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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

CNS Drug Development – Lost in Translation?

Author(s): A. Talevi, C. L. Bellera, M. Di Ianni, M. Gantner, L. E. Bruno-Blanch and . A. Castro

Volume 12 , Issue 10 , 2012

Page: [959 - 970] Pages: 12

DOI: 10.2174/138955712802762356

Price: $65


CNS drug development is characterized by an especially high attrition rate, despite clear unmet medical needs in the field of neuro-pharmacology and significant investment in R&D of novel CNS drug treatments. Here, we overview the issues underlying the intrinsic difficulty of CNS drugs development, including obstacles of pharmacokinetic nature and lack of predictivity of preclinical tests. We highlight current efforts to overcome these limitations, with an emphasis on modeling opportunities towards early recognition of CNS candidates (stressing the possibilities of multi-target directed ligands or “magic shotguns”) and different approaches to improve CNS bioavailability.

Keywords: ADMET models, biomarkers, CNS drugs, in vitro models, in silico models, multi-target directed ligands.

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