Foreword 2

Since the discovery of therapeutically important hormones such as insulin and oxytocin, peptide-based drug discovery has gained significant importance. In addition to demonstrating their utility as therapeutic agents, peptides are finding increased use as molecular probes to understand biological pathways of human disease and as diagnostic tools.

As a therapeutic modality, peptides address an important gap between classical small-molecule drugs and antibodies with a rather high molecular weight. The latter agents are typically administered via intravenous or subcutaneous routes. The significant success of peptides in biomedicine has become possible as a result of the remarkable progress that has been made with respect to peptide design, manufacturing, improved stability, half-life prolongation and new delivery systems. Nowadays, peptides can be designed to address targets in the intracellular space, and research into the oral delivery of peptides is making significant progress.

Currently, more than 60 peptidic drugs are approved as marketed medicines and more than 350 peptide therapeutics are under clinical investigation targeting a wide variety of disease indications; oncology and metabolic disorders, but also neurological and inflammatory disorders. Remarkably, the current scope of peptide drugs is not limited to injectables, since alternative formulations and needle-free systems allowing for pulmonary, transdermal and oral delivery have either advanced to the market or are in late-stage clinical studies. Although the United States and Europe have so far been the key markets for therapeutic peptides, Asia Pacific and Latin America will offer significant opportunities in the coming years.

Today, peptide-based drug discovery is undertaken in a large number of laboratories across the world, including in large pharmaceutical companies and biotech and academic institutions. In fact, the enormous progress and opportunities in peptide therapeutics outlined above have led to the launching of several peptide-focused new companies in Europe, the US and Asia over the past decade—biotech or contract research or manufacturing organizations. This book attests to a promising future for the field of peptide science, which could further broaden in scope and offer new opportunities and therapeutic applications.

In Peptide-based Drug Discovery, well recognized experts in the field share their insight and views on many of these aspects. Central topics include the early identification of lead structures, design considerations and peptide optimization strategies with the overall goal to develop next-generation peptides as effective drugs for a variety of indications, as well as diagnostic tools and biomarkers.

I strongly applaud and recommend this book; it will serve as a valuable source of knowledge for experienced peptide and protein scientists in industry and academia, and also for the many young scientists aspiring to enter this field of research.

Michael Wagner

Sanofi-Aventis Deutschland GmbH

Frankfurt, Germany