PCSK9 inhibitor products are expensive and are not included in medical insurance. PCK9 inhibitors, which are expected to be included in medical insurance in the future, are a class of compounds that inhibit PCK9 (the ninth member of subtilisin family of Cushing-like transprotein). At present, these inhibitors are a new class of lipid-lowering drugs. Extended data PCK9 is a liver-derived secretory protein, which binds to the extracellular domain of LDLR. However, the degradation of LDLR by PCK9 is intracellular. PCSK9 does not need the catalytic activity of kinase to affect the transformation of LDLR, and the catalytic activity of kinase can not guide the complex with receptor into lysosomes degraded by the complex or inhibit the circulation of the complex.

PCSK9, as a invertase that regulates neuronal apoptosis, not only participates in liver regeneration and regulates neuronal apoptosis, but also affects the internalization of LDL by reducing the amount of LDLR on hepatocytes, so that LDL in blood cannot be removed, resulting in hypercholesterolemia. Studies have shown that PCSK9 levels are significantly correlated with cholesterol, ox-LDL and triglycerides. PCSK9, as a serine protease, not only degrades LDLR and increases blood LDL level, but also has many other biological functions, such as participating in the development of nervous system, apoptosis of nerve cells, regulating sodium channels and islet cells.

The production process of PCK9 is firstly to synthesize PCK9 proenzyme in endoplasmic reticulum, and autocatalytic reaction occurs in endoplasmic reticulum or Golgi apparatus, which cleaves and releases propeptide to form mature protease, which is immediately secreted into the blood. By regulating LDLR, the plasma lipid can be maintained in a stable state, which can not only affect the plasma cholesterol level and regulate the apoptosis of nerve cells, but also have a certain correlation with inflammatory reaction. PCK9 inhibitor is a new drug used in clinic recently, and it is a completely humanized monoclonal antibody, which can bind with free PCK9 in plasma, thus reducing the plasma low density lipoprotein level.