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Balanced Permeability Index: A Multiparameter Index for Improved In Vitro Permeability.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2024 Mar 19; Vol. 15 (4), pp. 457-462. Date of Electronic Publication: 2024 Mar 19 (Print Publication: 2024). - Publication Year :
- 2024
-
Abstract
- The optimization of passive permeability is a key objective for orally available small molecule drug candidates. For drugs targeting the central nervous system (CNS), minimizing P-gp-mediated efflux is an additional important target for optimization. The physicochemical properties most strongly associated with high passive permeability and lower P-gp efflux are size, polarity, and lipophilicity. In this study, a new metric called the Balanced Permeability Index (BPI) was developed that combines these three properties. The BPI was found to be more effective than any single property in classifying molecules based on their permeability and efflux across a diverse range of chemicals and assays. BPI is easy to understand, allowing researchers to make decisions about which properties to prioritize during the drug development process.<br />Competing Interests: The authors declare no competing financial interest.<br /> (© 2024 American Chemical Society.)
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 15
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 38628792
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.3c00542