siRNA drug Leqvio (inclisiran) to lower cholesterol.
作者信息
Migliorati Julia M, Jin Jing, Zhong Xiao-Bo
机构信息
Department of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut, Storrs, CT 06269, USA.
Department of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut, Storrs, CT 06269, USA.
出版信息
Trends Pharmacol Sci. 2022 May;43(5):455-456. doi: 10.1016/j.tips.2022.02.003. Epub 2022 Mar 17.
Abstract
摘要
相似文献
1
siRNA drug Leqvio (inclisiran) to lower cholesterol.小干扰RNA药物Leqvio（英克西兰钠）可降低胆固醇。
Trends Pharmacol Sci. 2022 May;43(5):455-456. doi: 10.1016/j.tips.2022.02.003. Epub 2022 Mar 17.
2
Inclisiran (Leqvio) for LDL-cholesterol lowering.英克西兰（Leqvio）用于降低低密度脂蛋白胆固醇。
Med Lett Drugs Ther. 2022 Mar 21;64(1646):43-45.
3
Inclisiran: First Approval.依洛尤单抗：首次获批
Drugs. 2021 Feb;81(3):389-395. doi: 10.1007/s40265-021-01473-6.
4
5
Low-density Lipoprotein-Cholesterol Lowering Strategies for Prevention of Atherosclerotic Cardiovascular Disease: Focus on siRNA Treatment Targeting PCSK9 (Inclisiran).用于预防动脉粥样硬化性心血管疾病的低密度脂蛋白胆固醇降低策略：聚焦靶向 PCSK9（inclisiran）的 siRNA 治疗。
Curr Cardiol Rep. 2020 Oct 21;22(12):176. doi: 10.1007/s11886-020-01427-6.
6
Effect of an siRNA Therapeutic Targeting PCSK9 on Atherogenic Lipoproteins: Prespecified Secondary End Points in ORION 1.靶向 PCSK9 的 siRNA 治疗对动脉粥样硬化脂蛋白的影响：ORION 1 的预先指定次要终点。
Circulation. 2018 Sep 25;138(13):1304-1316. doi: 10.1161/CIRCULATIONAHA.118.034710.
7
Effect of inclisiran, the small-interfering RNA against proprotein convertase subtilisin/kexin type 9, on platelets, immune cells, and immunological biomarkers: a pre-specified analysis from ORION-1.针对前蛋白转化酶枯草杆菌蛋白酶/ kexin 9型的小干扰RNA英克西兰对血小板、免疫细胞和免疫生物标志物的影响：来自ORION-1的预先指定分析。
Cardiovasc Res. 2021 Jan 1;117(1):284-291. doi: 10.1093/cvr/cvaa077.
8
Small interfering ribonucleic acid for cholesterol lowering - Inclisiran: Inclisiran for cholesterol lowering.用于降胆固醇的小干扰核糖核酸 - 依洛西仑：用于降胆固醇的依洛西仑。
J Clin Lipidol. 2022 Sep-Oct;16(5):574-582. doi: 10.1016/j.jacl.2022.06.009. Epub 2022 Jun 28.
9
Inclisiran in Patients at High Cardiovascular Risk with Elevated LDL Cholesterol.依洛尤单抗在 LDL 胆固醇升高的高心血管风险患者中的应用。
N Engl J Med. 2017 Apr 13;376(15):1430-1440. doi: 10.1056/NEJMoa1615758. Epub 2017 Mar 17.
10
Inclisiran inhibits oxidized low-density lipoprotein-induced foam cell formation in Raw264.7 macrophages via activating the PPARγ pathway.依洛昔兰通过激活 PPARγ 通路抑制氧化型低密度脂蛋白诱导的 Raw264.7 巨噬细胞泡沫细胞形成。
Autoimmunity. 2022 Jun;55(4):223-232. doi: 10.1080/08916934.2022.2051142. Epub 2022 Mar 15.
引用本文的文献
1
Intracellular fatty acid levels differentially impact target silencing by FDA-approved siRNA drugs.细胞内脂肪酸水平对FDA批准的小干扰RNA（siRNA）药物的靶点沉默有不同影响。
Biochem Pharmacol. 2025 Jul 27;242(Pt 2):117192. doi: 10.1016/j.bcp.2025.117192.
2
Biological and Biosimilar Medicines in Contemporary Pharmacotherapy for Metabolic Syndrome.当代代谢综合征药物治疗中的生物药和生物类似药
Pharmaceutics. 2025 Jun 11;17(6):768. doi: 10.3390/pharmaceutics17060768.
3
The Fomivirsen, Patisiran, and Givosiran Odyssey: How the Success Stories May Pave the Way for Future Clinical Translation of Nucleic Acid Drugs.福米韦生、帕替拉韦和吉沃赛生的历程：成功案例如何为核酸药物未来的临床转化铺平道路。
BioDrugs. 2025 May;39(3):359-371. doi: 10.1007/s40259-025-00711-7. Epub 2025 Apr 5.
4
Chemical Process Development in the Pharmaceutical Industry in Europe-Insights and Perspectives from Industry Scientists.欧洲制药行业的化学工艺开发——来自行业科学家的见解与观点
Angew Chem Int Ed Engl. 2025 May;64(19):e202420719. doi: 10.1002/anie.202420719. Epub 2025 Mar 27.
5
Nucleic Acid Conjugates: Unlocking Therapeutic Potential.核酸缀合物：释放治疗潜力。
ACS Bio Med Chem Au. 2024 Dec 18;5(1):3-15. doi: 10.1021/acsbiomedchemau.4c00092. eCollection 2025 Feb 19.
6
Delivery Strategies of siRNA Therapeutics for Hair Loss Therapy.用于脱发治疗的 siRNA 治疗药物的递药策略。
Int J Mol Sci. 2024 Jul 11;25(14):7612. doi: 10.3390/ijms25147612.
7
pH-Responsive polymer boosts cytosolic siRNA release for retinal neovascularization therapy.pH响应性聚合物促进细胞溶质小干扰RNA释放用于视网膜新生血管治疗。
Acta Pharm Sin B. 2024 Feb;14(2):781-794. doi: 10.1016/j.apsb.2023.09.001. Epub 2023 Sep 9.
8
Targeting the Liver with Nucleic Acid Therapeutics for the Treatment of Systemic Diseases of Liver Origin.针对肝脏的核酸治疗药物用于治疗肝脏起源的系统性疾病。
Pharmacol Rev. 2023 Dec 15;76(1):49-89. doi: 10.1124/pharmrev.123.000815.
9
Chemistry, structure and function of approved oligonucleotide therapeutics.已获批的寡核苷酸治疗药物的化学、结构和功能。
Nucleic Acids Res. 2023 Apr 11;51(6):2529-2573. doi: 10.1093/nar/gkad067.
10
RNAi in cell nuclei: potential for a new layer of biological regulation and a new strategy for therapeutic discovery.RNAi 在细胞核内：潜在的新生物学调控层和治疗发现的新策略。
RNA. 2023 Apr;29(4):415-422. doi: 10.1261/rna.079500.122. Epub 2023 Jan 19.
本文引用的文献
1
The growth of siRNA-based therapeutics: Updated clinical studies.基于 siRNA 的治疗药物的发展：更新的临床研究。
Biochem Pharmacol. 2021 Jul;189:114432. doi: 10.1016/j.bcp.2021.114432. Epub 2021 Jan 26.
2
Inclisiran Durably Lowers Low-Density Lipoprotein Cholesterol and Proprotein Convertase Subtilisin/Kexin Type 9 Expression in Homozygous Familial Hypercholesterolemia: The ORION-2 Pilot Study.inclisiran持久降低纯合子家族性高胆固醇血症患者的低密度脂蛋白胆固醇及前蛋白转化酶枯草溶菌素/kexin 9型表达：ORION-2初步研究
Circulation. 2020 Jun 2;141(22):1829-1831. doi: 10.1161/CIRCULATIONAHA.119.044431. Epub 2020 Jun 1.
3
Inclisiran for the Treatment of Heterozygous Familial Hypercholesterolemia.英克西兰用于治疗杂合子家族性高胆固醇血症。
N Engl J Med. 2020 Apr 16;382(16):1520-1530. doi: 10.1056/NEJMoa1913805. Epub 2020 Mar 18.
4
Two Phase 3 Trials of Inclisiran in Patients with Elevated LDL Cholesterol.两项降低 LDL 胆固醇的依洛尤单抗 3 期临床试验。
N Engl J Med. 2020 Apr 16;382(16):1507-1519. doi: 10.1056/NEJMoa1912387. Epub 2020 Mar 18.
5
Inclisiran-New hope in the management of lipid disorders?依洛尤单抗——血脂异常管理的新希望？
J Clin Lipidol. 2020 Jan-Feb;14(1):16-27. doi: 10.1016/j.jacl.2019.11.001. Epub 2019 Nov 12.
6
Inclisiran: A New Promising Agent in the Management of Hypercholesterolemia.英克西兰：高胆固醇血症管理中的一种新的有前景的药物。
Diseases. 2018 Jul 13;6(3):63. doi: 10.3390/diseases6030063.
7
Inclisiran in Patients at High Cardiovascular Risk with Elevated LDL Cholesterol.依洛尤单抗在 LDL 胆固醇升高的高心血管风险患者中的应用。
N Engl J Med. 2017 Apr 13;376(15):1430-1440. doi: 10.1056/NEJMoa1615758. Epub 2017 Mar 17.
8
A Highly Durable RNAi Therapeutic Inhibitor of PCSK9.一种高度耐用的PCSK9的RNAi治疗抑制剂。
N Engl J Med. 2017 Jan 5;376(1):41-51. doi: 10.1056/NEJMoa1609243. Epub 2016 Nov 13.
Zotero 插件