Pro protein convertase subtilisin kexin type 9 (PCSK9) inhibitors Pharmacological review and update

被引:0
|
作者
Corral, Pablo [1 ,2 ]
Suter, Agustina [3 ]
Rusconi, Alejandro [3 ]
Trigo, Leandro [3 ]
机构
[1] Univ Fraternidad Agrupaciones Santo Tomas Aquino, Med Interna, Buenos Aires, DF, Argentina
[2] Univ Fraternidad Agrupaciones Santo Tomas Aquino, Fac Med, Farmacol, Buenos Aires, DF, Argentina
[3] Univ FASTA, Fac Med, Med, Buenos Aires, DF, Argentina
关键词
Pro protein convertase subtilisin kexin type 9; PCSK9; inhibitors; Familial hypercholesterolemia; LDL cholesterol;
D O I
暂无
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Atherosclerotic cardiovascular disease is the leading cause of morbidity and mortality worldwide. The direct relationship between cholesterol levels lipoprotein low density and atherosclerosis has led to optimize efforts to regulate and control this lipoprotein sub-fraction. The discovery of the pro protein convertase subtilisin kexin type 9 (PCSK9) as regulator receptor low-density lipoprotein in liver and therefore circulating levels of cholesterol bound to low density lipoprotein, triggered an unusual effort to reduce its plasma concentration. Inhibition of PCSK9 through monoclonal antibodies, it has proved to be a pharmacologic strategy with a broad safety profile and high efficacy in the phase 3 trials. This has led to approval by several regulatory entities in certain specific groups, such as patients with familial hypercholesterolemia and patients in secondary prevention who not reaching goals with the pharmacological tools available. Pending results of clinical events, the aim of this article is to review the pharmacological aspects of the inhibitors of PCSK9.
引用
收藏
页码:122 / 129
页数:8
相关论文
共 50 条
  • [41] Efficacy and Safety of Alirocumab and Evolocumab as Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors in Familial Hypercholesterolemia: A Systematic Review and Meta-Analysis
    Ghasempour, Ghasem
    Zamani-Garmsiri, Fahimeh
    Shaikhnia, Farhad
    Soleimani, Ali Akbar
    Fard, Syed Reza Hosseini
    Leila, Janani
    Teimuri, Shohreh
    Parvaz, Najmeh
    Mohammadi, Payam
    Najafi, Mohammad
    CURRENT MEDICINAL CHEMISTRY, 2024, 31 (02) : 223 - 241
  • [42] Early administration of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors in patients with acute coronary syndrome: a systematic review and meta-analysis
    Hosseini, Kaveh
    Soleimani, Hamidreza
    Maleki, Saba
    Nasrollahizadeh, Amir
    Tayebi, Sima
    Nelson, John
    Heffron, Sean P.
    BMC CARDIOVASCULAR DISORDERS, 2024, 24 (01):
  • [43] Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Single Domain Antibodies Are Potent Inhibitors of Low Density Lipoprotein Receptor Degradation
    Weider, Elodie
    Susan-Resiga, Delia
    Essalmani, Rachid
    Hamelin, Josee
    Asselin, Marie-Claude
    Nimesh, Surendra
    Ashraf, Yahya
    Wycoff, Keith L.
    Zhang, Jianbing
    Prat, Annik
    Seidah, Nabil G.
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2016, 291 (32) : 16659 - 16671
  • [44] Update on proprotein convertase subtilisin/kexin type 9 inhibitors, lipoprotein(a) and cardiovascular risk
    Martinez, Laurent O.
    Perret, Bertrand
    Genoux, Annelise
    CURRENT OPINION IN LIPIDOLOGY, 2021, 32 (05) : 324 - 327
  • [45] Proprotein Convertase Subtilisin-Kexin type-9 (PCSK9) and triglyceride-rich lipoprotein metabolism: Facts and gaps
    Baragetti, Andrea
    Grejtakova, Daniela
    Casula, Manuela
    Olmastroni, Elena
    Jotti, Gloria Saccani
    Norata, Giuseppe Danilo
    Catapano, Alberico L.
    Bellosta, Stefano
    PHARMACOLOGICAL RESEARCH, 2018, 130 : 1 - 11
  • [46] Mutations and Polymorphisms in the Proprotein Convertase Subtilisin Kexin 9 (PCSK9) Gene in Cholesterol Metabolism and Disease
    Abifadel, Marianne
    Rabes, Jean-Pierre
    Devillers, Martine
    Munnich, Arnold
    Erlich, Daniele
    Junien, Claudine
    Varret, Mathilde
    Boileau, Catherine
    HUMAN MUTATION, 2009, 30 (04) : 520 - 529
  • [47] Lipoprotein(a) and inhibitors of proprotein convertase subtilisin/kexin type 9
    Kotani, Kazuhiko
    Banach, Maciej
    JOURNAL OF THORACIC DISEASE, 2017, 9 (01) : E78 - E82
  • [48] Proprotein Convertase subtilisin Kexin 9 Inhibitors
    Pirillo, Angela
    Catapano, Alberico Luigi
    CARDIOLOGY CLINICS, 2018, 36 (02) : 241 - +
  • [49] Effects of a Proprotein Convertase Subtilisin/kexin Type 9 (PCSK9) Inhibitor, Alirocumab, on Lipid and Lipoprotein Metabolism in Healthy Subjects
    Reyes-Soffer, Gissette
    Pavlyha, Marianna
    Ngai, Colleen
    Thomas, Tiffany
    Holleran, Stephen
    Ramakrishnan, Sekhar
    Karmally, Wahida
    Donovan, Daniel
    Cowan, Lisa
    Sasiela, William
    Surks, Howard
    Rey, Jacques
    Poitiers, Frank
    Ginsberg, Henry
    CIRCULATION, 2015, 132
  • [50] The efficacy and safety of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors combined with statins in patients with hypercholesterolemia: a network meta-analysis
    Liu, Dong
    Zhang, Jin
    Zhang, Xiaoyu
    Jiang, Fengli
    Wu, Yiping
    Yang, Beibei
    Li, Xinghuan
    Fan, Xiongxiong
    Li, Han
    Sun, Yu
    Gou, Ruijie
    Wang, Xinyu
    FRONTIERS IN CARDIOVASCULAR MEDICINE, 2024, 11