Amino acids (AAs) play an important role in the modern health industry. The aim of this article was to assess that AAs’ residues are frequently found in the structures of smallmolecule modern pharmaceuticals, while peptidomimetics and peptide-based drugs are entirely derived from AAs. Currently, AAs serve as key structural features in numerous successful pharmaceuticals, so-called blockbuster drugs. In this work, we provide a detailed profile of 5 peptidomimetics and 4 peptide drugs. For each compound, we describe the spectrum of biological activity, medicinal chemistry discovery, and synthetic preparation.