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Alirocumab and evolocumab are the two primary fully human monoclonal antibodies belonging to the proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor class. Alirocumab (Praluent) was developed by Sanofi and Regeneron, while evolocumab (Repatha) was developed by Amgen. Both agents are approved for the treatment of hypercholesterolemia, including heterozygous and homozygous familial hypercholesterolemia, and for reducing cardiovascular risk in patients with established atherosclerotic cardiovascular disease (ASCVD). They function by binding to circulating PCSK9, preventing it from interacting with and inducing the degradation of low-density lipoprotein receptors (LDLR) on hepatocytes. This increases the density of LDLR on the cell surface, thereby enhancing the clearance of LDL-cholesterol from the bloodstream. In clinical research, such as the Phase 4 trial in Tianjin (ChiCTR2000034635) and real-world registries like PERI-DYS (NCT03110432), these two drugs are often evaluated together as a therapeutic class to assess their impact on lipid profiles, endothelial function, and cardiovascular outcomes.
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