FERNANDO ALBERICIO1,2
1. Peptide Science Laboratory, School of Chemistry and Physics,
University of KwaZulu-Natal, Westville, South Africa.
2. Department of Organic Chemistry and CIBER‑BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine, University of Barcelona, Barcelona, Spain

Abstract

Last year in this same forum, we affirmed that we are witnessing a golden age of peptides and oligonucleotides as pharmaceuticals (1)…

Last year in this same forum, we affirmed that we are witnessing a golden age of peptides and oligonucleotides as pharmaceuticals (1). In this regard, from 1 January 2016 to 30 April 2023, the US Food and Drug Administration (FDA) approved 31 new drugs whose active pharmaceutical ingredients (APIs) contain peptides (Table 1). This list includes six radioactive peptide‐based thera/diagnostic agents and four antibody drug conjugates (ADCs) with a peptide drug.

The consolidation of peptides as a key class of new drugs was facilitated by three events that took place in 2022. First, in October, Professor Morten Meldal was awarded the 2022 Nobel Prize in Chemistry, together with Professors Barry Sharpless (La Jolla Scripps Research Institute) and Carolyn Bertozzi (Stanford University). Although the prize was given “for the development of Click (Huisgen cycloaddition) chemistry and bioorthogonal chemistry”, it is important to remember that Morten Meldal is a peptide chemist who has made significant contributions to the development of Fmoc chemistry and peptide-based nanotechnologies. After Vincent du Vigneaud (1955) and Bruce Merrifield (1984), Morten Melda ...