{"title":"inclisiran的疗效、获益和安全性。","authors":"José López-Miranda","doi":"10.1016/j.arteri.2024.07.003","DOIUrl":null,"url":null,"abstract":"<div><div>Hypercholesterolemia is a causal factor of atherosclerotic cardiovascular disease (ASCVD), which is one of the main causes of morbidity and mortality in Spain. The reduction of LDL cholesterol (LDL-C) decreases the risk of ASCVD and adverse cardiovascular events. Targeted therapy for the proprotein convertase subtilisin/kexin type 9 (PCSK-9) has emerged as a novel tool for the treatment of hyperlipidemia. Inclisiran is a small double-stranded small interfering RNA that acts by blocking PCSK-9 transcription in hepatocytes, leading to a marked and sustained reduction in circulating LDL-C levels. In contrast to other lipid-lowering therapies such as statins, ezetimibe and monoclonal antibodies PCSK-9 inhibitors, Inclisiran proposes an infrequent dosing regimen of twice times a year. Its prolonged effect represents an advantage over non-compliance of the treatment, which is one of the main reasons why LDL-C goals are not achieved with standard therapy. This review aims to present and discuss current scientific data regarding the efficacy, tolerability and safety of Inclisiran in the treatment of hypercholesterolemia. Inclisiran has been shown to provide significant long-term reductions in LDL-C levels associated with notable decreases in levels of PCSK9 and other atherogenic lipoproteins with a highly favourable side effect profile similar to placebo. The convenience of a twice-yearly dosing regimen promotes adherence to therapy and facilitates achievement of LDL-C goals. Results from ongoing trials designed to determine its effect on cardiovascular events are expected to provide further information about the cardiovascular benefit of inclisiran in patients with ACVD and in patients at high cardiovascular risk.</div></div>","PeriodicalId":45230,"journal":{"name":"Clinica e Investigacion en Arteriosclerosis","volume":"36 ","pages":"Pages S24-S30"},"PeriodicalIF":1.9000,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Eficacia, beneficio y seguridad de inclisiran\",\"authors\":\"José López-Miranda\",\"doi\":\"10.1016/j.arteri.2024.07.003\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Hypercholesterolemia is a causal factor of atherosclerotic cardiovascular disease (ASCVD), which is one of the main causes of morbidity and mortality in Spain. The reduction of LDL cholesterol (LDL-C) decreases the risk of ASCVD and adverse cardiovascular events. Targeted therapy for the proprotein convertase subtilisin/kexin type 9 (PCSK-9) has emerged as a novel tool for the treatment of hyperlipidemia. Inclisiran is a small double-stranded small interfering RNA that acts by blocking PCSK-9 transcription in hepatocytes, leading to a marked and sustained reduction in circulating LDL-C levels. In contrast to other lipid-lowering therapies such as statins, ezetimibe and monoclonal antibodies PCSK-9 inhibitors, Inclisiran proposes an infrequent dosing regimen of twice times a year. Its prolonged effect represents an advantage over non-compliance of the treatment, which is one of the main reasons why LDL-C goals are not achieved with standard therapy. This review aims to present and discuss current scientific data regarding the efficacy, tolerability and safety of Inclisiran in the treatment of hypercholesterolemia. Inclisiran has been shown to provide significant long-term reductions in LDL-C levels associated with notable decreases in levels of PCSK9 and other atherogenic lipoproteins with a highly favourable side effect profile similar to placebo. The convenience of a twice-yearly dosing regimen promotes adherence to therapy and facilitates achievement of LDL-C goals. Results from ongoing trials designed to determine its effect on cardiovascular events are expected to provide further information about the cardiovascular benefit of inclisiran in patients with ACVD and in patients at high cardiovascular risk.</div></div>\",\"PeriodicalId\":45230,\"journal\":{\"name\":\"Clinica e Investigacion en Arteriosclerosis\",\"volume\":\"36 \",\"pages\":\"Pages S24-S30\"},\"PeriodicalIF\":1.9000,\"publicationDate\":\"2024-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Clinica e Investigacion en Arteriosclerosis\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0214916824000767\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"PERIPHERAL VASCULAR DISEASE\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Clinica e Investigacion en Arteriosclerosis","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0214916824000767","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PERIPHERAL VASCULAR DISEASE","Score":null,"Total":0}
Hypercholesterolemia is a causal factor of atherosclerotic cardiovascular disease (ASCVD), which is one of the main causes of morbidity and mortality in Spain. The reduction of LDL cholesterol (LDL-C) decreases the risk of ASCVD and adverse cardiovascular events. Targeted therapy for the proprotein convertase subtilisin/kexin type 9 (PCSK-9) has emerged as a novel tool for the treatment of hyperlipidemia. Inclisiran is a small double-stranded small interfering RNA that acts by blocking PCSK-9 transcription in hepatocytes, leading to a marked and sustained reduction in circulating LDL-C levels. In contrast to other lipid-lowering therapies such as statins, ezetimibe and monoclonal antibodies PCSK-9 inhibitors, Inclisiran proposes an infrequent dosing regimen of twice times a year. Its prolonged effect represents an advantage over non-compliance of the treatment, which is one of the main reasons why LDL-C goals are not achieved with standard therapy. This review aims to present and discuss current scientific data regarding the efficacy, tolerability and safety of Inclisiran in the treatment of hypercholesterolemia. Inclisiran has been shown to provide significant long-term reductions in LDL-C levels associated with notable decreases in levels of PCSK9 and other atherogenic lipoproteins with a highly favourable side effect profile similar to placebo. The convenience of a twice-yearly dosing regimen promotes adherence to therapy and facilitates achievement of LDL-C goals. Results from ongoing trials designed to determine its effect on cardiovascular events are expected to provide further information about the cardiovascular benefit of inclisiran in patients with ACVD and in patients at high cardiovascular risk.
期刊介绍:
La publicación idónea para acceder tanto a los últimos originales de investigación como a formación médica continuada sobre la arteriosclerosis y su etiología, epidemiología, fisiopatología, diagnóstico y tratamiento. Además, es la publicación oficial de la Sociedad Española de Arteriosclerosis.