Compound high-quality criteria: a new vision to guide the development of drugs, current situation

Mignani, Serge; Huber, Scot; Tomás, Helena; Rodrigues, João; Majoral, Jean-Pierre

http://hdl.handle.net/10400.13/2428

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Abstract(s)

For several decades, the pharmaceutical industry has suffered due to major issues such as reductions of the number of FDA approved drugs and biologics. Several analyses have been highlighted that the 'druglikeness' is one of the strategies to improve succeed rates of screening such as, for instance, high-throughput screening (HTS), and then hits (as starting point), leads and clinical candidates. It is clear that the improvement of compound quality accelerates the drug discovery projects. The monitoring of several indices to avoid 'molecular obesity' (ADMET problems) of final drugs from good-quality 'low-fat' starting points represents today a powerful strategy of optimization process. The development of the new guides to find drugs highlighting attempts at improving the attrition rate from hits to final medicines by focusing on how to improve the druggability of hits, leads and drugs during the drug discovery process represents a key approach to design next better generation of medicines.

Keywords

Drug industry Development of drugs Drug discovery . Faculdade de Ciências Exatas e da Engenharia Centro de Química da Madeira

URI

http://hdl.handle.net/10400.13/2428

Citation

Mignani, S., Huber, S., Tomas, H., Rodrigues, J., & Majoral, J. P. (2016). Compound high-quality criteria: a new vision to guide the development of drugs, current situation. Drug Discovery Today, 21(4), 573-584.