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To reach their site of action following oral administration, drugs must first be absorbed from the gastrointestinal tract. Therefore, design of compounds capable of passing through the gut wall is a key aspect of drug discovery and overwhelmingly this is achieved through the optimization of passive permeability to enable absorption by the transcellular route. In this chapter we describe methods for screening, the physicochemical principles underlying optimal passive permeability and provide examples of how these principles can be leveraged to optimise passive permeability during drug design. Additionally, given the changing pharmacological target landscape and the pressure it imposes on historical physicochemical design guidelines, we briefly discuss the implications of working in so called “beyond rule-of-five” space and how this might affect future drug design strategies.

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