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Published on: August 28, 2018
Emerging PCSK9 inhibitors for treating dyslipidaemia: buttressing the gaps in coronary prevention
Michael M Page1, Gerald F Watts
1Lipid Disorders Clinic, Cardiovascular Medicine, Royal Perth Hospital , Perth , Australia.
Insights
New proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors offer hope for high-risk patients with high cholesterol and elevated lipoprotein(a). These therapies may reduce cardiovascular events, especially for those with familial hypercholesterolaemia or statin intolerance.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Background:
- Atherosclerotic cardiovascular disease (ACVD) is a leading global cause of death.
- High low-density lipoprotein-cholesterol (LDL-C) levels significantly contribute to ACVD.
- Statins are primary cholesterol-lowering therapies, but additional options are needed.
Purpose of the Study:
- To discuss the medical need for novel cholesterol-lowering treatments.
- To review the scientific rationale for proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors.
- To outline the current therapeutic status of PCSK9 inhibitors.
Main Methods:
- Literature review on ACVD, LDL-C, and PCSK9 inhibitors.
- Discussion of clinical evidence and ongoing trials for PCSK9 inhibitors.
- Analysis of PCSK9 inhibition mechanisms and therapeutic applications.
Main Results:
- PCSK9 inhibitors represent a new class of cholesterol-lowering drugs.
- These inhibitors are particularly beneficial for patients with familial hypercholesterolaemia (FH) and statin intolerance.
- Elevated lipoprotein(a) (Lp(a)) levels may also respond to PCSK9 inhibition.
Conclusions:
- Anti-PCSK9 monoclonal antibodies (mAbs) are a promising therapy for managing high cholesterol.
- PCSK9 inhibitors offer hope for patients with FH, statin intolerance, and elevated Lp(a).
- Further clinical trials are investigating the efficacy of PCSK9 inhibitors in reducing cardiovascular events in high-risk populations.
Introduction:
Atherosclerotic cardiovascular disease (ACVD) is the leading cause of mortality worldwide. An abnormally high plasma level of low-density lipoprotein-cholesterol is a major contributor to ACVD, an effect that can be attenuated by cholesterol-lowering therapies, particularly statins. A new class of drugs, the proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, will add another option for further reducing cardiovascular events in patients at high risk of ACVD, including those with familial hypercholesterolaemia (FH) and intolerance to statins. Patients with elevated levels of lipoprotein(a) (Lp(a)) are difficult to treat with conventional therapies, and may also benefit from PCSK9 inhibitors.
Areas Covered:
This paper discusses the medical need for additional cholesterol-lowering therapies and the scientific rationale and current therapeutic status of PCSK9 inhibitors.
Expert Opinion:
The use of anti-PCSK9 mAbs is the leading form of therapy for inhibiting PCSK9 and is likely to provide genuine hope for patients with FH, statin intolerance and elevated Lp(a). Their ability to reduce cardiovascular events in patients maximally treated with statins and other existing therapies remains to be proven, and is the subject of major ongoing clinical trials.
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