New players in the treatment of hypercholesterolaemia: focus on bempedoic acid and inclisiran

Ruscica, Massimiliano; Sirtori, Cesare R.; Ferri, Nicola; Corsini, Alberto

doi:10.1093/eurheartj/suab090

Cited by 6 publications

(8 citation statements)

References 17 publications

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“…None of the patients in our study were prescribed PCSK9 inhibitors, since PCSK9 inhibitors just came into Chinese market then and were not covered by medical insurance. Additionally, two new drugs, bempedoic acid and inclisiran, have recently been approved and provided potential choices for the lowering of LDL-C levels (28). Cost has been a hurdle for use of new therapies, and recent price reductions may trigger increased use.…”

Section: Discussionmentioning

confidence: 99%

Achievement of low-density lipoprotein cholesterol targets in Chinese patients with atherosclerotic cardiovascular disease after receiving statins and ezetimibe

Cheng

Dong

Shen

et al. 2022

Front. Cardiovasc. Med.

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BackgroundThe importance of low-density lipoprotein cholesterol (LDL-C) lowering to reduce atherosclerotic cardiovascular disease (ASCVD) risk is strongly emphasized. If the LDL-C goals are not achieved with statin therapy, combination with ezetimibe is recommended. Studies revealed a substantial gap between obtained LDL-C levels and LDL-C target in ASCVD patients. However, little is known about the achievement of LDL-lowering treatment targets in ASCVD patients receiving ezetimibe in addition to statins.Materials and methodsThis was a retrospective cohort study based on EHR data from the regional health information system of Yinzhou, an eastern coastal area of China. ASCVD Patients stratified as very high risk, taking both statin and ezetimibe for lipid control, and had at least one lipid test after ezetimibe initiation were included between January 2013 and July 2020. Descriptive statistics were used to summarize the LDL-C values and target value (1.8 mmol/L according to the Chinese guideline, 1.4 mmol/L according to the European guideline) achievements. Multivariable logistic regression was used to explore the influencing factors of target achievement rate.ResultsA total of 1,727 patients were included. The median follow-up time was 15.0 months. Taking 1.8 mmol/L as the target value, the achievement rates of LDL-C over the first 3 follow up years were 50.6, 31.3, and 30.3%, respectively. Taking 1.4 mmol/L as the target value, the achievement rates were 25.6, 15.5, and 16.5%, respectively. Multivariable analysis suggested that male patients (OR = 1.78, 95%CI: 1.27–2.49), combined use of atorvastatin or rosuvastatin with ezetimibe (vs other statins, OR = 4.64, 95% CI: 1.83–11.76), better medication adherence (OR = 1.03, 95% CI: 1.01–1.04) and smoking cessation (vs smoking, OR = 2.26, 95% CI: 1.27–4.02) were associated with a higher achievement rate, while baseline LDL-C level (OR = 0.48, 95% CI: 0.41–0.56) and treatment course of statin before ezetimibe (OR = 0.93, 95% CI: 0.89–0.98) were negatively associated with achievement rate.ConclusionLong-term follow-up data based on a Chinese regional database shows that in very high-risk ASCVD patients taking ezetimibe in addition to statins, achievement rate of LDL-lowering treatment targets is still low and far from satisfactory in real-world setting. More efforts are needed to achieve optimal LDL-C levels.

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Section: Discussionmentioning

confidence: 99%

Achievement of low-density lipoprotein cholesterol targets in Chinese patients with atherosclerotic cardiovascular disease after receiving statins and ezetimibe

Cheng

Dong

Shen

et al. 2022

Front. Cardiovasc. Med.

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“…Bempedoic acid may raise serum uric acid levels due to inhibition of renal tubular OAT2 OAT2/OAT3 organic anion transporter-2/3, OATP1B1/3 organic anion-transporting polypeptide 1B1/3, UGT2B7 UDP glucuronosyltransferase family 2 member B7. (adapted with permission of Oxford University [ 27 ].) …”

Section: Why a New Oral Non-statin Cholesterol-lowering Drug?mentioning

confidence: 99%

Bempedoic Acid: for Whom and When

Ruscica

Sirtori

Carugo

et al. 2022

Curr Atheroscler Rep

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Purpose of Review The aim of creating an orally active non-statin cholesterol-lowering drug was achieved with bempedoic acid, a small linear molecule providing both a significant low-density lipoprotein cholesterol (LDL-C) reduction and an anti-inflammatory effect by decreasing high-sensitivity C-reactive protein. Bempedoic acid antagonizes ATP citrate-lyase, a cytosolic enzyme upstream of HMGCoA reductase which is the rate-limiting step of cholesterol biosynthesis. Bempedoic acid is a pro-drug converted to its active metabolite by very-long-chain acyl-CoA synthetase 1 which is present mostly in the liver and absent in skeletal muscles. This limits the risk of myalgia and myopathy. The remit of this review is to give clinical insights on the safety and efficacy of bempedoic acid and to understand for whom it should be prescribed. Recent Findings Bempedoic acid with a single daily dose (180 mg) reduces LDL-C by a mean 24.5% when given alone, by 18% when given on top of a major statin and by 38–40% when given in a fixed-dose combination with ezetimibe. Bempedoic acid does not lead to the risk of new-onset diabetes, and moderately improves the glycaemic profile. Summary The extensive knowledge on bempedoic acid mechanism, metabolism and side effects has led to an improved understanding of the potential benefits of this agent and offers a possible alternative to cardiologists and clinical practitioners somewhat worn out today by the occurrence of the muscular side effects of statins.

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“…Bempedoic acid is a prodrug that gets activated to bempedoyl-CoA by liver long-chain acyl-CoA-synthetase I (ACSVL I) [6]. Bempedoyl-CoA inhibits ACL (Fig.…”

Section: Bempedoic Acidmentioning

confidence: 99%

Effects of bempedoic acid on markers of inflammation and Lp(a)

Reddy,

Deoker

2024

Current Opinion in Cardiology

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Purpose of review To study the effect of bempedoic acid on markers of inflammation and lipoprotein (a) to help determine if the drug would be useful to treat patients with elevated cardiovascular risks and residual cardiovascular risk despite optimal low-density lipoprotein cholesterol (LDL-C) levels. Recent findings Bempedoic acid is found to cause significant reduction in LDL-C and high-sensitivity C-reactive protein (hs-CRP) in various randomized clinical trials. Multiple meta-analyses have also found that bempedoic acid therapy leads to reduction in non–high-density lipoprotein cholesterol (non-HDL-C), total cholesterol (TC) and apolipoprotein B (ApoB) levels. However, it has minimal effect on lipoprotein (a) (Lp(a)) level. Summary Bempedoic acid is a new lipid-lowering agent that inhibits enzyme ATP-citrate lyase in the cholesterol biosynthesis pathway. Major risk of cardiovascular events and its associated morbidity and mortality are proportional to LDL-C and inflammatory markers levels. It was found that bempedoic acid significantly lowers LDL-C, hs-CRP and other inflammatory markers levels. This drug could potentially be used in patients with elevated cardiovascular risk, in patients with residual cardiovascular risk despite attaining LDL-C goal and in statin intolerant patients.

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New players in the treatment of hypercholesterolaemia: focus on bempedoic acid and inclisiran

Cited by 6 publications

References 17 publications

Achievement of low-density lipoprotein cholesterol targets in Chinese patients with atherosclerotic cardiovascular disease after receiving statins and ezetimibe

Achievement of low-density lipoprotein cholesterol targets in Chinese patients with atherosclerotic cardiovascular disease after receiving statins and ezetimibe

Bempedoic Acid: for Whom and When

Effects of bempedoic acid on markers of inflammation and Lp(a)

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