Reducing the bottleneck in target synthesis

Executive summary

Using the Biotage automated workflow, models have shown that the time taken to produce a target molecule can be reduced by up to eighty percent, allowing project delivery timescales to be reduced accordingly. In a normal chemical laboratory the chemists multitask to make the most efficient use of their time, but this does not reduce the actual time taken to move from molecule concept to a synthesized, purified target molecule. The Biotage automated workflow addresses this directly with methodologies expressly designed to reduce the time taken from target identification to delivery of purified product. 

Introduction

The spiralling cost of pharmaceutical R&D means that pressure to work smarter in drug discovery has never been greater. The cost of launching a drug on to the market has recently been estimated at $2.7 billion1, over fifty percent of which is accounted for in investor losses while research into the new drug is on-going. Identifying and completing research into that new drug is principally an act of finding and dismissing unsuitable molecules from the billions available in the chemical research space until the right molecule is found—on average it is estimated that between 5,000 and 10,000 potential drug molecules are investigated to produce one approved therapy2. The huge cost of drug discovery has forced new paths for R&D, with CROs and outsourcing becoming increasingly competitive alternative models to traditional pharmaceutical R&D.
The potential profitability of drugs is also influenced by their development time, as it takes on average 10 years to move a molecule from the discovery stage to an approved drug on the shelves, and the twenty year patent exclusivity period begins when human trials are underway.
In the laboratory, the integrated approach to drug discovery presents the laboratory head with a target list of potential molecules with required physio-chemical parameters that must be made to the necessary purity within as short timeframe as possible. Chemists multitask to ensure their time is used most efficiently, but the process of delivering the appropriate library by creating molecules on the target list is still time consuming and a potential bottleneck to project progression. Longer timescales in synthesis also restrict chemists from a more agile approach to projects, reducing flexibility of the laboratory to take on new projects.

Literature number: PPS466