Department of Cardiovascular Medicine, Cleveland Clinic Foundation, Cleveland, OH, USA.
Section of Preventive Cardiology and Rehabilitation, Department of Cardiovascular Medicine, Cleveland Clinic Foundation, 9500 Euclid Avenue, Mail Code JB1, Cleveland, OH, 44195, USA.
Curr Atheroscler Rep. 2024 Oct;26(10):603-608. doi: 10.1007/s11883-024-01231-5. Epub 2024 Aug 16.
To provide perspective on the current development status, and potential future role, of obicetrapib, a third-generation cholesterylester transfer protein (CETP) inhibitor. Obicetrapib has received recent attention following positive Phase II clinical trial data and initiation of Phase III trials for the treatment of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).
The ROSE and ROSE2 trials are Phase II studies that examined the lipid lowering effects of obicetrapib in patients on pre-existing high-intensity statin therapy. Obicetrapib significantly reduced key dyslipidemia biomarkers including low density lipoprotein cholesterol (LDL-C), Apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) while increasing high-density lipoprotein cholesterol (HDL-C). Four phase III clinical trials, including a cardiovascular outcomes trial, are ongoing. Preliminary data for obicetrapib shows favorable effects on dyslipidemia, which could theoretically lead to a decrease in ASCVD clinical events. Short-term safety data in preliminary studies shows no significant safety signals.
提供第三代胆固醇酯转移蛋白（CETP）抑制剂依泽替米贝的当前发展状况和未来可能的作用。依泽替米贝在治疗血脂异常和动脉粥样硬化性心血管疾病（ASCVD）的 III 期临床试验启动后，根据 II 期临床试验的阳性数据，近期受到了关注。
ROSE 和 ROSE2 是两项 II 期研究，旨在评估依泽替米贝在已接受高强度他汀类药物治疗的患者中的降脂作用。依泽替米贝可显著降低关键的血脂异常生物标志物，包括低密度脂蛋白胆固醇（LDL-C）、载脂蛋白 B（Apo B）和非高密度脂蛋白胆固醇（非-HDL-C），同时增加高密度脂蛋白胆固醇（HDL-C）。四项 III 期临床试验正在进行中，其中包括一项心血管结局试验。依泽替米贝的初步数据显示对血脂异常有良好的影响，理论上可降低 ASCVD 临床事件的发生。初步研究的短期安全性数据未显示出明显的安全性信号。
