Home Health News New Drugs for Cholesterol Lowering: PCSK9 Inhibitors

New Drugs for Cholesterol Lowering: PCSK9 Inhibitors

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By Riddhi Patel, MD | Image – BladeTucker/Shutterstock |

Hyperlipidemia is a common medical problem in the United States and worldwide. Total cholesterol is directly related to cardiovascular risk. As a result, there are several classes of drugs intended to lower lipids and there is constantly new research done developing new medicaitons. The first line agent used by most providers are statins as they are relatively safe and effective at lowering cholesterol. However, there are several patients who cannot tolerate these medications and for these patients another class of medications known as PCSK9 inhibitors may be beneficial.

Who should not use statins?

Like all medications, statin can result in a variety of side effects. The most commonly reported side effect is myopathy. These medications can also result in hepatic dysfunction, renal dysfunction, irritability, and aggression. For patients who are intolerant of statins due to side effects, it is recommended that they discontinue statins and use use an alternative method of lipid reduction.

PCSK9 Inhibitors

Proprotein convertase subtilisin kexin 9, or PCSK9, is a serine protease that is made by the liver and leads to the degradation of hepatocyte LDL receptors and thereby leads to increased LDL cholesterol levels. Drugs that inhibit this protease are known as PCSK9 Inhibitors and have shown to be promising. It has been found that these medications have good lipid-lowering abilities both on their own and in combination with statins. PCSK9 Inhibitors can reduce LDL-C by 70% on their own and by 60% in patients on statin therapy.

What makes PCSK9 Inhibitors different?

Unlike the many different agents used for hyperlipidemia, PCSK9 Inhibitors have shown to provide greater reductions in LDL-C and have significant benefits. They have been shown to reduce all-cause mortality, cardiovascular mortality, and MI in patients. The also result in additional cardiovascular risk reductions in patients that are already on maximum statin therapy.

Drugs in this class

Examples of PCSK9 inhibitors are: evolocumab, alirocumab, and bococizumab. Although this category of medications has shown incredible promise in lipid lowering, they are not commonly used because there is not yet good long-term evidence of using these medications as primary prevention.

 

References

  1. McKenney JM, Koren MJ, Kereiakes DJ, et al. Safety and efficacy of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 serine protease, SAR236553/REGN727, in patients with primary hypercholesterolemia receiving ongoing stable atorvastatin therapy. J Am Coll Cardiol 2012; 59:2344.
  2. Navarese EP, Kolodziejczak M, Schulze V, et al. Effects of Proprotein Convertase Subtilisin/Kexin Type 9 Antibodies in Adults With Hypercholesterolemia: A Systematic Review and Meta-analysis. Ann Intern Med 2015; 163:40.
  3. Pignone, M. Treatment of lipids in primary prevention. Up to date. 2016.
  4. Rosenson, RS. Lipid lowering with drugs other than statins and fibrates. Up to date. 2016.

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