A Site and Subject Blinded Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of BMS 852927 in Patients With Primary Hypercholesterolemia on a Stable Dose of Statin Therapy

The purpose of this study is to evaluate the safety of BMS-852927 after 28 days of dosing in patients with high cholesterol.

开始日期2012-11-01

申办/合作机构

Bristol Myers Squibb Co.

100 项与 BMS-852927 相关的临床结果

登录后查看更多信息

100 项与 BMS-852927 相关的转化医学

登录后查看更多信息

100 项与 BMS-852927 相关的专利（医药）

登录后查看更多信息

项与 BMS-852927 相关的文献（医药）

2016-08-01·Cell Metabolism1区 · 生物学

Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils

1区 · 生物学

Article

作者: Sleph, Paul ; Garcia, Ricardo ; Grimm, Denise ; Zhang, Jane ; Malone, Harold ; Shipkova, Petia ; Salvador, Lisa ; Gandhi, Mohit D ; Wang, Zhaoqing ; Lee, John ; Ryan, Carol S ; Zhu, Jun ; Garmise, Robert J ; Martin, Richard ; Mohan, Raju ; Lupisella, John ; Ostrowski, Jacek ; Liu, Xiaoqin ; Zhang, Rongan ; Kick, Ellen ; Frost, Robert J A ; Barrett, Yu Chen ; Behnia, Kamelia ; Li, Tong ; Du, Shuyan ; He, Aiqing ; Wastall, Philip ; Yuan, Long ; Fernando, Gayani ; Cantor, Glenn H ; Kirchgessner, Todd G

The development of LXR agonists for the treatment of coronary artery disease has been challenged by undesirable properties in animal models. Here we show the effects of an LXR agonist on lipid and lipoprotein metabolism and neutrophils in human subjects. BMS-852927, a novel LXRβ-selective compound, had favorable profiles in animal models with a wide therapeutic index in cynomolgus monkeys and mice. In healthy subjects and hypercholesterolemic patients, reverse cholesterol transport pathways were induced similarly to that in animal models. However, increased plasma and hepatic TG, plasma LDL-C, apoB, apoE, and CETP and decreased circulating neutrophils were also evident. Furthermore, similar increases in LDL-C were observed in normocholesterolemic subjects and statin-treated patients. The primate model markedly underestimated human lipogenic responses and did not predict human neutrophil effects. These studies demonstrate both beneficial and adverse LXR agonist clinical responses and emphasize the importance of further translational research in this area.

100 项与 BMS-852927 相关的药物交易

登录后查看更多信息

研发状态

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
原发性高胆固醇血症	临床1期	加拿大	Bristol Myers Squibb Co.	2012-11-01
原发性高胆固醇血症	临床1期	德国	Bristol Myers Squibb Co.	2012-11-01
动脉粥样硬化	临床1期	美国	Bristol Myers Squibb Co.	-
动脉粥样硬化	临床1期	-	Exelixis, Inc.	-