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PF-06815345 is an orally active, investigational small molecule developed by Pfizer as a selective inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). It acts by inhibiting the ribosomal synthesis of PCSK9, a protein that regulates cholesterol homeostasis by promoting the degradation of low-density lipoprotein receptors (LDLR) in the liver. By reducing PCSK9 levels, PF-06815345 aims to increase LDLR availability and lower plasma LDL cholesterol. The compound demonstrated potent inhibition of PCSK9 with an IC50 value of approximately 13.4 μM and showed efficacy in lowering plasma PCSK9 in humanized mouse models. Its development reached Phase 1 clinical trials for hypercholesterolemia but was subsequently discontinued[1][2][3][4][5].
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