Alirocumab: Uses, Interactions, Mechanism of Action - DrugBank …
Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have "gain of function" mutations in autosomal dominant hypercholesterolemia.
PCSK9 Inhibitors - StatPearls - NCBI Bookshelf
Feb 25, 2024 · Proprotein convertase subtilisin/kexin type 9 (PCSK9) has emerged as an important regulator of cholesterol metabolism. 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.
PCSK9 Inhibitors: Mechanisms of Action, Metabolic ... - Annual …
This review discusses the history and mechanism of action of PCSK9 inhibitors, their metabolic effects, and clinical outcomes associated with these medications, highlighting recent large cardiovascular outcome trials investigating these therapies.
PCSK9 - Wikipedia
With the new knowledge about the role of PCSK9 and its location in the genome, they sequenced the relevant region of chromosome 1 in people with very low cholesterol and they found nonsense mutations in the gene, thus validating PCSK9 as a biological target for drug discovery.
Molecular population genetics of PCSK9: a signature of recent …
Whether the effects of PCSK9 on neuronal cell differentiation and apoptosis confer a selective advantage remains speculative. It is also unclear whether gain-of-function mutations in PCSK9 confer novel biochemical and biological functions. Several evolutionary studies have shown evidence of positive selection on gain-of-function mutations.
PCSK9 Inhibition: From Current Advances to Evolving Future
This paper reviewed the mechanism of PCSK9, the classification and clinical application of existing PCSK9 inhibitors, and the latest progress in PCSK9-related research, aiming to provide a reference for clinical drug use and later drug development.
PCSK9 Inhibitors: Clinical Relevance, Molecular Mechanisms, and …
The inhibition of PCSK9 represents a novel approach to reducing LDL levels and preventing adverse CV outcomes in high-risk patients who have not achieved recommended levels of LDL despite the use of a maximally optimized therapeutic arsenal.
PCSK9 Inhibitors: Mechanism of Action, Efficacy, and Safety
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a proteolytic enzyme that indirectly regulates serum LDL cholesterol (LDL-C) by causing the destruction of LDL receptors.
Contrasting effects of intracellular and extracellular human PCSK9 …
Aug 13, 2024 · PCSK9 inhibition affect biological pathways, induces lipid peroxidation, and higher level of apoptosis in response to staurosporine. Our results suggest that higher levels of PCSK9 in BALF...
Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): …
Jan 8, 2024 · Proprotein convertase subtilisin/kexin type 9 (PCSK9) has evolved as a pivotal enzyme in lipid metabolism and a revolutionary therapeutic target for hypercholesterolemia and its related...
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