Abstract
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.
Mini-Reviews in Medicinal Chemistry
Title:CNS Drug Development – Lost in Translation?
Volume: 12 Issue: 10
Author(s): A. Talevi, C. L. Bellera, M. Di Ianni, M. Gantner, L. E. Bruno-Blanch and . A. Castro
Affiliation:
Keywords: ADMET models, biomarkers, CNS drugs, in vitro models, in silico models, multi-target directed ligands.
Abstract: 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.
Export Options
About this article
Cite this article as:
Talevi A., Bellera L. C., Ianni Di M., Gantner M., Bruno-Blanch E. L. and Castro A. ., CNS Drug Development – Lost in Translation?, Mini-Reviews in Medicinal Chemistry 2012; 12(10) . https://dx.doi.org/10.2174/138955712802762356
DOI https://dx.doi.org/10.2174/138955712802762356 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |

- Author Guidelines
- Editorial Policies
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Allegations from Whistleblowers
- Publishing Ethics and Rectitude
- Increase Visibility Of Your Article
- Archiving Policies
- Reviewer Guidelines
- Guest Editor Guidelines
- Board Recruitment Workflow
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Announcements
- Forthcoming Thematic Issues
Related Articles
-
Zinc and its Specific Transporters as Potential Targets in Airway Disease
Current Drug Targets Is Src a Viable Target for Treating Solid Tumours?
Current Cancer Drug Targets Can Breast Cancer Stem Cells Evade the Immune System?
Current Medicinal Chemistry Monoclonal Antibodies as a Tool for Structure-Function Studies of the MDR1-P-Glycoprotein
Current Protein & Peptide Science Trends and Applications of Brain Computer Interfaces
Current Signal Transduction Therapy Evaluation of Local Injection of Bevacizumab against Triple-Negative Breast Cancer Xenograft Tumors
Current Pharmaceutical Design Potential Use of Nanomedicine for Drug Delivery Across the Blood-Brain Barrier in Healthy and Diseased Brain
CNS & Neurological Disorders - Drug Targets Mitochondrial Dysfunction and Lipid Homeostasis
Current Drug Metabolism A Small-molecule Inhibitor, 5'-O-Tritylthymidine, Targets FAK and Mdm-2 Interaction, and Blocks Breast and Colon Tumorigenesis in vivo
Anti-Cancer Agents in Medicinal Chemistry Photo- and Sono-Dynamic Therapy: A Review of Mechanisms and Considerations for Pharmacological Agents Used in Therapy Incorporating Light and Sound
Current Pharmaceutical Design Blockade of Insulin-Like Growth Factor Type-1 Receptor with Cixutumumab (IMC-A12): A Novel Approach to Treatment for Multiple Cancers
Current Drug Targets Zinc Dependent Histone Deacetylase Inhibitors in Cancer Therapeutics: Recent Update
Current Medicinal Chemistry Perspective of Molecular Hydrogen in the Treatment of Sepsis
Current Pharmaceutical Design Peptides for In Vivo Target-Specific Cancer Imaging
Mini-Reviews in Medicinal Chemistry Menopause, A Universal Female Experience: Lessons from Mexico and Central America
Current Women`s Health Reviews Transcriptional Analysis of JAK/STAT Signaling in Glioblastoma Multiforme
Current Pharmacogenomics and Personalized Medicine Cathepsin D as a Promising Target for the Discovery of Novel Anticancer Agents
Current Cancer Drug Targets Synthesis, <i>In Silico</i> and <i>In Vivo</i> Evaluation of Novel 1, 3, 4-Thiadiazole Analogues as Novel Anticancer Agents
Letters in Drug Design & Discovery Reactive Oxygen Production Induced by the Gut Microbiota: Pharmacotherapeutic Implications
Current Medicinal Chemistry Drug-induced Cholelithiasis
Current Reviews in Clinical and Experimental Pharmacology