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7475778 
Journal Article 
Review 
Tailor-made amino acid-derived pharmaceuticals approved by the FDA in 2019 
Yin, Z; Hu, W; Zhang, W; Konno, H; Moriwaki, H; Izawa, K; Han, J; Soloshonok, VA 
2020 
Yes 
Amino Acids
ISSN: 0939-4451
EISSN: 1438-2199 
52 
9 
1227-1261 
English 
32880009 
Amino acids (AAs) are among a handful of paramount classes of compounds innately involved in the origin and evolution of all known life-forms. Along with basic scientific explorations, the major goal of medicinal chemistry research in the area of tailor-made AAs is the development of more selective and potent pharmaceuticals. The growing acceptance of peptides and peptidomimetics as drugs clearly indicates that AA-based molecules become the most successful structural motif in the modern drug design. In fact, among 24 small-molecule drugs approved by FDA in 2019, 13 of them contain a residue of AA or di-amines or amino-alcohols, which are commonly considered to be derived from the parent AAs. In the present review article, we profile 13 new tailor-made AA-derived pharmaceuticals introduced to the market in 2019. Where it is possible, we will discuss the development form drug-candidates, total synthesis, with emphasis on the core-AA, therapeutic area, and the mode of biological activity.