, Ayu Hutami Syarif, Dewi Aisyah Mukarramah, Rio Hermawan & Dewi Iriani. (2021) Everolimus for the treatment of epithelioid hemangioma: a case report. Medical Journal of Indonesia 30:4, pages 301-5.
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Amani A. Gillette, Christopher P. Babiarz, Ava R. VanDommelen, Cheri A. Pasch, Linda Clipson, Kristina A. Matkowskyj, Dustin A. Deming & Melissa C. Skala. (2021) Autofluorescence Imaging of Treatment Response in Neuroendocrine Tumor Organoids. Cancers 13:8, pages 1873.
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Carine Mauro, Victor Hugo Fonseca de Jesus, Milton Barros, Frederico Perego Costa, Rui F. Weschenfelder, Nathalia D'Agustini, Martin Angel, Romina Luca, Jose Eduardo Nuñez, Juan Manuel O'Connor & Rachel P. Riechelmann. (2021) Opportunistic and Serious Infections in Patients with Neuroendocrine Tumors Treated with Everolimus: A Multicenter Study of Real-World Patients. Neuroendocrinology 111:7, pages 631-638.
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Tina Hörbelt, Anna Lena Kahl, Frederike Kolbe, Susann Hetze, Benjamin Wilde, Oliver Witzke & Manfred Schedlowski. (2020) Dose‐Dependent Acute Effects of Everolimus Administration on Immunological, Neuroendocrine and Psychological Parameters in Healthy Men. Clinical and Translational Science 13:6, pages 1251-1259.
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Weijie Liu, Qingshan Li, Junhua Hu, Hongxue Wang, Fengbo Xu & Qiang Bian. (2019) Application of natural products derivatization method in the design of targeted anticancer agents from 2000 to 2018. Bioorganic & Medicinal Chemistry 27:23, pages 115150.
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Hilde M. Norum, Annika E. Michelsen, Tove Lekva, Satish Arora, Kari Otterdal, Maria Belland Olsen, Xiang Yi Kong, Einar Gude, Arne K. Andreassen, Dag Solbu, Kristjan Karason, Göran Dellgren, Lars Gullestad, Pål Aukrust & Thor Ueland. (2019) Circulating delta-like Notch ligand 1 is correlated with cardiac allograft vasculopathy and suppressed in heart transplant recipients on everolimus-based immunosuppression. American Journal of Transplantation 19:4, pages 1050-1060.
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Denise Wang, Bruno Meiser, Howard J. Eisen & Sandra Eifert. 2019. Heart Failure. Heart Failure 241 253 .
J. Salman, K. Jansson, Th. Siemeni, W. Sommer, A.-K. Knoefel, L. Ahrens, T. Nakagiri, F. Ius, I. Tudorache, B. Kruse, S. Thissen, D. Jonigk, M. Strüber, A. Haverich, G. Warnecke & M. Avsar. (2018) Role for primary immunosuppression with everolimus after pulmonary transplantation. Transplant Immunology 49, pages 12-19.
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Jinyu Liu, Dong Liu, Juan Li, Lan Zhu, Chengliang Zhang, Kai Lei, Qiling Xu & Ruxu You. (2017) Efficacy and Safety of Everolimus for Maintenance Immunosuppression of Kidney Transplantation: A Meta-Analysis of Randomized Controlled Trials. PLOS ONE 12:1, pages e0170246.
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Klemens Budde, Claudia Sommerer, Olesja Rissling, Maja T. Dieterlen & Markus J. Barten. (2016) Target Enzyme Activity and Phosphorylation of Pathway Molecules As Specific Biomarkers in Transplantation. Therapeutic Drug Monitoring 38:Supplement 1, pages S43-S49.
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Raül Rigo-Bonnin, Ariadna Arbiol-Roca, José Manuel González de Aledo-Castillo & Pedro Alía. (2015) Simultaneous Measurement of Cyclosporine A, Everolimus, Sirolimus and Tacrolimus Concentrations in Human Blood by UPLC–MS/MS. Chromatographia 78:23-24, pages 1459-1474.
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Björn Schniedewind, Stefanie Niederlechner, Jeffrey L. Galinkin, Kamisha L. Johnson-Davis, Uwe Christians & Eric J. Meyer. (2015) Long-Term Cross-Validation of Everolimus Therapeutic Drug Monitoring Assays. Therapeutic Drug Monitoring 37:3, pages 296-303.
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Tanya Dorff & Philip C. Mack. 2015. Kidney Cancer. Kidney Cancer 295 314 .
S Mielke, M Lutz, J Schmidhuber, M Kapp, D Ditz, J Ammer, H Einsele, G U Grigoleit, E Holler & D Wolff. (2014) Salvage therapy with everolimus reduces the severity of treatment-refractory chronic GVHD without impairing disease control: A dual center retrospective analysis. Bone Marrow Transplantation 49:11, pages 1412-1418.
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Marigdalia K. Ramirez-Fort, Emily C. Case, Alyx C. Rosen, Felipe B. Cerci, Shenhong Wu & Mario E. Lacouture. (2014) Rash to the mTOR Inhibitor Everolimus. American Journal of Clinical Oncology 37:3, pages 266-271.
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Y.-M. Liu, Y.Q. Shao & Q. He. (2014) Sirolimus for Treatment of Autosomal-Dominant Polycystic Kidney Disease: A Meta-Analysis of Randomized Controlled Trials. Transplantation Proceedings 46:1, pages 66-74.
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Carlo Palmieri, Darren K. Patten, Adam Januszewski, Giorgia Zucchini & Sacha J. Howell. (2014) Breast cancer: Current and future endocrine therapies. Molecular and Cellular Endocrinology 382:1, pages 695-723.
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David J. Taber, Lindsey Belk, Holly Meadows, Nicole Pilch, James Fleming, Titte Srinivas, John McGillicuddy, Charles Bratton, Kenneth Chavin & Prabhakar Baliga. (2013) Racial Comparisons of Everolimus Pharmacokinetics and Pharmacodynamics in Adult Kidney Transplant Recipients. Therapeutic Drug Monitoring 35:6, pages 753-759.
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C. Krautz, S. Wolk, A. Steffen, K.-P. Knoch, U. Ceglarek, J. Thiery, S. Bornstein, H.-D. Saeger, M. Solimena & S. Kersting. (2013) Effects of immunosuppression on alpha and beta cell renewal in transplanted mouse islets. Diabetologia 56:7, pages 1596-1604.
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Makoto Endo, Hidetaka Yamamoto, Nokitaka Setsu, Kenichi Kohashi, Yusuke Takahashi, Takeaki Ishii, Kei-ichiro Iida, Yoshihiro Matsumoto, Michiyuki Hakozaki, Mikiko Aoki, Hiroshi Iwasaki, Yoh Dobashi, Kenichi Nishiyama, Yukihide Iwamoto & Yoshinao Oda. (2013) Prognostic Significance of AKT/mTOR and MAPK Pathways and Antitumor Effect of mTOR Inhibitor in NF1-Related and Sporadic Malignant Peripheral Nerve Sheath Tumors. Clinical Cancer Research 19:2, pages 450-461.
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E. Claire Dees & Lisa A. Carey. (2013) Improving Endocrine Therapy for Breast Cancer: It's Not That Simple. Journal of Clinical Oncology 31:2, pages 171-173.
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Stephan W. Hirt, Christoph Bara, Markus J. Barten, Tobias Deuse, Andreas O. Doesch, Ingo Kaczmarek, Uwe Schulz, Jörg Stypmann, Assad Haneya & Hans B. Lehmkuhl. (2013) Everolimus in Heart Transplantation: An Update. Journal of Transplantation 2013, pages 1-12.
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Eric Jonasch & Michel Choueiri. 2013. Renal Cell Carcinoma. Renal Cell Carcinoma 317 337 .
Maja‐Theresa Dieterlen, Hartmuth B. Bittner, Sara Klein, Sandy von Salisch, Anja Mittag, Attila Tárnok, Stefan Dhein, Friedrich W. Mohr & Markus J. Barten. (2011) Assay validation of phosphorylated S6 ribosomal protein for a pharmacodynamic monitoring of mTOR‐inhibitors in peripheral human blood. Cytometry Part B: Clinical Cytometry 82B:3, pages 151-157.
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Chad M. Barnett. (2012) Everolimus: Targeted Therapy on the Horizon for the Treatment of Breast Cancer. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy 32:4, pages 383-396.
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Satish Arora, Einar Gude, Vilborg Sigurdardottir, Svend Aage Mortensen, Hans Eiskjær, Gerdt Riise, Lena Mared, Øystein Bjørtuft, Bjørn Ekmehag, Kjell Jansson, Svein Simonsen, Pål Aukrust, Dag Solbu, Martin Iversen & Lars Gullestad. (2012) Improvement in renal function after everolimus introduction and calcineurin inhibitor reduction in maintenance thoracic transplant recipients: The significance of baseline glomerular filtration rate. The Journal of Heart and Lung Transplantation 31:3, pages 259-265.
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Michael A. Acker & Mariell Jessup. 2012. Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine. Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine 601 616 .
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Michel Choueiri & Philip Mack. 2012. Kidney Cancer. Kidney Cancer 209 223 .
Joyce S. Lee & Harold R. Collard. (2011) Primum non nocere: Safety in clinical trials for IPF. Respirology 16:5, pages 723-724.
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MONIQUE A. MALOUF, PETER HOPKINS, GREGORY SNELL & ALLAN R. GLANVILLE. (2011) An investigator-driven study of everolimus in surgical lung biopsy confirmed idiopathic pulmonary fibrosis. Respirology 16:5, pages 776-783.
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Mariell Jessup & Michael Acker. 2011. Heart Failure: A Companion to Braunwald's Heart Disease. Heart Failure: A Companion to Braunwald's Heart Disease 787 801 .
Henk-Jan Schuurman. 2011. Principles of Immunopharmacology. Principles of Immunopharmacology 525 556 .
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Darcy A. Krueger, Marguerite M. Care, Katherine Holland, Karen Agricola, Cynthia Tudor, Prajakta Mangeshkar, Kimberly A. Wilson, Anna Byars, Tarek Sahmoud & David Neal Franz. (2010) Everolimus for Subependymal Giant-Cell Astrocytomas in Tuberous Sclerosis. New England Journal of Medicine 363:19, pages 1801-1811.
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M. Carmellini, A. Collini, G. Ruggieri & M. Bernini. (2010) Conversion of Stable Kidney Transplant Recipients From a Twice-Daily to Once-Daily Everolimus Regimen. Transplantation Proceedings 42:4, pages 1312-1313.
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