Evacetrapib (BioDeep_00000762773)

   


代谢物信息卡片


Evacetrapib (LY2484595)

化学式: C31H36F6N6O2 (638.2803788)
中文名称: Evacetrapib
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CC1=CC(=C2C(=C1)C(CCCN2CC3CCC(CC3)C(=O)O)N(CC4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)C5=NN(N=N5)C)C
InChI: InChI=1S/C31H36F6N6O2/c1-18-11-19(2)27-25(12-18)26(5-4-10-42(27)16-20-6-8-22(9-7-20)28(44)45)43(29-38-40-41(3)39-29)17-21-13-23(30(32,33)34)15-24(14-21)31(35,36)37/h11-15,20,22,26H,4-10,16-17H2,1-3H3,(H,44,45)/t20?,22?,26-/m0/s1

描述信息

D057847 - Lipid Regulating Agents > D000960 - Hypolipidemic Agents > D000924 - Anticholesteremic Agents
C78276 - Agent Affecting Digestive System or Metabolism > C29703 - Antilipidemic Agent
D009676 - Noxae > D000963 - Antimetabolites
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.

同义名列表

3 个代谢物同义名

Evacetrapib (LY2484595); Evacetrapib; LY2484595



数据库引用编号

7 个数据库交叉引用编号

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代谢反应

0 个相关的代谢反应过程信息。

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COVID-19 Disease Map(0)

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在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：

  • PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
  • NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
  • Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
  • Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。

点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。



文献列表

  • Jeremy D Furtado, Giacomo Ruotolo, Stephen J Nicholls, Robert Dullea, Santos Carvajal-Gonzalez, Frank M Sacks. Pharmacological Inhibition of CETP (Cholesteryl Ester Transfer Protein) Increases HDL (High-Density Lipoprotein) That Contains ApoC3 and Other HDL Subspecies Associated With Higher Risk of Coronary Heart Disease. Arteriosclerosis, thrombosis, and vascular biology. 2022 02; 42(2):227-237. doi: 10.1161/atvbaha.121.317181. [PMID: 34937388]
  • Amand F Schmidt, Nicholas B Hunt, Maria Gordillo-Marañón, Pimphen Charoen, Fotios Drenos, Mika Kivimaki, Deborah A Lawlor, Claudia Giambartolomei, Olia Papacosta, Nishi Chaturvedi, Joshua C Bis, Christopher J O'Donnell, Goya Wannamethee, Andrew Wong, Jackie F Price, Alun D Hughes, Tom R Gaunt, Nora Franceschini, Dennis O Mook-Kanamori, Magdalena Zwierzyna, Reecha Sofat, Aroon D Hingorani, Chris Finan. Cholesteryl ester transfer protein (CETP) as a drug target for cardiovascular disease. Nature communications. 2021 09; 12(1):5640. doi: 10.1038/s41467-021-25703-3. [PMID: 34561430]
  • Petr Vachal, Joseph L Duffy, Louis-Charles Campeau, Rupesh P Amin, Kaushik Mitra, Beth Ann Murphy, Pengcheng P Shao, Peter J Sinclair, Feng Ye, Revathi Katipally, Zhijian Lu, Debra Ondeyka, Yi-Heng Chen, Kake Zhao, Wanying Sun, Sriram Tyagarajan, Jianming Bao, Sheng-Ping Wang, Josee Cote, Concetta Lipardi, Daniel Metzger, Dennis Leung, Georgy Hartmann, Gordon K Wollenberg, Jian Liu, Lushi Tan, Yingju Xu, Qinghao Chen, Guiquan Liu, Robert O Blaustein, Douglas G Johns. Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties. Journal of medicinal chemistry. 2021 09; 64(18):13215-13258. doi: 10.1021/acs.jmedchem.1c00959. [PMID: 34375108]
  • Anirudh Kumar, Divyang R Patel, Danielle M Brennan, Kathy E Wolski, A Michael Lincoff, Giacomo Ruotolo, Ellen McErlean, Govinda Weerakkody, Jeffrey S Riesmeyer, Stephen J Nicholls, Steven E Nissen, Venu Menon. Plasma Aldosterone Levels Are Not Associated With Cardiovascular Events Among Patients With High-Risk Vascular Disease: Insights From the ACCELERATE Trial. Journal of the American Heart Association. 2019 12; 8(23):e013790. doi: 10.1161/jaha.119.013790. [PMID: 31752637]
  • Zhiwei Yang, Yang Cao, Dongxiao Hao, Xiaohui Yuan, Lei Zhang, Shengli Zhang. Binding profiles of cholesterol ester transfer protein with current inhibitors: a look at mechanism and drawback. Journal of biomolecular structure & dynamics. 2018 Aug; 36(10):2567-2580. doi: 10.1080/07391102.2017.1363661. [PMID: 28777919]
  • Ken Yamada, Margaret Brousseau, Wataru Honma, Akiko Iimura, Hidetomo Imase, Yuki Iwaki, Toshio Kawanami, Daniel LaSala, Guiqing Liang, Hironobu Mitani, Kazuhiko Nonomura, Osamu Ohmori, Meihui Pan, Dean F Rigel, Ichiro Umemura, Kayo Yasoshima, Guoming Zhu, Muneto Mogi. Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma. Journal of medicinal chemistry. 2017 10; 60(20):8466-8481. doi: 10.1021/acs.jmedchem.7b00900. [PMID: 29035537]
  • Dongyin Chen, Xin Huang, Hongwen Zhou, Hanqiong Luo, Pengfei Wang, Yongzhi Chang, Xinyi He, Suiying Ni, Qingqing Shen, Guoshen Cao, Hongbin Sun, Xiaoan Wen, Jun Liu. Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors. European journal of medicinal chemistry. 2017 Oct; 139(?):201-213. doi: 10.1016/j.ejmech.2017.08.012. [PMID: 28802120]
  • Stephen J Nicholls, Kausik K Ray, Christie M Ballantyne, Lauren A Beacham, Debra L Miller, Giacomo Ruotolo, Steven E Nissen, Jeffrey S Riesmeyer. Comparative effects of cholesteryl ester transfer protein inhibition, statin or ezetimibe on lipid factors: The ACCENTUATE trial. Atherosclerosis. 2017 06; 261(?):12-18. doi: 10.1016/j.atherosclerosis.2017.04.008. [PMID: 28412650]
  • Spencer Phillips Hey, Jessica M Franklin, Jerry Avorn, Aaron S Kesselheim. Success, Failure, and Transparency in Biomarker-Based Drug Development: A Case Study of Cholesteryl Ester Transfer Protein Inhibitors. Circulation. Cardiovascular quality and outcomes. 2017 Jun; 10(6):. doi: 10.1161/circoutcomes.116.003121. [PMID: 28611186]
  • A Michael Lincoff, Stephen J Nicholls, Jeffrey S Riesmeyer, Philip J Barter, H Bryan Brewer, Keith A A Fox, C Michael Gibson, Christopher Granger, Venu Menon, Gilles Montalescot, Daniel Rader, Alan R Tall, Ellen McErlean, Kathy Wolski, Giacomo Ruotolo, Burkhard Vangerow, Govinda Weerakkody, Shaun G Goodman, Diego Conde, Darren K McGuire, Jose C Nicolau, Jose L Leiva-Pons, Yves Pesant, Weimin Li, David Kandath, Simon Kouz, Naeem Tahirkheli, Denise Mason, Steven E Nissen. Evacetrapib and Cardiovascular Outcomes in High-Risk Vascular Disease. The New England journal of medicine. 2017 05; 376(20):1933-1942. doi: 10.1056/nejmoa1609581. [PMID: 28514624]
  • Vaughn A Eyvazian, William H Frishman. Evacetrapib: Another CETP Inhibitor for Dyslipidemia With No Clinical Benefit. Cardiology in review. 2017 Mar; 25(2):43-52. doi: 10.1097/crd.0000000000000137. [PMID: 28099220]
  • Ziyun Wang, Manabu Niimi, Qianzhi Ding, Zhenming Liu, Ling Wang, Jifeng Zhang, Jun Xu, Jianglin Fan. Comparative studies of three cholesteryl ester transfer proteins and their interactions with known inhibitors. PloS one. 2017; 12(8):e0180772. doi: 10.1371/journal.pone.0180772. [PMID: 28767652]
  • T D Filippatos, E Klouras, F Barkas, M Elisaf. Cholesteryl ester transfer protein inhibitors: challenges and perspectives. Expert review of cardiovascular therapy. 2016 Aug; 14(8):953-62. doi: 10.1080/14779072.2016.1189327. [PMID: 27171534]
  • David S Small, Jane Royalty, Ellen A Cannady, Christine Hale, Ming-Dauh Wang, Delyn Downs, Jeffrey G Suico. Impact of Increased Gastric pH on the Pharmacokinetics of Evacetrapib in Healthy Subjects. Pharmacotherapy. 2016 07; 36(7):749-56. doi: 10.1002/phar.1778. [PMID: 27284735]
  • Eder C R Quintão. The controversy over the use of cholesteryl ester transfer protein inhibitors: is there some light at the end of the tunnel?. European journal of clinical investigation. 2016 Jun; 46(6):581-9. doi: 10.1111/eci.12626. [PMID: 26992444]
  • Ellen A Cannady, Aktham Aburub, Chris Ward, Chris Hinds, Boris Czeskis, Kenneth Ruterbories, Jeffrey G Suico, Jane Royalty, Demetrio Ortega, Brian W Pack, Syeda L Begum, William F Annes, Qun Lin, David S Small. Absolute bioavailability of evacetrapib in healthy subjects determined by simultaneous administration of oral evacetrapib and intravenous [(13) C8 ]-evacetrapib as a tracer. Journal of labelled compounds & radiopharmaceuticals. 2016 05; 59(6):238-44. doi: 10.1002/jlcr.3358. [PMID: 26639670]
  • Stephen J Nicholls, Giacomo Ruotolo, H Bryan Brewer, Ming-Dauh Wang, Liping Liu, Mark B Willey, Mark A Deeg, Kathryn A Krueger, Steven E Nissen. Evacetrapib alone or in combination with statins lowers lipoprotein(a) and total and small LDL particle concentrations in mildly hypercholesterolemic patients. Journal of clinical lipidology. 2016 May; 10(3):519-527.e4. doi: 10.1016/j.jacl.2015.11.014. [PMID: 27206939]
  • David S Small, Wei Zhang, Jane Royalty, Ellen A Cannady, Delyn Downs, Demetrio Ortega, Jeffrey G Suico. Effect of hepatic or renal impairment on the pharmacokinetics of evacetrapib. European journal of clinical pharmacology. 2016 May; 72(5):563-72. doi: 10.1007/s00228-016-2017-1. [PMID: 26857125]
  • Amirhossein Sahebkar, Luis E Simental-Mendía, Fernando Guerrero-Romero, Jonathan Golledge, Gerald F Watts. Efficacy and Safety of Evacetrapib for Modifying Plasma Lipids: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Current pharmaceutical design. 2016; 22(5):595-608. doi: 10.2174/1381612822666151125000035. [PMID: 26601964]
  • David S Small, Wei Zhang, Jane Royalty, Ellen A Cannady, Delyn Downs, Stuart Friedrich, Jeffrey G Suico. A Multidose Study to Examine the Effect of Food on Evacetrapib Exposure at Steady State. Journal of cardiovascular pharmacology and therapeutics. 2015 Sep; 20(5):483-9. doi: 10.1177/1074248415575153. [PMID: 25736283]
  • Philip J Barter, Stephen J Nicholls, John J P Kastelein, Kerry-Anne Rye. Is Cholesteryl Ester Transfer Protein Inhibition an Effective Strategy to Reduce Cardiovascular Risk? CETP Inhibition as a Strategy to Reduce Cardiovascular Risk: The Pro Case. Circulation. 2015 Aug; 132(5):423-32. doi: 10.1161/circulationaha.114.014025. [PMID: 26240263]
  • G Kees Hovingh, Kausik K Ray, S Matthijs Boekholdt. Is Cholesteryl Ester Transfer Protein Inhibition an Effective Strategy to Reduce Cardiovascular Risk? CETP as a Target to Lower CVD Risk: Suspension of Disbelief?. Circulation. 2015 Aug; 132(5):433-40. doi: 10.1161/circulationaha.115.014026. [PMID: 26240264]
  • Hiroshi Mabuchi, Atsushi Nohara, Akihiro Inazu. Cholesteryl ester transfer protein (CETP) deficiency and CETP inhibitors. Molecules and cells. 2014 Nov; 37(11):777-84. doi: 10.14348/molcells.2014.0265. [PMID: 25410905]
  • Jeffrey G Suico, Ming-Dauh Wang, Stuart Friedrich, Ellen A Cannady, Christopher S Konkoy, Giacomo Ruotolo, Kathryn A Krueger. Effects of the cholesteryl ester transfer protein inhibitor evacetrapib on lipoproteins, apolipoproteins and 24-h ambulatory blood pressure in healthy adults. The Journal of pharmacy and pharmacology. 2014 Nov; 66(11):1576-85. doi: 10.1111/jphp.12287. [PMID: 24961753]
  • Nikhilesh Arya, Mangesh D Kharjul, Chamanlal J Shishoo, Vishnu N Thakare, Kishor S Jain. Some molecular targets for antihyperlipidemic drug research. European journal of medicinal chemistry. 2014 Oct; 85(?):535-68. doi: 10.1016/j.ejmech.2014.08.013. [PMID: 25127148]
  • Amirhossein Sahebkar, Gerard T Chew, Gerald F Watts. Recent advances in pharmacotherapy for hypertriglyceridemia. Progress in lipid research. 2014 Oct; 56(?):47-66. doi: 10.1016/j.plipres.2014.07.002. [PMID: 25083925]
  • Tamio Teramoto, Masakazu Takeuchi, Yoji Morisaki, Giacomo Ruotolo, Kathryn A Krueger. Efficacy, safety, tolerability, and pharmacokinetic profile of evacetrapib administered as monotherapy or in combination with atorvastatin in Japanese patients with dyslipidemia. The American journal of cardiology. 2014 Jun; 113(12):2021-9. doi: 10.1016/j.amjcard.2014.03.045. [PMID: 24786356]
  • Jeffrey G Suico, Stuart Friedrich, Kathryn A Krueger, Wei Zhang. Evacetrapib at a supratherapeutic steady state concentration does not prolong QT in a thorough QT/QTc study in healthy participants. Journal of cardiovascular pharmacology and therapeutics. 2014 May; 19(3):283-9. doi: 10.1177/1074248413510784. [PMID: 24271137]
  • Nathan B Mantlo, Ana Escribano. Update on the discovery and development of cholesteryl ester transfer protein inhibitors for reducing residual cardiovascular risk. Journal of medicinal chemistry. 2014 Jan; 57(1):1-17. doi: 10.1021/jm400574e. [PMID: 23941686]
  • Ioanna Gouni-Berthold, Heiner K Berthold. Familial hypercholesterolemia: etiology, diagnosis and new treatment options. Current pharmaceutical design. 2014; 20(40):6220-9. doi: 10.2174/1381612820666140620125213. [PMID: 24953396]
  • Hyun Joon Shin, Peter A McCullough. Focus on lipids: high-density lipoprotein cholesterol and its associated lipoproteins in cardiac and renal disease. Nephron. Clinical practice. 2014; 127(1-4):158-64. doi: 10.1159/000363552. [PMID: 25343842]
  • Daniel J Rader, Emil M deGoma. Future of cholesteryl ester transfer protein inhibitors. Annual review of medicine. 2014; 65(?):385-403. doi: 10.1146/annurev-med-050311-163305. [PMID: 24422575]
  • Amir Hooshang Mohammadpour, Fatemeh Akhlaghi. Future of cholesteryl ester transfer protein (CETP) inhibitors: a pharmacological perspective. Clinical pharmacokinetics. 2013 Aug; 52(8):615-26. doi: 10.1007/s40262-013-0071-8. [PMID: 23658137]
  • Chuanwei Li, Wen Zhang, Faying Zhou, Caiyu Chen, Liang Zhou, Yafei Li, Ling Liu, Fang Pei, Hao Luo, Zhangxue Hu, Jing Cai, Chunyu Zeng. Cholesteryl ester transfer protein inhibitors in the treatment of dyslipidemia: a systematic review and meta-analysis. PloS one. 2013; 8(10):e77049. doi: 10.1371/journal.pone.0077049. [PMID: 24204732]
  • Bernd Hewing, Edward A Fisher. Rationale for cholesteryl ester transfer protein inhibition. Current opinion in lipidology. 2012 Aug; 23(4):372-6. doi: 10.1097/mol.0b013e328353ef1d. [PMID: 22517614]
  • Stephen J Nicholls. Evacetrapib. Current cardiology reports. 2012 Jun; 14(3):245-50. doi: 10.1007/s11886-012-0252-3. [PMID: 22362199]
  • Maria-Carmen Fernandez, Ana Escribano, Ana I Mateo, Saravanan Parthasarathy, Eva M Martin de la Nava, Xiaodong Wang, Sandra L Cockerham, Thomas P Beyer, Robert J Schmidt, Guoqing Cao, Youyan Zhang, Timothy M Jones, Anthony Borel, Stephanie A Sweetana, Ellen A Cannady, Gregory Stephenson, Scott Frank, Nathan B Mantlo. Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors. Bioorganic & medicinal chemistry letters. 2012 May; 22(9):3056-62. doi: 10.1016/j.bmcl.2012.03.075. [PMID: 22497761]
  • Alyse S Goldberg, Robert A Hegele. Cholesteryl ester transfer protein inhibitors for dyslipidemia: focus on dalcetrapib. Drug design, development and therapy. 2012; 6(?):251-9. doi: 10.2147/dddt.s34976. [PMID: 23055695]
  • 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 B Mantlo. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure. Journal of lipid research. 2011 Dec; 52(12):2169-2176. doi: 10.1194/jlr.m018069. [PMID: 21957197]
  • Ján Murín, Miroslav Pernický, Soňa Kiňová. [Treatment of dyslipidemia - is here still place for CETP-inhibitors?]. Vnitrni lekarstvi. Fall 201; 62(10):789-794. doi: NULL. [PMID: 27900865]