4.3 Review

New pharmaceuticals approved by FDA in 2020: Small-molecule drugs derived from amino acids and related compounds

Journal

CHIRALITY
Volume 34, Issue 1, Pages 86-103

Publisher

WILEY
DOI: 10.1002/chir.23376

Keywords

anticancer; asymmetric synthesis; biological activity; COVID-19; peptides; peptidomimetics; small-molecule drugs; tailor-made amino acids

Funding

  1. IKERBASQUE, Basque Foundation for Science
  2. Jiangsu Province
  3. Qing Lan Project
  4. National Natural Science Foundation of China

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Amino acids play a crucial role in the modern health industry as key synthetic precursors for pharmaceuticals, biomaterials, biosensors, and drug delivery systems. In 2020, FDA approved 12 newly introduced pharmaceuticals derived from amino acids, covering various therapeutic areas.
Amino acids (AAs) play an important role in the modern health industry as key synthetic precursors for pharmaceuticals, biomaterials, biosensors, and drug delivery systems. Currently, over 30% of small-molecule drugs contain residues of tailor-made AAs or derived from them amino-alcohols and di-amines. In this review article, we profile 12 AA-derived new pharmaceuticals approved by the FDA in 2020. These newly introduced drugs include Tazverik (epithelioid sarcoma), Gemtesa (overactive bladder), Zeposia (multiple sclerosis), Byfavo (induction and maintenance of procedural sedation), Cu 64 dotatate, and Gallium 68 PSMA-11 (both PET imaging), Rimegepant (acute migraine), Zepzelca (lung cancer), Remdesivir (COVID-19), Amisulpride (nausea and vomiting), Setmelanotide (obesity), and Lonafarnib (progeria syndrome). For each compound, we describe the spectrum of biological activity, medicinal chemistry discovery, and synthetic preparation.

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