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Evolocumab
Mechanism of action:
Evolocumab is a PCSK9 inhibitor and a monoclonal antibody. Under normal conditions, PCSK9 binds to low-density lipoprotein receptors (LDLR) on the surface of hepatocytes and, after receptor internalization, promotes their degradation in lysosomes, preventing receptor recycling back to the cell surface. Evolocumab specifically binds to PCSK9 and prevents its interaction with LDLR. This increases the availability of LDLR on the hepatocyte surface and promotes LDL-C clearance.
Reference(s):
Kasichayanula S et al. (2018). Clinical Pharmacokinetics and Pharmacodynamics of Evolocumab, a PCSK9 Inhibitor. Clin Pharmacokinet.
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