Development, optimization and scale up of therapeutic peptides: approaches to solid phase synthesis and purification

The application and reliance on Solid Phase Peptide Synthesis (SPPS) has increased dramatically over recent years with the rise of peptides in diagnostic and therapeutic research. With this rapid increase in development activity, automated synthesis methods have had to adapt to be compatible with the wide range of coupling chemistries, reaction conditions and synthesis monitoring available to the practicing chemist. The subsequent purification of the synthesized peptides in that process demands rapid scale-up what is easily achieved using the Peptide Easy Clean (PEC) technology. The need for parallel, simultaneous reaction screening to optimize SPPS and purification conditions has never been greater. Here we describe the automated screening of multiple reaction conditions for the synthesis of a selection of therapeutic peptides, enabling the optimum synthetic conditions to be selected for each target, followed by the scale-up of the synthesis on a pilot-scale instrument. The rapid purification from mg to gram-scale using the PEC technology is show-cased on Liraglutide

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