Todd Fields
Eli Lilly and Company
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Publication
Featured researches published by Todd Fields.
Journal of Lipid Research | 2011
Guoqing Cao; Thomas P. Beyer; Youyan Zhang; Robert J. Schmidt; Yan Q. Chen; Sandra L. Cockerham; Karen M. Zimmerman; Sotirios K. Karathanasis; Ellen A. Cannady; Todd Fields; Nathan Bryan Mantlo
Cholesteryl ester transfer protein (CETP) catalyses the exchange of cholesteryl ester and triglyceride between HDL and apoB containing lipoprotein particles. The role of CETP in modulating plasma HDL cholesterol levels in humans is well established and there have been significant efforts to develop CETP inhibitors to increase HDL cholesterol for the treatment of coronary artery disease. These efforts, however, have been hampered by the fact that most CETP inhibitors either have low potency or have undesirable side effects. In this study, we describe a novel benzazepine compound evacetrapib (LY2484595), which is a potent and selective inhibitor of CETP both in vitro and in vivo. Evacetrapib inhibited human recombinant CETP protein (5.5 nM IC50) and CETP activity in human plasma (36 nM IC50) in vitro. In double transgenic mice expressing human CETP and apoAI, evacetrapib exhibited an ex vivo CETP inhibition ED50 of less than 5 mg/kg at 8 h post oral dose and significantly elevated HDL cholesterol. Importantly, no blood pressure elevation was observed in rats dosed with evacetrapib at high exposure multiples compared with the positive control, torcetrapib. In addition, in a human adrenal cortical carcinoma cell line (H295R cells), evacetrapib did not induce aldosterone or cortisol biosynthesis whereas torcetrapib dramatically induced aldosterone and cortisol biosynthesis. Our data indicate that evacetrapib is a potent and selective CETP inhibitor without torcetrapib-like off-target liabilities. Evacetrapib is currently in phase II clinical development.
Archive | 2005
Xinchao Chen; Christopher L. Cioffi; Sean Richard Dinn; Ana Maria Escribano; Maria Carmen Fernandez; Todd Fields; Robert Jason Herr; Nathan Bryan Mantlo; De La Nava Eva Maria Martin; Ana Isabel Mateo-Herranz; Saravanan Parthasarathy; Xiaodong Wang
Bioorganic & Medicinal Chemistry Letters | 2005
David Andrew Neel; Matthew L. Brown; Peter Ambrose Lander; Timothy Alan Grese; Jean Marie Defauw; Robert Anthony Doti; Todd Fields; Sally Ann Kelley; Stephon C. Smith; Karen M. Zimmerman; Mitchell I. Steinberg; Prabhakar Kondaji Jadhav
Archive | 2005
Xinchao Chen; Christopher L. Cioffi; Sean Richard Dinn; Ana Maria Escribano; Maria Carmen Fernandez; Todd Fields; Robert Jason Herr; Nathan Bryan Mantlo; Eva Maria Martin De La Nava; Ana Isabel Mateo-Herranz; Saravanan Parthasarathy; Xiaodong Wang
Archive | 2004
Guoqing Cao; Ana Maria Escribano; Maria Carmen Fernandez; Todd Fields; Douglas Linn Gernert; Christopher L. Cioffi; Robert Jason Herr; Nathan Bryan Mantlo; Eva Maria Martin De La Nava; Ana Isabel Mateo Herranz; Daniel Ray Mayhugh; Xiaodong Wang
Archive | 2015
Todd Fields
Archive | 2015
Todd Fields
Archive | 2005
Xinchao Chen; Christopher L. Cioffi; Sean Richard Dinn; Ana Maria Escribano; Maria Carmen Fernandez; Todd Fields; Robert Jason Herr; Nathan Bryan Mantlo; De La Nava Eva Maria Martin; Ana Isabel Mateo-Herranz; Saravanan Parthasarathy; Xiaodong Wang
Archive | 2005
Xinchao Chen; Christopher L. Cioffi; Sean Richard Dinn; Ana Maria Escribano; Maria Carmen Fernandez; Todd Fields; Robert Jason Herr; Nathan Bryan Mantlo; De La Nava Eva Maria Martin; Ana Isabel Mateo-Herranz; Saravanan Parthasarathy; Xiaodong Wang
Archive | 2005
Xinchao Chen; Christopher L. Cioffi; Sean Richard Dinn; Todd Fields; Robert Jason Herr; Nathan Bryan Mantlo; Saravanan Parthasarathy; Xiaodong Wang; Ana Maria Escribano; Maria Carmen Fernandez; De La Nava Eva Maria Martin; Ana Isabel Mateo-Herranz