Therapeutic peptides – a revival of interest

The innovation process in the pharmaceutical industry is, as for all evolutionary models of technological change, both ‘pushed by technology’ and ‘demand driven’. The core of the innovation relies on the research for new high value-added drugs to address unmet medical needs. To this end, tens of billions of dollars are invested per year in R&D. However, the decreasing number of approved drugs, which is accompanied by increasing R&D expenditures, demands alternative approaches to increase R&D productivity. This situation contributes to a revival of interest in peptides as potential tools and drug candidates.

The field of therapeutic peptides is undergoing a very exciting revival owing to substantial technological progresses during the last decade. Indeed, therapeutic peptides are likely to boost pharmaceutical industry pipelines by providing effective and innovative solutions for unmet medical needs, thus meeting the strict demands from regulatory authorities. In this issue of Drug Discovery Today Editor’s Choice, we will be looking at the recent progresses in technology-related research on peptides and market data.
The first of our free downloads from Gert N. Moll, Anneke Kuipers, Louwe de Vries, Tjibbe Bosma and Rick Rink deals with “A biological stabilization technology for peptide drugs: enzymatic introduction of thioether-bridges”. The authors explain how the introduction of thioether-bridges, which are more stable than peptide bonds and disulfide bridges, confer strong resistance against proteolytic degradation. They describe how nisin-modifying enzymes, contained in the Lactococcus lactis bacterium, introduce chemo-, regio- and stereo-specific thioether-bridges in peptides. This emerging biological technology has huge potential for producing highly effective peptide drug-candidates.
The next review “HIV-derived peptide mimics” by Kalle Moebius and Jutta Eichler deals with synthetic peptides as tools for the mimicry of specific protein sites. In this review, the authors make use of peptides capable of mimicking functionally important regions of HIV proteins as tools to explore their structure and function. Furthermore, the authors cover the topic of the use of such peptides as starting points for novel therapeutic and preventive anti-HIV strategies, which will be of paramount importance to the development of new treatments for AIDS. Enfuvirtide (Fuzeon®), a 36 amino acid peptide derived from HIV-1 glycoprotein-41, was the first HIV fusion inhibitor approved for clinical use.
In the next review from Lawrence R. Dick and Paul E. Fleming entitled “Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy”, inhibition of the proteasome degradation machinery is presented as a novel effective anti-cancer therapeutic approach, as exemplified by the discovery of the first-in-class drug bortezomib, a peptide boronic acid. Since the approval of bortezomib (Velcade®) for the treatment of multiple myeloma and mantle cell lymphoma, more promising second-generation proteasome inhibitors, including peptide boronic acid analogues and peptide epoxyketones, are currently in preclinical or clinical development phases.
We conclude this series with our recent review entitled “Synthetic therapeutic peptides: science and market”. My colleagues (Vincent Lisowski, Jean Martinez and Michel Khrestchatisky) and I address the science and the market for synthetic therapeutic peptides. We discuss the pros and cons of the use of peptides as drug candidates. This review reports on the unexpected and considerable number of peptides that are currently available as drugs and the chemical strategies that were used to bring them into the market. Approximately 70 synthetic therapeutic peptides (including those used for medical diagnosis or imaging), less than 50 amino acids in length, have been approved in the American, European and/or Japanese pharmaceutical markets (see Table 2). To date, in addition to these synthetic therapeutic peptides, more than 150 other peptide drugs and related compounds (i.e. biologic drugs) are also marketed (see Table 3).
As demonstrated herein, peptide-based drug discovery provides a serious option for addressing new therapeutic challenges in multiple pathologies.
Patrick Vlieghe is a Senior Scientist and is currently the Head of Development at Vect-Horus, a drug targeting company. He studied Organic Chemistry at the University of Montpellier, France, where he obtained a BSc in Chemistry and a MSc in Biomolecular Chemistry. He completed his PhD degree in Medicinal Chemistry at the University of Aix-Marseilles, France. He then received a Specialized Master's in Healthcare Company Management at Euromed Management, a French Business School in Marseilles, France. He has 15 years of pharmaceutical and biotech experience, working notably in drug discovery, chemical optimization, vectorization (drug targeting, drug delivery and targeted drug delivery) and early-stage preclinical drug development. He has held several positions as Research Scientist in Medicinal Chemistry, Scientist Project Manager in Business Intelligence & Business Development and Consultant in Entrepreneurship & Biotechnologies. His scientific work has resulted in 10 patents and 12 peer-reviewed articles.

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