During the last decade, GlaxoSmithKline Pharmaceuticals (GSK) has carried out much of the seminal work in the area of micro fluidics and micro flow assay for lead optimisation. It has pioneered and built an in-house micro fluidic system for drug discovery. The huge and diverse advantages of this approach come from its miniaturised nature and its scale, which makes it easily automatable. As a result of its miniaturised nature it allows for greater control over heat and mass transfer, along with lower consumption of reagents (both chemical and biological) and solvents, less waste generation and decreased exposure to potentially toxic materials. But for a pharmaceutical company, the main advantage of this technology is the capability of coupling a fast microfluidic chemistry generator with a modern compatible miniaturised screening technique to generate instant biological information (i.e. the assay results) in “real time” that can be used to refine the chemistry (closing the feedback loop) and therefore allowing for a much faster lead optimisation. We will review some of the efforts within GSK towards this pioneering work in the development of miniaturised chemistry platforms capable of performing multiple functions such as synthesis, separation, quantification and screening.

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