Literature DB >> 21147869

Inhibitors of mTOR.

Heinz-Josef Klümpen1, Jos H Beijnen, Howard Gurney, Jan H M Schellens.   

Abstract

Inhibitors of mammalian target of rapamycin (mTOR) have been approved for the treatment of renal cell carcinoma and appear to have a role in the treatment of other malignancies. The primary objective of this drug review is to provide pharmacokinetic and dynamic properties of the commonly used drugs everolimus and temsirolimus. Additionally, information on clinical use, mechanism of action, bioanalysis, drug-drug interactions, alterations with disease or age, pharmacogenetics, and drug resistance is given. This overview should assist the treating medical oncologist in adjusting treatment with mTOR inhibitors to individual patient circumstances.

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Year:  2010        PMID: 21147869      PMCID: PMC3227930          DOI: 10.1634/theoncologist.2010-0196

Source DB:  PubMed          Journal:  Oncologist        ISSN: 1083-7159


  67 in total

1.  Influence of hepatic impairment on everolimus pharmacokinetics: implications for dose adjustment.

Authors:  J M Kovarik; H D Sabia; J Figueiredo; H Zimmermann; C Reynolds; S C Dilzer; K Lasseter; C Rordorf
Journal:  Clin Pharmacol Ther       Date:  2001-11       Impact factor: 6.875

2.  Rapamycin inhibits primary and metastatic tumor growth by antiangiogenesis: involvement of vascular endothelial growth factor.

Authors:  Markus Guba; Philipp von Breitenbuch; Markus Steinbauer; Gudrun Koehl; Stefanie Flegel; Matthias Hornung; Christiane J Bruns; Carl Zuelke; Stefan Farkas; Matthias Anthuber; Karl-Walter Jauch; Edward K Geissler
Journal:  Nat Med       Date:  2002-02       Impact factor: 53.440

3.  Phase I and pharmacokinetic study of CCI-779, a novel cytostatic cell-cycle inhibitor, in combination with 5-fluorouracil and leucovorin in patients with advanced solid tumors.

Authors:  C J A Punt; J Boni; U Bruntsch; M Peters; C Thielert
Journal:  Ann Oncol       Date:  2003-06       Impact factor: 32.976

4.  Effect of rifampin on apparent clearance of everolimus.

Authors:  John M Kovarik; Stefan Hartmann; Joaquim Figueiredo; Marisel Rouilly; Andreas Port; Christiane Rordorf
Journal:  Ann Pharmacother       Date:  2002-06       Impact factor: 3.154

5.  Pharmacokinetic and pharmacodynamic assessments of HMG-CoA reductase inhibitors when coadministered with everolimus.

Authors:  John M Kovarik; Stefan Hartmann; Martine Hubert; Stephane Berthier; Werner Schneider; Bernd Rosenkranz; Christiane Rordorf
Journal:  J Clin Pharmacol       Date:  2002-02       Impact factor: 3.126

6.  Clinical development of an everolimus pediatric formulation: relative bioavailability, food effect, and steady-state pharmacokinetics.

Authors:  John M Kovarik; Adele Noe; Stephane Berthier; Louis McMahon; Wayne K Langholff; Alan S Marion; Peter Friedrich Hoyer; Robert Ettenger; Christiane Rordorf
Journal:  J Clin Pharmacol       Date:  2003-02       Impact factor: 3.126

7.  Pharmacodynamic Evaluation of CCI-779, an Inhibitor of mTOR, in Cancer Patients.

Authors:  Josep Maria Peralba; Linda DeGraffenried; William Friedrichs; Letitia Fulcher; Viktor Grünwald; Geoffrey Weiss; Manuel Hidalgo
Journal:  Clin Cancer Res       Date:  2003-08-01       Impact factor: 12.531

8.  Antitumor efficacy of intermittent treatment schedules with the rapamycin derivative RAD001 correlates with prolonged inactivation of ribosomal protein S6 kinase 1 in peripheral blood mononuclear cells.

Authors:  Anne Boulay; Sabine Zumstein-Mecker; Christine Stephan; Iwan Beuvink; Frederic Zilbermann; Roland Haller; Sonja Tobler; Christoph Heusser; Terence O'Reilly; Barbara Stolz; Andreas Marti; George Thomas; Heidi A Lane
Journal:  Cancer Res       Date:  2004-01-01       Impact factor: 12.701

9.  Everolimus for the prevention of allograft rejection and vasculopathy in cardiac-transplant recipients.

Authors:  Howard J Eisen; E Murat Tuzcu; Richard Dorent; Jon Kobashigawa; Donna Mancini; Hannah A Valantine-von Kaeppler; Randall C Starling; Keld Sørensen; Manfred Hummel; Joan M Lind; Kamal H Abeywickrama; Peter Bernhardt
Journal:  N Engl J Med       Date:  2003-08-28       Impact factor: 91.245

10.  mTOR interacts with raptor to form a nutrient-sensitive complex that signals to the cell growth machinery.

Authors:  Do-Hyung Kim; D D Sarbassov; Siraj M Ali; Jessie E King; Robert R Latek; Hediye Erdjument-Bromage; Paul Tempst; David M Sabatini
Journal:  Cell       Date:  2002-07-26       Impact factor: 41.582

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  18 in total

Review 1.  Autophagy and haematopoietic stem cell transplantation.

Authors:  Lucie Leveque; Laetitia Le Texier; Katie E Lineburg; Geoffrey R Hill; Kelli P A MacDonald
Journal:  Immunol Cell Biol       Date:  2014-11-04       Impact factor: 5.126

Review 2.  Roles of the immune system in skin cancer.

Authors:  S Rangwala; K Y Tsai
Journal:  Br J Dermatol       Date:  2011-11       Impact factor: 9.302

3.  Reduction behavior induced by HL010183, a metformin derivative against the growth of cutaneous squamous cell carcinoma.

Authors:  Guoying Miao; Baoguo Liu; Xiaohui Guo; Xike Zhang; Gui-Jing Liu
Journal:  Int J Clin Exp Pathol       Date:  2015-01-01

4.  Differences in adverse event profiles between everolimus and temsirolimus and the risk factors for non-infectious pneumonitis in advanced renal cell carcinoma.

Authors:  Masahiro Nozawa; Takayuki Ohzeki; Satoshi Tamada; Fumiya Hongo; Satoshi Anai; Kiyohide Fujimoto; Tsuneharu Miki; Tatsuya Nakatani; Satoshi Fukasawa; Hirotsugu Uemura
Journal:  Int J Clin Oncol       Date:  2014-10-25       Impact factor: 3.402

Review 5.  Molecular targeting agents associated with transarterial chemoembolization or radiofrequency ablation in hepatocarcinoma treatment.

Authors:  Girolamo Ranieri; Ilaria Marech; Vito Lorusso; Veronica Goffredo; Angelo Paradiso; Domenico Ribatti; Cosmo Damiano Gadaleta
Journal:  World J Gastroenterol       Date:  2014-01-14       Impact factor: 5.742

Review 6.  mTOR Inhibitors in Castration-Resistant Prostate Cancer: A Systematic Review.

Authors:  Cara M Statz; Sara E Patterson; Susan M Mockus
Journal:  Target Oncol       Date:  2017-02       Impact factor: 4.493

7.  Glucosamine activates autophagy in vitro and in vivo.

Authors:  Beatriz Caramés; William B Kiosses; Yukio Akasaki; Diana C Brinson; William Eap; James Koziol; Martin K Lotz
Journal:  Arthritis Rheum       Date:  2013-07

8.  Peripheral administration of translation inhibitors reverses increased hyperalgesia in a model of chronic pain in the rat.

Authors:  Luiz F Ferrari; Oliver Bogen; Carissa Chu; Jon D Levine
Journal:  J Pain       Date:  2013-05-08       Impact factor: 5.820

9.  Weekly nab-Rapamycin in patients with advanced nonhematologic malignancies: final results of a phase I trial.

Authors:  Ana M Gonzalez-Angulo; Funda Meric-Bernstam; Sant Chawla; Gerald Falchook; David Hong; Argun Akcakanat; Huiqin Chen; Aung Naing; Siqing Fu; Jennifer Wheler; Stacy Moulder; Thorunn Helgason; Shaoyi Li; Ileana Elias; Neil Desai; Razelle Kurzrock
Journal:  Clin Cancer Res       Date:  2013-10-01       Impact factor: 12.531

10.  A phase I/II, non-randomized, feasibility/safety and efficacy study of the combination of everolimus, cetuximab and capecitabine in patients with advanced pancreatic cancer.

Authors:  Sil Kordes; Dick J Richel; Heinz-Josef Klümpen; Mariëtte J Weterman; Arnoldus J W M Stevens; Johanna W Wilmink
Journal:  Invest New Drugs       Date:  2012-02-25       Impact factor: 3.850

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