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Updated: Jul 19, 2025
Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
Beyond statins: New pharmacological targets to decrease LDL-cholesterol and cardiovascular events
Emanuel Raschi1, Manuela Casula2, Arrigo F G Cicero3
1Department of Medical and Surgical Sciences, Alma Mater Studiorum - University of Bologna, Bologna, Italy.
Insights
Newer medications offer innovative ways to lower low-density lipoprotein cholesterol (LDL-C) for atherosclerotic cardiovascular disease (ASCVD) risk. This review details their pharmacology, benefits, and risks to guide clinical practice.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
- Lipidology
Background:
- Dyslipidemia is a key modifiable risk factor for atherosclerotic cardiovascular disease (ASCVD).
- Current dyslipidemia treatment guidelines emphasize low-density lipoprotein cholesterol (LDL-C) reduction intensity based on ASCVD risk.
- Debate persists regarding optimal lipid targets and treatment strategies (stepwise vs. upstream therapy).
Purpose of the Study:
- To provide an evidence-based review of novel pharmacological agents for dyslipidemia.
- To detail the pharmacological aspects, benefit-risk profiles, and patient-centered advantages of emerging LDL-C-lowering medications.
- To support clinical practice by minimizing therapeutic inertia in managing dyslipidemia.
Main Methods:
- Review of pharmacological aspects of recently approved LDL-C-targeting medications.
- Analysis of benefit-risk profiles, including impact on cardiovascular endpoints.
- Evaluation of patient-centered advantages, such as adherence.
Main Results:
- Several novel drug classes targeting LDL-C are now available, including PCSK9 inhibitors, ACL inhibitors, ANGPTL3 inhibitors, and MTP inhibitors.
- These agents offer innovative mechanisms of action beyond statins and ezetimibe.
- Understanding their specific profiles is crucial for effective clinical application.
Conclusions:
- Novel pharmacological agents provide new therapeutic options for managing dyslipidemia and reducing ASCVD risk.
- A comprehensive understanding of these drugs' pharmacology, efficacy, safety, and patient impact is essential for optimal treatment selection.
- This knowledge empowers clinicians to tailor therapies, improve patient adherence, and ultimately reduce cardiovascular events.
Abstract:
The pharmacological treatment of dyslipidemia, a major modifiable risk factor for developing atherosclerotic cardiovascular disease (ASCVD), remains a debated and controversial issue, not only in terms of the most appropriate therapeutic range for lipid levels, but also with regard to the optimal strategy and sequence approach (stepwise vs upstream therapy). Current treatment guidelines for the management of dyslipidemia focus on the intensity of low-density lipoprotein cholesterol (LDL-C) reduction, stratified according to risk for developing ASCVD. Beyond statins and ezetimibe, different medications targeting LDL-C have been recently approved by regulatory agencies with potential innovative mechanisms of action, including proprotein convertase subtilisin/kexin type 9 modulators (monoclonal antibodies such as evolocumab and alirocumab; small interfering RNA molecules such as inclisiran), ATP-citrate lyase inhibitors (bempedoic acid), angiopoietin-like 3 inhibitors (evinacumab), and microsomal triglyceride transfer protein inhibitors (lomitapide). An understanding of their pharmacological aspects, benefit-risk profile, including impact on hard cardiovascular endpoints beyond LDL-C reduction, and potential advantages from the patient perspective (e.g., adherence) - the focus of this evidence-based review - is crucial for practitioners across medical specialties to minimize therapeutic inertia and support clinical practice.
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