A Comprehensive, Updated Review of Ezetimibe: Evidence-Based Clinical Use for Atherosclerotic Cardiovascular Disease

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Abstract
Elevated low-density lipoprotein cholesterol (LDL-C) is a key modifiable risk factor in atherosclerotic cardiovascular diseases. While statins are the first-line therapy for LDL-C management, challenges such as limited additional benefits with dose escalation and an increased risk of adverse drug reactions at higher doses remain. Ezetimibe is widely recommended in clinical guidelines and has become an essential component of lipid-lowering therapy, particularly for patients requiring additional LDL-C reduction beyond what statins alone can achieve. Ezetimibe monotherapy reduces LDL-C levels by approximately 17.1-25.9% and significantly lowers the risk of major adverse cardiovascular events compared with placebo. For patients whose LDL-C levels remain uncontrolled with statin therapy, adding ezetimibe not only achieves greater LDL-C reduction but also improves goal attainment, reduces plaque burden, enhances plaque stability, and lowers the incidence of cardiovascular events. Furthermore, combining ezetimibe with statins into one tablet offers advantages in medication management, improving patient compliance and convenience. In addition, combining ezetimibe with nonstatin lipid-lowering agents also offers a comprehensive approach to lipid management, especially in complex cases of dyslipidemia or cardiovascular risk management. Despite robust clinical evidence and good tolerability, the adoption of ezetimibe combination therapy in real-world practice remains limited, likely owing to insufficient awareness among clinicians and patients. In this review, we summarize the current evidence to support clinical decision-making and promote the optimal use of ezetimibe in the management of atherosclerotic cardiovascular diseases.
Funding Information
  • Fuwai Hospital, Chinese Academy of Medical Sciences (2025-I2M-C&T-B-022)
  • Fuwai Hospital, Chinese Academy of Medical Sciences (2021-I2M-1-008)

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