Preclinical lead optimization Preparative

The principal issue in the drug discovery process is the high failure rate in the clinical trials, mainly due to liabilities related to poor pharmacokinetics (PK), poor efficacy, and high toxicity. The earlier lead optimization (LO) phase then represents a crucial step in the drug discovery process, since it involves the preparation and the selection of suitable drug candidates. In view of the increasing need for speed in the preclinical research and development, the determination of activity and selectivity is performed simultaneously with the evaluation of pharmacokinetic and toxicity properties. This multiparametric approach allows the early selection of the compounds with the best overall balanced druglike profile [1]. 

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