2021年9月1日 · PCSK9 inhibitors can help treat high cholesterol by directly modifying this gene to reduce the amount of LDL in your body. Learn about the PCSK9 gene, how PCSK9 inhibitors affect LDL cholesterol...

PCSK9, an enzyme (serine protease) encoded by the PCSK9 gene, is predominantly produced in the liver . PCSK9 binds to the LDL receptor (LDL-R) on the surface of hepatocytes, leading to the degradation of the LDL-R and subsequently to higher plasma LDL-C levels .

What are PCSK9 inhibitors? Proprotein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme that binds to low-density lipoprotein receptors (LDL receptors), which stops LDL being removed from the blood, leading to an increase in blood levels of LDL.

PCSK9 inhibitors are a cholesterol-lowering medicine. They work by decreasing your levels of low-density lipoprotein (LDL) cholesterol. Your provider may prescribe PCSK9 inhibitors if you have tried other medicines and still have high cholesterol.

2024年2月25日 · In the United States, 2 fully humanized monoclonal antibodies—alirocumab and evolocumab— have been approved by the US Food and Drug Administration (FDA) to inhibit or reduce PCSK9 activity. Recently, both the European Union and FDA have approved inclisiran, a small interfering mRNA, that inhibits intracellular PCSK9 synthesis.

Proprotein convertase subtilisin/kexin type 9 serine protease (PCSK9) plays an important role in cholesterol metabolism by regulating LDL receptor degradation. Shortly after its discovery in 2001, the gene encoding PCSK9 was implicated in familial hypercholesterolemia (FH).

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme encoded by the PCSK9 gene in humans on chromosome 1. [5] It is the 9th member of the proprotein convertase family of proteins that activate other proteins. [6] Similar genes are found across many species.

2016年10月1日 · PCSK9 inhibitory antibody therapies target a novel pathway in LDL-cholesterol metabolism, and early phase I and II trials show highly promising results. Results of large-scale and longer term phase III trials are awaited and these will yield better information about efficacy and adverse effects.

Over the last decade, inhibition of proprotein convertase subtilisin/kexin type 9 (PCSK9) has emerged as a promising therapeutic strategy to reduce residual cardiovascular disease risk. Binding of PCSK9 to the LDL receptor targets the receptor for lysosomal degradation.

PCSK9 is a hepatic protease that attaches to and internalizes LDLR into lysosomes hence promoting their destruction. Clinical studies have shown that PCSK9 gain of function mutation is associated with familial hypercholesterolemia and premature CVD[10,11].