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Lead optimization: delivering molecules fit for preclinical development

A careful lead optimization program is critical if a molecule is to progress successfully through preclinical studies and into clinical development. The initial leads that emerge from a hit-to-lead program, while they may show promising early signs of efficacy, may have features or properties that make them less likely to make a successful medicine.

In a lead optimization program, there is no substitute for experience. Medicinal chemists and other drug discovery specialists who have been working in the field for years are well placed to know what to look for – and what to avoid. Making the best use of the modern tools at their disposal, allied to skills and expertise developed across multiple lead optimization programs in the past, will make success more likely.