Abstract
Aim: PCSK9 has been shown to be a favorable target for treating patients with hypercholesterolemia whose LDL-C cannot be achieved the target level using statins and ezetimibe. We have already reported the efficacy and safety of 2',4'-bridged nucleic acid (BNA)/locked nucleic acid (LNA)-based antisense oligonucleotides (ASO) targeting PCSK9 (Mol Ther Nucleic Acids, 2012). Towards clinical use of anti-PCSK9 ASO, the sequences of ASOs targeting human PCSK9 were optimized and their in vivo efficacy and safety were evaluated using nonhuman primates.
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