A major milestone for peptide therapeutics: the FDA has approved LIPFENDRA® (enlicitide), the first and only once-daily oral PCSK9 inhibitor for lowering LDL cholesterol in adults with hypercholesterolemia. Merck and others are leading this exciting trend in macrocyclic peptides. This approval represents more than a new cholesterol therapy—it is an important milestone for the entire field. Macrocyclization offers significant advantages by improving peptide stability, target binding, and oral bioavailability. This approval clearly demonstrates its potential.