Parham Johnathon Seth, Goldberg Anne Carol
Division of Endocrinology, Metabolism and Lipid Research, Washington University School of Medicine, 660 South Euclid, Campus Box 8127, St. Louis, MO, 63110, USA.
Curr Atheroscler Rep. 2022 Aug;24(8):619-625. doi: 10.1007/s11883-022-01036-4. Epub 2022 Jun 6.
There have been recent developments of novel therapeutic agents for lipid lowering. This article reviews treatment concepts for two of the newest lipid-lowering medications.
Bempedoic acid inhibits adenosine citrate lyase, decreasing intracellular lipogenesis. This oral medication is a prodrug and requires activation by enzymes present in hepatocytes but absent in the skeletal muscle. Clinical trials demonstrated additive benefit with statin therapy, and it was well tolerated in statin-intolerant populations. Inclisiran uses RNA interference to prevent translation of PCSK9 mRNA. Due to its stability, it can be given as an injection every 6 months and produces consistent, durable, and potent cholesterol lowering. Bempedoic acid and inclisiran represent new avenues of treatment for the prevention and treatment of cardiovascular disease. This will allow for more comprehensive care by addressing challenges with medication adherence, such as adverse effects to prior medications as well as ease of dosing.
近年来出现了新型降脂治疗药物。本文综述了两种最新降脂药物的治疗理念。
贝派地酸抑制柠檬酸腺苷裂解酶,减少细胞内脂肪生成。这种口服药物是一种前体药物,需要肝细胞中存在但骨骼肌中不存在的酶来激活。临床试验表明,与他汀类药物联合使用有额外益处,且在他汀类药物不耐受人群中耐受性良好。英克西兰利用RNA干扰来阻止PCSK9 mRNA的翻译。由于其稳定性,每6个月注射一次即可,能持续、持久且有效地降低胆固醇。贝派地酸和英克西兰为心血管疾病的预防和治疗提供了新的治疗途径。这将通过应对药物依从性方面的挑战,如对先前药物的不良反应以及给药便利性,实现更全面的治疗。