The DOI matches its Crossref record; 104 of the 104 references it cites were found in a registry or an index.
Long‐lasting target binding and rebinding as mechanisms to prolong in vivo drug action
Open accessAbstract
An increasing number of examples in the literature suggest that the in vivo duration of drug action not only depends on macroscopic pharmacokinetic properties like plasma half‐life and the time needed to equilibrate between the plasma and the effect compartments, but is also influenced by long‐lasting target binding and rebinding. The present review combines information from different research areas and simulations to explore the nature of these mechanisms and the conditions in which they are most prevalent. Simulations reveal that these latter phenomena become especially influential when there is no longer sufficient free drug around to maintain high levels of receptor occupancy. There is not always a direct link between slow dissociation and long‐lasting in vivo target protection, as the rate of free drug elimination from the effect compartment is also a key influencing factor. Local phenomena that hinder the diffusion of free drug molecules away from their target may allow them to consecutively bind to the same target and/or targets nearby (denoted as ‘rebinding’) even when their concentration in the bulk phase has already dropped to insignificant levels. The micro‐anatomic properties of many effect compartments are likely to intensify this phenomenon. By mimicking the complexity of tissues, intact cells offer the opportunity to investigate both mechanisms under the same, physiologically relevant conditions.
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Cited by
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Copeland, R. A. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2015.18 · Cited by 722
Inhaled Therapy in Respiratory Disease: The Complex Interplay of Pulmonary Kinetic Processes
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Drug–Target Kinetics in Drug Discovery
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Self-citation
Metadata
- Authors
- Vauquelin, G., & Charlton, S. J.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2010-09-03
- Volume
- 161
- Issue
- 3
- Pages
- 488-508
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W1501203786
- Cited by
- 298
- References
- 104
- FWCI
- 5.08
- Type
- journal article
- Language
- en
- Open access
- green
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
