Peptides as Drugs: Is There a Market?

Abstract

The first synthetic peptide was prepared by Emil Fischer a century ago, but the medicinal use of synthetic peptides started after the Second World War, and only when peptides could be prepared pure by du Vigneaud’s group in the USA, and by the Swiss industrial groups of Robert Schwyzer (Ciba) and Huguenin (Sandoz). This was the time of oxytocin and vasopressin, cyclic nonapeptides with one disulphide bridge, and of the angiotensins. The synthesis of peptides was a long and difficult task, a single peptide taking 1–2 years to produce by conventional methods. It was the genius of Bruce Merrifield, in 1963, who hastened and automated this long process using the method he named Solid Phase Peptide Synthesis (SPPS). The acceptance of the method was rather fast, helped by the development of new purification methods (HPLC) which allowed purification of some incredible mixtures. From the 1960s to the end of the Millennium, peptides were often considered as the drugs of the future. Their main drawback was their low bioavailability. Further, some major pharmaceutical companies, which had invested heavily in peptide projects, had to drop some of these in the late clinical phase.