Peptide Therapeutics 2.0

In recent years, the peptide drug discovery field has shown a high level of dynamism, with hundreds of academic groups working on this topic, the creation of new peptide-focused companies, and the consolidation of peptide business by so-called big pharma [...].

In recent years, the peptide drug discovery field has shown a high level of dynamism, with hundreds of academic groups working on this topic, the creation of new peptide-focused companies, and the consolidation of peptide business by so-called big pharma [1][2][3][4].
In the last five years (2015-2019), the U.S. Food Drug Administration (FDA) have authorized a total of 208 new drugs (150 new chemical entities and 58 biologics) [5,6], 15 of which were peptides or peptide-containing molecules (Table 1), which account for 7% of the total number of drugs [4,7]. This is a rather impressive number, if we consider the efforts of the pharmaceutical industry in peptides in comparison to small molecules (in the context of this work, a peptide is defined as a compound that contains two or more amino acids linked by an amide (peptide) bond and that can be synthesized chemically).
The chemical structure and medical indication of the active principle ingredient of these drugs show an excellent representation of the diversity of the peptide world.
Oncology, with five drugs (two radio peptides and two ADCs), metabolism (three), and endocrinology (two) are the most frequent medical indications for peptides. However, cardiovascular conditions, gastroenterology, bone diseases, dermatology, and sexual dysfunction are also targeted by peptides.
Of note, between 2015 and 2019, several of the new peptide-based drugs accepted by the FDA came about from the efforts of academic groups. This highlights the importance of fostering solid and efficient cooperation channels between academia and industry with the aim to maintain and improve the well-being of society.
In addition to the use of peptides as drugs or in diagnostics, these molecules are playing an increasingly important role as drug delivery systems and as the base for new biomaterials with broad potential applications in medicine. This analysis supports the strength of peptides in the medicinal field. In this context, we have decided to publish a Special Issue in Molecules, termed "Peptide Therapeutics 2.0", which contains excellent quality research articles and comprehensive reviews on peptides. It is hoped that some of the peptides introduced herein will reach the market in the coming years.