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Let's revisit a modern “classic in drug discovery” and a lesson that nothing is impossible in the #small_molecule R&D: Macrocyclic PCSK9 protein-protein interaction (PPI) inhibitor, MK-0616, is a once-daily #PCSK9-lowering and #LDL_cholesterol-lowering small molecule that has recently demonstrated antibody-like efficacy as an oral agent in the clinic. Origins of the compound here: https://lnkd.in/eqXdj8Fh

A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors

A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors

pubs.acs.org

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