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Underberg - Figure 21 - Proprotein Convertase subtilisin/kexin Type 9 (PCSK9) Inhibitors

PCSK9 inhibitors represent a class of medications that act directly or indirectly on a protein called PCSK9 that modulates the expression of the LDL receptor.  Patients with nonsense mutations in the PCSK9 gene have a significantly lower level of LDL-C and a decreased incidence of CHD.  In preclinical trials, over-expression of PCSK9 has resulted in increased levels of non-HDL cholesterol.  Two recent monoclonal antibody trials that were presented at the American Heart Association (AHA) meeting in 2011 showed that LDL-C was lowered by an average of up to 60%.
Underberg J Clin Lipidol. 2012;
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References

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[38] Cohen JC, et al. NEJM. 2006;354:1264-1272

[43] Bejannet S, et al. J Biol Chem. 2004;279:48865-48875.

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