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Microfluidics use at early phases of target discovery and validation are reviewed.Synthesis and formulation are improved when realized in microfluidic devices.Rejection rate in clinical trials can be reduced by organs-on-a-chip drug testing.Less animals are employed by using miniaturized sampling and analytical instruments.Drug discovery and development is a long-lasting process in which many challenges have to be addressed at every stage, from the discovery of the target biomolecule to the commercialization of the discovered drugs and its quality control. From thousands of hits identified during early drug discovery only one drug is eventually efficient and safe enough to be commercialized. This high rejection rate, especially during preclinical and clinical studies have led to an exponential increase of costs to develop new medicines thereby strongly impacting healthcare systems. In this context, miniaturized devices have the potency to significantly reduce the cost and the time needed to develop new therapeutics by streamlining drug development and rejecting drug candidates earlier in the process prior to costly animal and human trials. In this review, we present recent advances involving miniaturized technologies in the field of drug discovery such as target discovery, drug screening, drug synthesis and formulation, in-vitro and in-vivo testing and quality control. We discuss opportunities enabled by miniaturized devices but also their limitations and challenges that need to be resolved in order to spread their use in the pharmaceutical industries.