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Review Article

降低胆固醇的三大利器:他汀类药物，依折麦布和依伏库单抗

卷 28, 期 5, 2021

发表于: 05 May, 2020

页: [1025 - 1041] 页: 17

弟呕挨: 10.2174/0929867327666200505091738

价格: $65

摘要

冠心病与高胆固醇血症密切相关，降低血清胆固醇是目前降低冠心病最重要的策略。在人体内，血清胆固醇水平主要是由三条代谢途径决定的，即膳食中胆固醇的摄入、胆固醇的合成和体内胆固醇的降解。针对三种途径的关键分子进行干预是降低血脂的重要策略。他汀类药物可抑制3-羟基-3-甲基戊二酰辅酶A还原酶(HMG-CoA还原酶)，使低密度脂蛋白(LDL)降低约20%至45%。然而，高达15%的患者不能忍受高剂量他汀类药物的潜在副作用，一些患者在接受他汀类药物治疗后仍不能达到其理想的LDL目标。依折麦布通过靶向Niemann-Pick C1-like 1蛋白(NPC1L1)来抑制胆固醇吸收，该蛋白与胆固醇在肠道中的吸收有关。依折麦布单独使用时可降低约18%的LDL，与他汀联合使用时可额外降低25%。原蛋白转化酶枯草素/可心9型(PCSK9)增加肝脏低密度脂蛋白的降解，从而降低肝脏清除低密度脂蛋白的能力，从而导致高胆固醇血症。Evolocumab是PCSK9单克隆抗体，可将LDL从基线水平降低53%至56%。这三种药物通过调节脂质代谢的三个关键通路发挥降脂作用。any在他汀治疗的基础上与其他两种药物联合使用，提高了降脂效果。三者结合是否能减少单药治疗的副作用，达到降脂的效果还有待进一步研究。

关键词: 冠心病，高胆固醇血症，胆固醇代谢，他汀类药物，依折麦布，依伏库单抗

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[1]
Murray, C.J.L.; Lopez, A.D. Mortality by cause for eight regions of the world: Global Burden of Disease Study. Lancet, 1997, 349(9061), 1269-1276.
[http://dx.doi.org/10.1016/S0140-6736(96)07493-4] [PMID: 9142060]
[2]
Niccoli, G.; Scalone, G.; Crea, F. Acute myocardial infarction with no obstructive coronary atherosclerosis: mechanisms and management. Eur. Heart J., 2015, 36(8), 475-481.
[http://dx.doi.org/10.1093/eurheartj/ehu469] [PMID: 25526726]
[3]
Roh, E.; Ko, S-H.; Kwon, H-S.; Kim, N.H.; Kim, J.H.; Kim, C.S.; Song, K-H.; Won, J.C.; Kim, D.J.; Choi, S.H.; Lim, S.; Cha, B-Y. Taskforce team of diabetes fact sheet of the Korean Diabetes Association. Prevalence and management of dyslipidemia in Korea: Korea national health and nutrition examination survey during 1998 to 2010. Diabetes Metab. J., 2013, 37(6), 433-449.
[http://dx.doi.org/10.4093/dmj.2013.37.6.433] [PMID: 24404515]
[4]
Robinson, J.G. Management of familial hypercholesterolemia: a review of the recommendations from the National Lipid Association expert panel on familial hypercholesterolemia. J. Manag. Care Pharm., 2013, 19(2), 139-149.
[http://dx.doi.org/10.18553/jmcp.2013.19.2.139] [PMID: 23461430]
[5]
Cohen, J.C.; Boerwinkle, E.; Mosley, T.H. Jr.; Hobbs, H.H. Sequence variations in PCSK9, low LDL, and protection against coronary heart disease. N. Engl. J. Med., 2006, 354(12), 1264-1272.
[http://dx.doi.org/10.1056/NEJMoa054013] [PMID: 16554528]
[6]
Nihei, W.; Nagafuku, M.; Hayamizu, H.; Odagiri, Y.; Tamura, Y.; Kikuchi, Y.; Veillon, L.; Kanoh, H.; Inamori, K.I.; Arai, K.; Kabayama, K.; Fukase, K.; Inokuchi, J.I. NPC1L1-dependent intestinal cholesterol absorption requires ganglioside GM3 in membrane microdomains. J. Lipid Res., 2018, 59(11), 2181-2187.
[http://dx.doi.org/10.1194/jlr.M089201] [PMID: 30242108]
[7]
Alberts, A.W.; Chen, J.; Kuron, G.; Hunt, V.; Huff, J.; Hoffman, C.; Rothrock, J.; Lopez, M.; Joshua, H.; Harris, E.; Patchett, A.; Monaghan, R.; Currie, S.; Stapley, E.; Albers-Schonberg, G.; Hensens, O.; Hirshfield, J.; Hoogsteen, K.; Liesch, J.; Springer, J. Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent. Proc. Natl. Acad. Sci. USA, 1980, 77(7), 3957-3961.
[http://dx.doi.org/10.1073/pnas.77.7.3957] [PMID: 6933445]
[8]
Smart, E.J.; De Rose, R.A.; Farber, S.A. Annexin 2-caveolin 1 complex is a target of ezetimibe and regulates intestinal cholesterol transport. Proc. Natl. Acad. Sci. USA, 2004, 101(10), 3450-3455.
[http://dx.doi.org/10.1073/pnas.0400441101] [PMID: 14985510]
[9]
Dias, C.S.; Shaywitz, A.J.; Wasserman, S.M.; Smith, B.P.; Gao, B.; Stolman, D.S.; Crispino, C.P.; Smirnakis, K.V.; Emery, M.G.; Colbert, A.; Gibbs, J.P.; Retter, M.W.; Cooke, B.P.; Uy, S.T.; Matson, M.; Stein, E.A. Effects of AMG 145 on low-density lipoprotein cholesterol levels: results from 2 randomized, double-blind, placebo-controlled, ascending-dose phase 1 studies in healthy volunteers and hypercholesterolemic subjects on statins. J. Am. Coll. Cardiol., 2012, 60(19), 1888-1898.
[http://dx.doi.org/10.1016/j.jacc.2012.08.986] [PMID: 23083772]
[10]
Endo, A.; Kuroda, M.; Tanzawa, K. Competitive inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase by ML-236A and ML-236B fungal metabolites, having hypocholesterolemic activity. FEBS Lett., 1976, 72(2), 323-326.
[http://dx.doi.org/10.1016/0014-5793(76)80996-9] [PMID: 16386050]
[11]
Singer, I.I.; Scott, S.; Kazazis, D.M.; Huff, J.W. Lovastatin, an inhibitor of cholesterol synthesis, induces hydroxymethylglutaryl-coenzyme A reductase directly on membranes of expanded smooth endoplasmic reticulum in rat hepatocytes. Proc. Natl. Acad. Sci. USA, 1988, 85(14), 5264-5268.
[http://dx.doi.org/10.1073/pnas.85.14.5264] [PMID: 3293052]
[12]
Steinberg, D. Thematic review series: the pathogenesis of atherosclerosis. An interpretive history of the cholesterol controversy, part V: the discovery of the statins and the end of the controversy. J. Lipid Res., 2006, 47(7), 1339-1351.
[http://dx.doi.org/10.1194/jlr.R600009-JLR200] [PMID: 16585781]
[13]
Goldstein, J.L.; Brown, M.S. A century of cholesterol and coronaries: from plaques to genes to statins. Cell, 2015, 161(1), 161-172.
[http://dx.doi.org/10.1016/j.cell.2015.01.036] [PMID: 25815993]
[14]
Oliveira, E.F.; Santos-Martins, D.; Ribeiro, A.M.; Brás, N.F.; Cerqueira, N.S.; Sousa, S.F.; Ramos, M.J.; Fernandes, P.A. HMG-CoA Reductase inhibitors: an updated review of patents of novel compounds and formulations (2011-2015). Expert Opin. Ther. Pat., 2016, 26(11), 1257-1272.
[http://dx.doi.org/10.1080/13543776.2016.1216977] [PMID: 27537201]
[15]
Bone, E.A.; Davidson, A.H.; Lewis, C.N.; Todd, R.S. Synthesis and biological evaluation of dihydroeptastatin, a novel inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. J. Med. Chem., 1992, 35(18), 3388-3393.
[http://dx.doi.org/10.1021/jm00096a015] [PMID: 1527791]
[16]
Hoffman, W.F.; Alberts, A.W.; Anderson, P.S.; Chen, J.S.; Smith, R.L.; Willard, A.K. 3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 4. Side chain ester derivatives of mevinolin. J. Med. Chem., 1986, 29(5), 849-852.
[http://dx.doi.org/10.1021/jm00155a040] [PMID: 3634830]
[17]
Connolly, P.J.; Westin, C.D.; Loughney, D.A.; Minor, L.K. HMG-CoA reductase inhibitors: design, synthesis, and biological activity of tetrahydroindazole-substituted 3,5-dihydroxy-6-heptenoic acid sodium salts. J. Med. Chem., 1993, 36(23), 3674-3685.
[http://dx.doi.org/10.1021/jm00075a024] [PMID: 8246237]
[18]
Roth, B.D. The discovery and development of atorvastatin, a potent novel hypolipidemic agent. Prog. Med. Chem., 2002, 40, 1-22.
[http://dx.doi.org/10.1016/S0079-6468(08)70080-8] [PMID: 12516521]
[19]
Park, W.K.; Kennedy, R.M.; Larsen, S.D.; Miller, S.; Roth, B.D.; Song, Y.; Steinbaugh, B.A.; Sun, K.; Tait, B.D.; Kowala, M.C.; Trivedi, B.K.; Auerbach, B.; Askew, V.; Dillon, L.; Hanselman, J.C.; Lin, Z.; Lu, G.H.; Robertson, A.; Sekerke, C. Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors. Bioorg. Med. Chem. Lett., 2008, 18(3), 1151-1156.
[http://dx.doi.org/10.1016/j.bmcl.2007.11.124] [PMID: 18155906]
[20]
Davidson, M.H. Rosuvastatin: a highly efficacious statin for the treatment of dyslipidaemia. Expert Opin. Investig. Drugs, 2002, 11(1), 125-141.
[PMID: 12769127]
[21]
Schachter, M. Chemical, pharmacokinetic and pharmacodynamic properties of statins: an update. Fundam. Clin. Pharmacol., 2005, 19(1), 117-125.
[http://dx.doi.org/10.1111/j.1472-8206.2004.00299.x] [PMID: 15660968]
[22]
Holdgate, G.A.; Ward, W.H.; McTaggart, F. Molecular mechanism for inhibition of 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase by rosuvastatin. Biochem. Soc. Trans., 2003, 31(Pt 3), 528-531.
[http://dx.doi.org/10.1042/bst0310528] [PMID: 12773150]
[23]
Hirano, M.; Maeda, K.; Matsushima, S.; Nozaki, Y.; Kusuhara, H.; Sugiyama, Y. Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin. Mol. Pharmacol., 2005, 68(3), 800-807.
[http://dx.doi.org/10.1124/mol.105.014019] [PMID: 15955871]
[24]
Wang, S-R.; Chen, Y.; Wu, L-P.; Miao, W-J.; Xiong, M-J.; Chen, C.; Zhong, Z-R.; Ye, L-M. Development of predictive quantitative retention-activity relationship models of HMG-CoA reductase inhibitors by biopartitioning micellar chromatography. J. Pharm. Biomed. Anal., 2008, 46(2), 243-249.
[http://dx.doi.org/10.1016/j.jpba.2007.09.024] [PMID: 18024049]
[25]
Istvan, E.S. Structural mechanism for statin inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Am. Heart J., 2002, 144(6)(Suppl.), S27-S32.
[http://dx.doi.org/10.1067/mhj.2002.130300] [PMID: 12486413]
[26]
Hobbs, H.H.; Brown, M.S.; Goldstein, J.L. Molecular genetics of the LDL receptor gene in familial hypercholesterolemia. Hum. Mutat., 1992, 1(6), 445-466.
[http://dx.doi.org/10.1002/humu.1380010602] [PMID: 1301956]
[27]
Istvan, E.S.; Deisenhofer, J. Structural mechanism for statin inhibition of HMG-CoA reductase. Science, 2001, 292(5519), 1160-1164.
[http://dx.doi.org/10.1126/science.1059344] [PMID: 11349148]
[28]
Endo, A. A gift from nature: the birth of the statins. Nat. Med., 2008, 14(10), 1050-1052.
[http://dx.doi.org/10.1038/nm1008-1050] [PMID: 18841147]
[29]
Endo, A. The discovery and development of HMG-CoA reductase inhibitors. J. Lipid Res., 1992, 33(11), 1569-1582.
[PMID: 1464741]
[30]
Tsujita, Y.; Kuroda, M.; Tanzawa, K.; Kitano, N.; Endo, A. Hypolipidemic effects in dogs of ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Atherosclerosis, 1979, 32(3), 307-313.
[http://dx.doi.org/10.1016/0021-9150(79)90174-6] [PMID: 223590]
[31]
Bilheimer, D.W.; Grundy, S.M.; Brown, M.S.; Goldstein, J.L. Mevinolin and colestipol stimulate receptor-mediated clearance of low density lipoprotein from plasma in familial hypercholesterolemia heterozygotes. Proc. Natl. Acad. Sci. USA, 1983, 80(13), 4124-4128.
[http://dx.doi.org/10.1073/pnas.80.13.4124] [PMID: 6575399]
[32]
Deedwania, P.C.; Shepherd, J.; Breazna, A.; De Micco, D.A. Treating to New Targets (TNT) Steering Committee Investigators. Effect of high-dose atorvastatin on the cardiovascular risk associated with individual components of metabolic syndrome: a subanalysis of the Treating to New Targets (TNT) study. Diabetes Obes. Metab., 2016, 18(1), 56-63.
[http://dx.doi.org/10.1111/dom.12581] [PMID: 26434404]
[33]
Downs, J.R.; Clearfield, M.; Weis, S.; Whitney, E.; Shapiro, D.R.; Beere, P.A.; Langendorfer, A.; Stein, E.A.; Kruyer, W.; Gotto, A.M. Jr. Primary prevention of acute coronary events with lovastatin in men and women with average cholesterol levels: results of AFCAPS/TexCAPS. Air Force/Texas Coronary Atherosclerosis Prevention Study. JAMA, 1998, 279(20), 1615-1622.
[http://dx.doi.org/10.1001/jama.279.20.1615] [PMID: 9613910]
[34]
Sever, P.S.; Dahlöf, B.; Poulter, N.R.; Wedel, H.; Beevers, G.; Caulfield, M.; Collins, R.; Kjeldsen, S.E.; Kristinsson, A.; McInnes, G.T.; Mehlsen, J.; Nieminen, M.; O’Brien, E.; Ostergren, J. ASCOT investigators. Prevention of coronary and stroke events with atorvastatin in hypertensive patients who have average or lower-than-average cholesterol concentrations, in the Anglo-Scandinavian Cardiac Outcomes Trial--Lipid Lowering Arm (ASCOT-LLA): a multicentre randomised controlled trial. Lancet, 2003, 361(9364), 1149-1158.
[http://dx.doi.org/10.1016/S0140-6736(03)12948-0] [PMID: 12686036]
[35]
Asselbergs, F.W.; Diercks, G.F.; Hillege, H.L.; van Boven, A.J.; Janssen, W.M.; Voors, A.A.; de Zeeuw, D.; de Jong, P.E.; van Veldhuisen, D.J.; van Gilst, W.H. Prevention of renal and vascular endstage disease intervention trial (PREVEND IT) investigators. Effects of fosinopril and pravastatin on cardiovascular events in subjects with microalbuminuria. Circulation, 2004, 110(18), 2809-2816.
[http://dx.doi.org/10.1161/01.CIR.0000146378.65439.7A] [PMID: 15492322]
[36]
Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: the Scandinavian Simvastatin Survival Study (4S). Lancet, 1994, 344(8934), 1383-1389.
[PMID: 7968073]
[37]
Shepherd, J.; Cobbe, S.M.; Ford, I.; Isles, C.G.; Lorimer, A.R.; MacFarlane, P.W.; McKillop, J.H.; Packard, C.J. West of Scotland Coronary Prevention Study Group. Prevention of coronary heart disease with pravastatin in men with hypercholesterolemia. N. Engl. J. Med., 1995, 333(20), 1301-1307.
[http://dx.doi.org/10.1056/NEJM199511163332001] [PMID: 7566020]
[38]
Sacks, F.M.; Pfeffer, M.A.; Moye, L.A.; Rouleau, J.L.; Rutherford, J.D.; Cole, T.G.; Brown, L.; Warnica, J.W.; Arnold, J.M.; Wun, C.C.; Davis, B.R.; Braunwald, E. The effect of pravastatin on coronary events after myocardial infarction in patients with average cholesterol levels. Cholesterol and recurrent events trial investigators. N. Engl. J. Med., 1996, 335(14), 1001-1009.
[http://dx.doi.org/10.1056/NEJM199610033351401] [PMID: 8801446]
[39]
Hague, W.E.; Simes, J.; Kirby, A.; Keech, A.C.; White, H.D.; Hunt, D.; Nestel, P.J.; Colquhoun, D.M.; Pater, H.; Stewart, R.A.; Sullivan, D.R.; Thompson, P.L.; West, M.; Glasziou, P.P.; Tonkin, A.M. LIPID study investigators. Long-term effectiveness and safety of pravastatin in patients with coronary heart disease: sixteen years of follow-up of the LIPID study. Circulation, 2016, 133(19), 1851-1860.
[http://dx.doi.org/10.1161/CIRCULATIONAHA.115.018580] [PMID: 27016105]
[40]
Heart Protection Study Collaborative Group. MRC/BHF Heart Protection Study of cholesterol lowering with simvastatin in 20,536 high-risk individuals: a randomised placebo-controlled trial. Lancet, 2002, 360(9326), 7-22.
[http://dx.doi.org/10.1016/S0140-6736(02)09327-3] [PMID: 12114036]
[41]
Shepherd, J.; Blauw, G.J.; Murphy, M.B.; Bollen, E.L.; Buckley, B.M.; Cobbe, S.M.; Ford, I.; Gaw, A.; Hyland, M.; Jukema, J.W.; Kamper, A.M.; Macfarlane, P.W.; Meinders, A.E.; Norrie, J.; Packard, C.J.; Perry, I.J.; Stott, D.J.; Sweeney, B.J.; Twomey, C.; Westendorp, R.G.; Risk, P.P.S.P.E. PROSPER study group. Prospective study of pravastatin in the elderly at risk. Pravastatin in elderly individuals at risk of vascular disease (PROSPER): a randomised controlled trial. Lancet, 2002, 360(9346), 1623-1630.
[http://dx.doi.org/10.1016/S0140-6736(02)11600-X] [PMID: 12457784]
[42]
Mosley, S.T.; Kalinowski, S.S.; Schafer, B.L.; Tanaka, R.D. Tissue-selective acute effects of inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase on cholesterol biosynthesis in lens. J. Lipid Res., 1989, 30(9), 1411-1420.
[PMID: 2513368]
[43]
White, C.M. A review of the pharmacologic and pharmacokinetic aspects of rosuvastatin. J. Clin. Pharmacol., 2002, 42(9), 963-970.
[http://dx.doi.org/10.1177/009127002401102876] [PMID: 12211221]
[44]
Ford, I.; Murray, H.; McCowan, C.; Packard, C.J. Long-term safety and efficacy of lowering low-density lipoprotein cholesterol with statin therapy: 20-year follow-up of West of Scotland Coronary Prevention Study. Circulation, 2016, 133(11), 1073-1080.
[http://dx.doi.org/10.1161/CIRCULATIONAHA.115.019014] [PMID: 26864092]
[45]
Nicholls, S.J.; Tuzcu, E.M.; Sipahi, I.; Schoenhagen, P.; Hazen, S.L.; Ntanios, F.; Wun, C.C.; Nissen, S.E. Effects of obesity on lipid-lowering, anti-inflammatory, and antiatherosclerotic benefits of atorvastatin or pravastatin in patients with coronary artery disease (from the REVERSAL Study). Am. J. Cardiol., 2006, 97(11), 1553-1557.
[http://dx.doi.org/10.1016/j.amjcard.2005.12.042] [PMID: 16728212]
[46]
Scheen, A.J. [JUPITER: reduction by rosuvastatin of cardiovascular events and mortality in healthy subjects without hyperlipidaemia but with elevated C-reactive protein] Rev. Med. Liege, 2008, 63(12), 749-753.
[PMID: 19180837]
[47]
Chan, K.L.; Teo, K.; Dumesnil, J.G.; Ni, A.; Tam, J.; Investigators, A. ASTRONOMER Investigators. Effect of Lipid lowering with rosuvastatin on progression of aortic stenosis: results of the aortic stenosis progression observation: measuring effects of rosuvastatin (ASTRONOMER) trial. Circulation, 2010, 121(2), 306-314.
[http://dx.doi.org/10.1161/CIRCULATIONAHA.109.900027] [PMID: 20048204]
[48]
Yusuf, S.; Panju, A.; Jaeschke, R. HOPE- 3, BP treatment, milestones in CV prevention. Dr. Salim Yusuf in an interview with Dr. Akbar Panju and Dr. Roman Jaeschke. Pol. Arch. Med. Wewn., 2016, 126(12), 1033-1035.
[http://dx.doi.org/10.20452/pamw.3765] [PMID: 28010010]
[49]
DuBroff, R.; de Lorgeril, M. Cholesterol confusion and statin controversy. World J. Cardiol., 2015, 7(7), 404-409.
[http://dx.doi.org/10.4330/wjc.v7.i7.404] [PMID: 26225201]
[50]
Artola, R.T.; Mihos, C.G.; Santana, O. Effects of statin therapy in patients with systemic lupus erythematosus. South. Med. J., 2016, 109(11), 705-711.
[http://dx.doi.org/10.14423/SMJ.0000000000000561] [PMID: 27812716]
[51]
Verdoia, M.; Pergolini, P.; Rolla, R.; Nardin, M.; Schaffer, A.; Barbieri, L.; Daffara, V.; Marino, P.; Bellomo, G.; Suryapranata, H.; De Luca, G. Novara atherosclerosis study Group (NAS). Impact of high-dose statins on vitamin D levels and platelet function in patients with coronary artery disease. Thromb. Res., 2017, 150, 90-95.
[http://dx.doi.org/10.1016/j.thromres.2016.12.019] [PMID: 28068529]
[52]
Sukpat, S.; Israsena, N.; Patumraj, S. Pleiotropic effects of simvastatin on wound healing in Diabetic Mice. J. Med. Assoc. Thai., 2016, 99(2), 213-219.
[PMID: 27249902]
[53]
Tun, T.; Kang, Y.S. Effects of simvastatin on CAT-1-mediated arginine transport and NO level under high glucose conditions in conditionally immortalized rat inner blood-retinal barrier cell lines (TR-iBRB). Microvasc. Res., 2017, 111, 60-66.
[http://dx.doi.org/10.1016/j.mvr.2017.01.002] [PMID: 28089735]
[54]
Rossi, A.; Inciardi, R.M.; Rossi, A.; Temporelli, P.L.; Lucci, D.; Gonzini, L.; Marchioli, R.; Nicolosi, G.L.; Tavazzi, L. GISSI-HF Investigators. Prognostic effects of rosuvastatin in patients with co-existing chronic obstructive pulmonary disease and chronic heart failure: A sub-analysis of GISSI-HF trial. Pulm. Pharmacol. Ther., 2017, 44, 16-23.
[http://dx.doi.org/10.1016/j.pupt.2017.03.001] [PMID: 28263812]
[55]
Oesterle, A.; Laufs, U.; Liao, J.K. Pleiotropic effects of statins on the cardiovascular system. Circ. Res., 2017, 120(1), 229-243.
[http://dx.doi.org/10.1161/CIRCRESAHA.116.308537] [PMID: 28057795]
[56]
Byrne, P.; Cullinan, J.; Smith, S.M. Statins for primary prevention of cardiovascular disease. BMJ, 2019, 367, l5674.
[http://dx.doi.org/10.1136/bmj.l5674] [PMID: 31619406]
[57]
Kavalipati, N.; Shah, J.; Ramakrishan, A.; Vasnawala, H. Pleiotropic effects of statins. Indian J. Endocrinol. Metab., 2015, 19(5), 554-562.
[http://dx.doi.org/10.4103/2230-8210.163106] [PMID: 26425463]
[58]
Lalani, S.R.; Vladutiu, G.D.; Plunkett, K.; Lotze, T.E.; Adesina, A.M.; Scaglia, F. Isolated mitochondrial myopathy associated with muscle coenzyme Q10 deficiency. Arch. Neurol., 2005, 62(2), 317-320.
[http://dx.doi.org/10.1001/archneur.62.2.317] [PMID: 15710863]
[59]
Stroes, E.S.; Thompson, P.D.; Corsini, A.; Vladutiu, G.D.; Raal, F.J.; Ray, K.K.; Roden, M.; Stein, E.; Tokgözoğlu, L.; Nordestgaard, B.G.; Bruckert, E.; De Backer, G.; Krauss, R.M.; Laufs, U.; Santos, R.D.; Hegele, R.A.; Hovingh, G.K.; Leiter, L.A.; Mach, F.; März, W.; Newman, C.B.; Wiklund, O.; Jacobson, T.A.; Catapano, A.L.; Chapman, M.J.; Ginsberg, H.N. European Atherosclerosis Society Consensus Panel. Statin-associated muscle symptoms: impact on statin therapy-European atherosclerosis society consensus panel statement on assessment, aetiology and management. Eur. Heart J., 2015, 36(17), 1012-1022.
[http://dx.doi.org/10.1093/eurheartj/ehv043] [PMID: 25694464]
[60]
Meng, C.Q. Ezetimibe. Schering-Plough. Curr. Opin. Investig. Drugs, 2002, 3(3), 427-432.
[PMID: 12054091]
[61]
Patrick, J.E.; Kosoglou, T.; Stauber, K.L.; Alton, K.B.; Maxwell, S.E.; Zhu, Y.; Statkevich, P.; Iannucci, R.; Chowdhury, S.; Affrime, M.; Cayen, M.N. Disposition of the selective cholesterol absorption inhibitor ezetimibe in healthy male subjects. Drug Metab. Dispos., 2002, 30(4), 430-437.
[http://dx.doi.org/10.1124/dmd.30.4.430] [PMID: 11901097]
[62]
van Heek, T.; Rader, A.E.; Offerhaus, G.J.; McCarthy, D.M.; Goggins, M.; Hruban, R.H.; Wilentz, R.E. K-ras, p53, and DPC4 (MAD4) alterations in fine-needle aspirates of the pancreas: a molecular panel correlates with and supplements cytologic diagnosis. Am. J. Clin. Pathol., 2002, 117(5), 755-765.
[http://dx.doi.org/10.1309/5RQ0-JCQU-5XF2-51LQ] [PMID: 12090425]
[63]
Clader, J.W. The discovery of ezetimibe: a view from outside the receptor. J. Med. Chem., 2004, 47(1), 1-9.
[http://dx.doi.org/10.1021/jm030283g] [PMID: 14695813]
[64]
Kosoglou, T.; Statkevich, P.; Johnson-Levonas, A.O.; Paolini, J.F.; Bergman, A.J.; Alton, K.B. Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin. Pharmacokinet., 2005, 44(5), 467-494.
[http://dx.doi.org/10.2165/00003088-200544050-00002] [PMID: 15871634]
[65]
Nutescu, E.A.; Shapiro, N.L. Ezetimibe: a selective cholesterol absorption inhibitor. Pharmacotherapy, 2003, 23(11), 1463-1474.
[http://dx.doi.org/10.1592/phco.23.14.1463.31942] [PMID: 14620392]
[66]
Phan, B.A.; Dayspring, T.D.; Toth, P.P. Ezetimibe therapy: mechanism of action and clinical update. Vasc. Health Risk Manag., 2012, 8, 415-427.
[http://dx.doi.org/10.2147/VHRM.S33664] [PMID: 22910633]
[67]
Kajinami, K.; Takekoshi, N. Cholesterol absorption inhibitors in development as potential therapeutics. Expert Opin. Investig. Drugs, 2002, 11(6), 831-835.
[http://dx.doi.org/10.1517/13543784.11.6.831] [PMID: 12036426]
[68]
Miettinen, T.A. Cholesterol absorption inhibition: a strategy for cholesterol-lowering therapy. Int. J. Clin. Pract., 2001, 55(10), 710-716.
[PMID: 11777299]
[69]
Miura, S.; Saku, K. Ezetimibe, a selective inhibitor of the transport of cholesterol. Intern. Med., 2008, 47(13), 1165-1170.
[http://dx.doi.org/10.2169/internalmedicine.47.1099] [PMID: 18591835]
[70]
Clarenbach, J.J.; Reber, M.; Lütjohann, D.; von Bergmann, K.; Sudhop, T. The lipid-lowering effect of ezetimibe in pure vegetarians. J. Lipid Res., 2006, 47(12), 2820-2824.
[http://dx.doi.org/10.1194/jlr.P600009-JLR200] [PMID: 16966491]
[71]
Wierzbicki, A.S.; Doherty, E.; Lumb, P.J.; Chik, G.; Crook, M.A. Efficacy of ezetimibe in patients with statin-resistant and statin-intolerant familial hyperlipidaemias. Curr. Med. Res. Opin., 2005, 21(3), 333-338.
[http://dx.doi.org/10.1185/030079905X28872] [PMID: 15811200]
[72]
Rosenblum, S.B.; Huynh, T.; Afonso, A.; Davis, H.R. Jr.; Yumibe, N.; Clader, J.W.; Burnett, D.A. Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypro-pyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption. J. Med. Chem., 1998, 41(6), 973-980.
[http://dx.doi.org/10.1021/jm970701f] [PMID: 9526571]
[73]
Pearson, T.A.; Denke, M.A.; McBride, P.E.; Battisti, W.P.; Brady, W.E.; Palmisano, J. A community-based, randomized trial of ezetimibe added to statin therapy to attain NCEP ATP III goals for LDL cholesterol in hypercholesterolemic patients: the ezetimibe add-on to statin for effectiveness (EASE) trial. Mayo Clin. Proc., 2005, 80(5), 587-595.
[http://dx.doi.org/10.4065/80.5.587] [PMID: 15887425]
[74]
Roeters van Lennep, H.W.; Liem, A.H.; Dunselman, P.H.; Dallinga-Thie, G.M.; Zwinderman, A.H.; Jukema, J.W. The efficacy of statin monotherapy uptitration versus switching to ezetimibe/simvastatin: results of the EASEGO study. Curr. Med. Res. Opin., 2008, 24(3), 685-694.
[http://dx.doi.org/10.1185/030079908X273273] [PMID: 18226326]
[75]
Ballantyne, C.M.; Houri, J.; Notarbartolo, A.; Melani, L.; Lipka, L.J.; Suresh, R.; Sun, S.; LeBeaut, A.P.; Sager, P.T.; Veltri, E.P. Ezetimibe Study Group. Effect of ezetimibe coadministered with atorvastatin in 628 patients with primary hypercholesterolemia: a prospective, randomized, double-blind trial. Circulation, 2003, 107(19), 2409-2415.
[http://dx.doi.org/10.1161/01.CIR.0000068312.21969.C8] [PMID: 12719279]
[76]
Padhy, B.M.; Yadav, R.; Gupta, Y.K. Hypolipidaemic and anti-inflammatory effects of fixed dose combination of atorvastatin plus ezetimibe in Indian patients with dyslipidaemia. Singapore Med. J., 2013, 54(2), 90-95.
[http://dx.doi.org/10.11622/smedj.2013031] [PMID: 23462833]
[77]
Madamanchi, N.R.; Vendrov, A.; Runge, M.S. Oxidative stress and vascular disease. Arterioscler. Thromb. Vasc. Biol., 2005, 25(1), 29-38.
[http://dx.doi.org/10.1161/01.ATV.0000150649.39934.13] [PMID: 15539615]
[78]
Nochioka, K.; Tanaka, S.; Miura, M.; Zhulanqiqige, E.; Fukumoto, Y.; Shiba, N.; Shimokawa, H. Ezetimibe improves endothelial function and inhibits Rho-kinase activity associated with inhibition of cholesterol absorption in humans. Circ. J., 2012, 76(8), 2023-2030.
[http://dx.doi.org/10.1253/circj.CJ-12-0331] [PMID: 22640986]
[79]
Hussein, O.; Minasian, L.; Itzkovich, Y.; Shestatski, K.; Solomon, L.; Zidan, J. Ezetimibe’s effect on platelet aggregation and LDL tendency to peroxidation in hypercholesterolaemia as monotherapy or in addition to simvastatin. Br. J. Clin. Pharmacol., 2008, 65(5), 637-645.
[http://dx.doi.org/10.1111/j.1365-2125.2007.03080.x] [PMID: 18241285]
[80]
Undas, A.; Machnik, A.; Potaczek, D.P.; Wypasek, E.; Zmudka, K.; Tracz, W. Ezetimibe combined with simvastatin compared with simvastatin alone results in a greater suppression of oxidative stress and enhanced fibrinolysis in patients after acute coronary events. J. Cardiovasc. Pharmacol., 2011, 58(2), 167-172.
[http://dx.doi.org/10.1097/FJC.0b013e31821e8cb2] [PMID: 21558878]
[81]
Nakamura, T.; Sato, E.; Fujiwara, N.; Kawagoe, Y.; Ueda, Y.; Suzuki, T.; Ueda, S.; Adachi, H.; Okuda, S.; Yamagishi, S. Ezetimibe decreases serum levels of asymmetric dimethylarginine (ADMA) and ameliorates renal injury in non-diabetic chronic kidney disease patients in a cholesterol-independent manner. Pharmacol. Res., 2009, 60(6), 525-528.
[http://dx.doi.org/10.1016/j.phrs.2009.04.011] [PMID: 19409491]
[82]
Krysiak, R.; Zmuda, W.; Okopien, B. The effect of ezetimibe, administered alone or in combination with simvastatin, on lymphocyte cytokine release in patients with elevated cholesterol levels. J. Intern. Med., 2012, 271(1), 32-42.
[http://dx.doi.org/10.1111/j.1365-2796.2011.02394.x] [PMID: 21623963]
[83]
Chalasani, N.; Aljadhey, H.; Kesterson, J.; Murray, M.D.; Hall, S.D. Patients with elevated liver enzymes are not at higher risk for statin hepatotoxicity. Gastroenterology, 2004, 126(5), 1287-1292.
[http://dx.doi.org/10.1053/j.gastro.2004.02.015] [PMID: 15131789]
[84]
Seidah, N.G.; Benjannet, S.; Wickham, L.; Marcinkiewicz, J.; Jasmin, S.B.; Stifani, S.; Basak, A.; Prat, A.; Chretien, M. The secretory proprotein convertase neural apoptosis-regulated convertase 1 (NARC-1): liver regeneration and neuronal differentiation. Proc. Natl. Acad. Sci. USA, 2003, 100(3), 928-933.
[http://dx.doi.org/10.1073/pnas.0335507100] [PMID: 12552133]
[85]
Latimer, J.; Batty, J.A.; Neely, R.D.; Kunadian, V. PCSK9 inhibitors in the prevention of cardiovascular disease. J. Thromb. Thrombolysis, 2016, 42(3), 405-419.
[http://dx.doi.org/10.1007/s11239-016-1364-1] [PMID: 27095708]
[86]
Burke, A.C.; Dron, J.S.; Hegele, R.A.; Huff, M.W. PCSK9: regulation and target for drug development for dyslipidemia. Annu. Rev. Pharmacol. Toxicol., 2017, 57, 223-244.
[http://dx.doi.org/10.1146/annurev-pharmtox-010716-104944] [PMID: 27575716]
[87]
Bergeron, N.; Phan, B.A.; Ding, Y.; Fong, A.; Krauss, R.M. Proprotein convertase subtilisin/kexin type 9 inhibition: a new therapeutic mechanism for reducing cardiovascular disease risk. Circulation, 2015, 132(17), 1648-1666.
[http://dx.doi.org/10.1161/CIRCULATIONAHA.115. 016080] [PMID: 26503748]
[88]
Durairaj, A.; Sabates, A.; Nieves, J.; Moraes, B.; Baum, S. Proprotein convertase subtilisin/kexin type 9 (PCSK9) and its inhibitors: a review of physiology, biology, and clinical data. Curr. Treat. Options Cardiovasc. Med., 2017, 19(8), 58.
[http://dx.doi.org/10.1007/s11936-017-0556-0] [PMID: 28639183]
[89]
Fisher, T.S.; Lo Surdo, P.; Pandit, S.; Mattu, M.; Santoro, J.C.; Wisniewski, D.; Cummings, R.T.; Calzetta, A.; Cubbon, R.M.; Fischer, P.A.; Tarachandani, A.; De Francesco, R.; Wright, S.D.; Sparrow, C.P.; Carfi, A.; Sitlani, A. Effects of pH and low density lipoprotein (LDL) on PCSK9-dependent LDL receptor regulation. J. Biol. Chem., 2007, 282(28), 20502-20512.
[http://dx.doi.org/10.1074/jbc.M701634200] [PMID: 17493938]
[90]
Dron, J.S.; Hegele, R.A. Complexity of mechanisms among human proprotein convertase subtilisin-kexin type 9 variants. Curr. Opin. Lipidol., 2017, 28(2), 161-169.
[http://dx.doi.org/10.1097/MOL.0000000000000386] [PMID: 28157721]
[91]
Reddy, S.S.; Connor, T.E.; Weeber, E.J.; Rebeck, W. Similarities and differences in structure, expression, and functions of VLDLR and ApoER2. Mol. Neurodegener., 2011, 6, 30.
[http://dx.doi.org/10.1186/1750-1326-6-30] [PMID: 21554715]
[92]
Dias, C.S.; Shaywitz, A.J.; Wasserman, S.M.; Smith, B.P.; Gao, B.; Stolman, D.S.; Crispino, C.P.; Smirnakis, K.V.; Emery, M.G.; Colbert, A.; Gibbs, J.P.; Retter, M.W.; Cooke, B.P.; Uy, S.T.; Matson, M.; Stein, E.A. Effects of AMG 145 on low-density lipoprotein cholesterol levels: results from 2 randomized, double-blind, placebo-controlled, ascending-dose phase 1 studies in healthy volunteers and hypercholesterolemic subjects on statins. J. Am. Coll. Cardiol., 2012, 60(19), 1888-1898.
[http://dx.doi.org/10.1016/j.jacc.2012.08.986] [PMID: 23083772]
[93]
Sullivan, D.; Olsson, A.G.; Scott, R.; Kim, J.B.; Xue, A.; Gebski, V.; Wasserman, S.M.; Stein, E.A. Effect of a monoclonal antibody to PCSK9 on low-density lipoprotein cholesterol levels in statin-intolerant patients: the GAUSS randomized trial. JAMA, 2012, 308(23), 2497-2506.
[http://dx.doi.org/10.1001/jama.2012.25790] [PMID: 23128163]
[94]
El Khoury, P.; Elbitar, S.; Ghaleb, Y.; Khalil, Y.A.; Varret, M.; Boileau, C.; Abifadel, M. PCSK9 mutations in familial hypercholesterolemia: from a groundbreaking discovery to Anti-PCSK9 therapies. Curr. Atheroscler. Rep., 2017, 19(12), 49.
[http://dx.doi.org/10.1007/s11883-017-0684-8] [PMID: 29038906]
[95]
Giugliano, R.P.; Desai, N.R.; Kohli, P.; Rogers, W.J.; Somaratne, R.; Huang, F.; Liu, T.; Mohanavelu, S.; Hoffman, E.B.; McDonald, S.T.; Abrahamsen, T.E.; Wasserman, S.M.; Scott, R.; Sabatine, M.S. LAPLACE-TIMI 57 Investigators. Efficacy, safety, and tolerability of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 in combination with a statin in patients with hypercholesterolaemia (LAPLACE-TIMI 57): a randomised, placebo-controlled, dose-ranging, phase 2 study. Lancet, 2012, 380(9858), 2007-2017.
[http://dx.doi.org/10.1016/S0140-6736(12)61770-X] [PMID: 23141813]
[96]
Koren, M.J.; Scott, R.; Kim, J.B.; Knusel, B.; Liu, T.; Lei, L.; Bolognese, M.; Wasserman, S.M. Efficacy, safety, and tolerability of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 as monotherapy in patients with hypercholesterolaemia (MENDEL): a randomised, double-blind, placebo-controlled, phase 2 study. Lancet, 2012, 380(9858), 1995-2006.
[http://dx.doi.org/10.1016/S0140-6736(12)61771-1] [PMID: 23141812]
[97]
Raal, F.; Scott, R.; Somaratne, R.; Bridges, I.; Li, G.; Wasserman, S.M.; Stein, E.A. Low-density lipoprotein cholesterol-lowering effects of AMG 145, a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 serine protease in patients with heterozygous familial hypercholesterolemia: the Reduction of LDL-C with PCSK9 inhibition in heterozygous familial hypercholesterolemia disorder (RUTHERFORD) randomized trial. Circulation, 2012, 126(20), 2408-2417.
[http://dx.doi.org/10.1161/CIRCULATIONAHA.112.144055] [PMID: 23129602]
[98]
He, X-X.; Zhang, R.; Zuo, P-Y.; Liu, Y-W.; Zha, X-N.; Shan, S-S.; Liu, C-Y. The efficacy advantage of evolocumab (AMG 145) dosed at 140mg every 2weeks versus 420mg every 4weeks in patients with hypercholesterolemia: Evidence from a meta-analysis. Eur. J. Intern. Med., 2017, 38, 52-60.
[http://dx.doi.org/10.1016/j.ejim.2016.10.009] [PMID: 28341307]
[99]
Sabatine, M.S.; Giugliano, R.P.; Keech, A.C.; Honarpour, N.; Wiviott, S.D.; Murphy, S.A.; Kuder, J.F.; Wang, H.; Liu, T.; Wasserman, S.M.; Sever, P.S.; Pedersen, T.R.; Committee, F.S. FOURIER steering committee and investigators. evolocumab and clinical outcomes in patients with cardiovascular disease. N. Engl. J. Med., 2017, 376(18), 1713-1722.
[http://dx.doi.org/10.1056/NEJMoa1615664] [PMID: 28304224]
[100]
Bellera, N.; Barba, I.; Rodriguez-Sinovas, A.; Ferret, E.; Asín, M.A.; Gonzalez-Alujas, M.T.; Pérez-Rodon, J.; Esteves, M.; Fonseca, C.; Toran, N.; Garcia Del Blanco, B.; Pérez, A.; García-Dorado, D. Single intracoronary injection of encapsulated antagomir-92a promotes angiogenesis and prevents adverse infarct remodeling. J. Am. Heart Assoc., 2014, 3(5)e000946
[http://dx.doi.org/10.1161/JAHA.114.000946] [PMID: 25240056]
[101]
Carè, A.; Catalucci, D.; Felicetti, F.; Bonci, D.; Addario, A.; Gallo, P.; Bang, M.L.; Segnalini, P.; Gu, Y.; Dalton, N.D.; Elia, L.; Latronico, M.V.; Høydal, M.; Autore, C.; Russo, M.A.; Dorn, G.W., II; Ellingsen, O.; Ruiz-Lozano, P.; Peterson, K.L.; Croce, C.M.; Peschle, C.; Condorelli, G. MicroRNA-133 controls cardiac hypertrophy. Nat. Med., 2007, 13(5), 613-618.
[http://dx.doi.org/10.1038/nm1582] [PMID: 17468766]
[102]
Raal, F.J.; Stein, E.A.; Dufour, R.; Turner, T.; Civeira, F.; Burgess, L.; Langslet, G.; Scott, R.; Olsson, A.G.; Sullivan, D.; Hovingh, G.K.; Cariou, B.; Gouni-Berthold, I.; Somaratne, R.; Bridges, I.; Scott, R.; Wasserman, S.M.; Gaudet, D.; Investigators, R. RUTHERFORD-2 Investigators. PCSK9 inhibition with evolocumab (AMG 145) in heterozygous familial hypercholesterolaemia (RUTHERFORD-2): a randomised, double-blind, placebo-controlled trial. Lancet, 2015, 385(9965), 331-340.
[http://dx.doi.org/10.1016/S0140-6736(14)61399-4] [PMID: 25282519]
[103]
Robinson, J.G.; Nedergaard, B.S.; Rogers, W.J.; Fialkow, J.; Neutel, J.M.; Ramstad, D.; Somaratne, R.; Legg, J.C.; Nelson, P.; Scott, R.; Wasserman, S.M.; Weiss, R.; Investigators, L. LAPLACE-2 Investigators. Effect of evolocumab or ezetimibe added to moderate- or high-intensity statin therapy on LDL-C lowering in patients with hypercholesterolemia: the LAPLACE-2 randomized clinical trial. JAMA, 2014, 311(18), 1870-1882.
[http://dx.doi.org/10.1001/jama.2014.4030] [PMID: 24825642]
[104]
Hadjiphilippou, S.; Ray, K.K. Evolocumab and clinical outcomes in patients with cardiovascular disease. J. R. Coll. Physicians Edinb., 2017, 47(2), 153-155.
[http://dx.doi.org/10.4997/JRCPE.2017.212] [PMID: 28675189]
[105]
Nissen, S.E.; Nicholls, S.J. Results of the GLAGOV trial. Cleve. Clin. J. Med., 2017, 84(12)(Suppl. 4), e1-e5.
[http://dx.doi.org/10.3949/ccjm.84.s4.01] [PMID: 29281604]
[106]
Chapman, M.J.; Ginsberg, H.N. Evolocumab treatment of hypercholesterolemia in OSLER-1: enduring efficacy, tolerability, and safety over 5 years. J. Am. Coll. Cardiol., 2019, 74(17), 2147-2149.
[http://dx.doi.org/10.1016/j.jacc.2019.07.087] [PMID: 31648706]
[107]
Raal, F.J.; Honarpour, N.; Blom, D.J.; Hovingh, G.K.; Xu, F.; Scott, R.; Wasserman, S.M.; Stein, E.A.; Investigators, T. TESLA Investigators. Inhibition of PCSK9 with evolocumab in homozygous familial hypercholesterolaemia (TESLA Part B): a randomised, double-blind, placebo-controlled trial. Lancet, 2015, 385(9965), 341-350.
[http://dx.doi.org/10.1016/S0140-6736(14)61374-X] [PMID: 25282520]
[108]
Plosker, G.L.; Wagstaff, A.J. Fluvastatin: a review of its pharmacology and use in the management of hypercholesterolaemia. Drugs, 1996, 51(3), 433-459.
[http://dx.doi.org/10.2165/00003495-199651030-00011] [PMID: 8882381]

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