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Novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors: a patent review
1Pfizer Global Research & Development, Cardiovascular, Metabolic & Endocrine Disease Chemistry, MS 8220-3020, Eastern Point Road, Groton, CT 06340, USA jeffrey.a.pfefferkorn@pfizer.com
Insights
New statins show promise for managing high cholesterol (hypercholesterolemia) and reducing cardiovascular disease (CVD) risk. Further research into next-generation HMG-CoA reductase inhibitors is crucial for patients not meeting LDL-C targets.
Area of Science:
- Cardiovascular medicine
- Pharmacology
- Medicinal chemistry
Background:
- Cardiovascular disease (CVD) remains a leading global cause of mortality.
- Elevated low-density lipoprotein cholesterol (LDL-C) is a primary risk factor for CVD.
- Statins (HMG-CoA reductase inhibitors) are the current standard for hypercholesterolemia treatment, effectively lowering cholesterol biosynthesis.
Purpose of the Study:
- To review patent literature and advancements in HMG-CoA reductase inhibitor discovery and development between 2000 and 2010.
- To examine the properties of next-generation statin candidates.
- To assess the potential of novel statins in further reducing cardiovascular disease incidence.
Main Methods:
- Comprehensive review of patent literature from 2000-2010.
- Analysis of clinical candidates for HMG-CoA reductase inhibition.
- Evaluation of efficacy and tolerability profiles of emerging statins.
Main Results:
- Statins have significantly impacted global CVD reduction.
- Many high-risk patients do not achieve target LDL-C levels with current statins.
- Novel statins with enhanced efficacy and tolerability are under development.
Conclusions:
- Despite statin advancements, CVD remains a major health concern, necessitating further innovation.
- Next-generation statins offer potential for improved LDL-C management in high-risk populations.
- Continued development of HMG-CoA reductase inhibitors is vital for reducing the global burden of cardiovascular disease.
Introduction:
Cardiovascular disease (CVD) is a leading cause of death worldwide and hypercholesterolemia, or elevated low-density lipoprotein cholesterol (LDL-C), is a key risk factor. The standard of care for treating hypercholesterolemia is the use of HMG-CoA reductase inhibitors, also known as statins, which block the rate-limiting step of cholesterol biosynthesis. In widespread clinical use, statins have proven safe and effective for both primary prevention of coronary heart disease and secondary prevention of coronary events.
Areas Covered:
This review summarizes the patent literature and advances in the discovery and development of new HMG-CoA reductase inhibitors from 2000 to 2010.
Expert Opinion:
The discovery of statins has had significant impact on reducing the worldwide burden of cardiovascular disease; nevertheless, the fact that heart disease remains a leading cause of death indicates that additional efforts are still needed. Using current statins, most patients at low and moderate risk of CVD reach recommended LDL-C targets, but a significant portion of patients in the high risk category fail to achieve optimal LDL-C targets. The potential introduction of novel statins with increased efficacy and tolerability profiles may represent an opportunity to further reduce the incidence of cardiovascular disease. Herein, I review the patent literature and examine the properties of several next generation statin clinical candidates.
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