Daniel P Rossignol
Affiliation: Eisai Medical Research
- Inhibition of endotoxin response by e5564, a novel Toll-like receptor 4-directed endotoxin antagonistMaureen Mullarkey
Biology Section, Eisai Research Institute of Boston, Inc, Andover, Massachusetts, USA
J Pharmacol Exp Ther 304:1093-102. 2003..These results indicate that E5564 is a potent antagonist of LPS and lacks agonistic activity in human and animal model systems, making it a potentially effective therapeutic agent for treatment of disease states caused by endotoxin...
- Continuous pharmacodynamic activity of eritoran tetrasodium, a TLR4 antagonist, during intermittent intravenous infusion into normal volunteersDaniel P Rossignol
Eisai Medical Research Inc, Ridgefield Park, New Jersey 07660, USA
Innate Immun 14:383-94. 2008..The objective of this study was to assess the safety, and pharmacokinetic and pharmacodynamic profile of E5564 infused twice-daily at three target steady-state plasma levels of approximately 1, 3 and 10 microg/ml in healthy volunteers...
- Antagonism of in vivo and ex vivo response to endotoxin by E5564, a synthetic lipid A analogueDaniel P Rossignol
Eisai Medical Research Inc, Teaneck, New Jersey 07666, USA
J Endotoxin Res 8:483-8. 2002..Results from these multiple-dose studies indicate that under these conditions of administration, plasma levels of E5564 can be predictive of long-term pharmacodynamic activity...
- TLR4 antagonists for endotoxemia and beyondDaniel P Rossignol
Eisai Medical Research Inc, NJ 07660, USA
Curr Opin Investig Drugs 6:496-502. 2005..This review discusses current, preclinical and clinical research regarding eritoran (E-5564), an analog of the non-toxic lipid A from Rhodobacter sphaeroides, as well as other antagonists of TLR4 in a variety of diseases...
- Safety, pharmacokinetics, pharmacodynamics, and plasma lipoprotein distribution of eritoran (E5564) during continuous intravenous infusion into healthy volunteersDaniel P Rossignol
Eisai Medical Research, Inc, Glenpointe Centre West, 500 Frank W Burr Blvd, Teaneck, NJ 07666 6741, USA
Antimicrob Agents Chemother 48:3233-40. 2004....
- Extended in vivo pharmacodynamic activity of E5564 in normal volunteers with experimental endotoxemia [corrected]Melvyn Lynn
Eisai Medical Research Inc, Glenpointe Centre West, Teaneck, New Jersey 07666 6741, USA
J Pharmacol Exp Ther 308:175-81. 2004..No differences were observed. These results demonstrate that E5564 blocks the effects of endotoxin in a human model of clinical sepsis and indicate its potential in the treatment and/or prevention of clinical sepsis...
- Blocking of responses to endotoxin by E5564 in healthy volunteers with experimental endotoxemiaMelvyn Lynn
Eisai Medical Research, Teaneck, New Jersey 07666 6741, USA
J Infect Dis 187:631-9. 2003..01). These results demonstrate that E5564 blocks the effects of LPS in a human model of clinical sepsis and indicate its potential in the treatment and/or prevention of clinical sepsis...
- Inhibition of endotoxin response by synthetic TLR4 antagonistsLynn D Hawkins
Eisai Medical Research Inc, Andover, MA, USA
Curr Top Med Chem 4:1147-71. 2004..This review discusses the evolution of synthetic LPS antagonists with emphasis on the SAR and development of E5564 and its precursors...
- Association of the endotoxin antagonist E5564 with high-density lipoproteins in vitro: dependence on low-density and triglyceride-rich lipoprotein concentrationsKishor M Wasan
Faculty of Pharmaceutical Sciences, The University of British Columbia, Vancouver, British Columbia, Canada
Antimicrob Agents Chemother 47:2796-803. 2003..Information from these studies could be used to help identify the possible components of lipoproteins which influence the interaction of E5564 with specific lipoprotein particles...
- Influence of plasma cholesterol and triglyceride concentrations and eritoran (E5564) micelle size on its plasma pharmacokinetics and ex vivo activity following single intravenous bolus dose into healthy female rabbitsKishor M Wasan
Faculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, British Columbia, Canada
Pharm Res 25:176-82. 2008..This was done with eritoran administered as stable micelle formulations of mean hydrodynamic diameters of 8 or 27 nm)...
- A novel class of endotoxin receptor agonists with simplified structure, toll-like receptor 4-dependent immunostimulatory action, and adjuvant activityLynn D Hawkins
Department of Medicinal Chemistry, Signal Transduction Research, Eisai Research Institute, Andover, Massachusetts 01810, USA
J Pharmacol Exp Ther 300:655-61. 2002..Our results indicate that these unique compounds behave as agonists of TLR4, resulting in responses similar to those elicited by LPS. They display adjuvant activity in vivo and may be useful for the development of vaccine therapies...
- A phase II, double-blind, placebo-controlled, ascending-dose study of Eritoran (E5564), a lipid A antagonist, in patients undergoing cardiac surgery with cardiopulmonary bypassElliott Bennett-Guerrero
Department of Anesthesiology, Duke University Medical Center, Durham, NC 27710, USA
Anesth Analg 104:378-83. 2007..In this study we assessed the safety of eritoran administration in patients undergoing cardiac surgery and obtained preliminary efficacy data for the prophylaxis of endotoxin-mediated surgical complications...