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A rapid vesicle electrokinetic chromatography method for the assessment of Non-Specific Binding of potential PET ligands in-vitro

Jiang, Zhengjin and Reilly, John and Everatt, Brian and Briard, Emmanuelle (2010) A rapid vesicle electrokinetic chromatography method for the assessment of Non-Specific Binding of potential PET ligands in-vitro. Journal of Pharmaceutical and Biomedical Analysis., 54 (4). pp. 722-729. ISSN 0731-7085

Abstract

High non-specific binding (NSB) is one of the most common reasons for candidate failure in potential Positron Emission Tomography (PET) radiotracer development. It is of interest to develop high throughput in vitro methods for predicting non-specific binding prior to radiolabeling, which would help guide radiotracer candidate selection and assist decision making in new radiotracer discovery.
Results: The AOT vesicle EKC analysis offered the best high throughput approach owing to the short run times, high reproducibility, high selectivity and low sample and solvent cost. It is clearly shown that there is a statistical correlation between the chromatographic retention parameters of tested drugs and their NSB. In brief, the higher the value of log kAOT, the higher the NSB.
Conclusions: The AOT vesicle EKC method can provide NSB in-vitro trend analysis for a large number of drug candidates early in the novel radiotracer discovery process with minimal resources.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
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Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/3492

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