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Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
Beyond statins: new lipid lowering strategies to reduce cardiovascular risk
Davide Noto1, Angelo B Cefalù, Maurizio R Averna
1Dipartimento Biomedico di Medicina Interna e Specialistica, Università degli Studi di Palermo, Palermo, Italy, notoddd@alice.it.
Insights
New therapies targeting proprotein convertase subtilisin/kexin type 9 (PCSK9), apolipoprotein-B100 (apoB), Cholesteryl ester transport protein (CETP), and microsomal triglyceride transfer protein (MTP) offer additional LDL-C reduction for high-risk patients. These novel agents may improve cardiovascular outcomes beyond statin therapy.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
- Biochemistry
Background:
- Statins are primary therapy for lowering LDL-Cholesterol (LDL-C), crucial for preventing atherosclerotic vascular disease.
- A significant patient subset remains at high risk despite statin use, necessitating advanced lipid-lowering strategies.
Purpose of the Study:
- To review novel therapeutic approaches for further LDL-C reduction.
- To evaluate agents for patients with high residual risk, severe hypercholesterolemia, or statin intolerance.
Main Methods:
- Review of four novel drug classes: PCSK9, apoB, CETP, and MTP inhibitors.
- Analysis of current clinical use and trial data for these emerging therapies.
Main Results:
- ApoB and MTP inhibitors (Mipomersen, Lomitapide) are approved for homozygous familial hypercholesterolemia.
- Ongoing trials for CETP and PCSK9 inhibitors show promise for broader application.
Conclusions:
- Novel inhibitors targeting PCSK9, apoB, CETP, and MTP represent significant advancements in lipid management.
- These agents hold potential for expanded use in high-risk cardiovascular populations, complementing statin therapy.
Abstract:
Statins are the first-line therapy in LDL-Cholesterol (LDL-C) reduction and its clinical use has contributed to significant prevention and treatment of atherosclerotic vascular disease. Yet, a significant proportion of patients remain at high risk. Recently, a number of new therapies have been developed to further lower LDL-C. These agents may provide clinical benefit on top of statin therapy in patients with high residual risk, severe hypercholesterolemia or as an alternative for patients who are intolerant to statins. We review four novel approaches based on the inhibition of proprotein convertase subtilisin/kexin type 9 (PCSK9), apolipoprotein-B100 (apoB), Cholesteryl ester transport protein (CETP) and microsomal triglyceride transfer protein (MTP). ApoB and MTP inhibitors (Mipomersen and Lomitapide) are indicated only for homozygous familial hypercholesterolemia patients. The results of ongoing trials with CETP and PCSK9 inhibitors may warrant a wider employment in different categories of patients at high risk for cardiovascular disease.
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