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Iodine-129 microdosing for protein and peptide drug development: erythropoietin as a case study

AuthorsLamers, Robert-Jan; Jong, Arie F. M. de; López-Gutiérrez, J. M. ; Gómez-Guzmán, J. M.
Issue Date2013
PublisherFuture Science
CitationBioanalysis 5(1): 53-63 (2013)
Abstract[Background]: Microdosing is a technique for studying the behavior of compounds in vivo at 1/100th of the dose of a test substance calculated, based on animal data, to yield a pharmacologic effect. In microdosing, use is made of accelerator MS (AMS). In this study, we investigated whether 129I-labeling of proteins with subsequent AMS measurements is a suitable method to perform microdose studies with therapeutic proteins. We used erythropoietin (EPO) as a case study. [Results]: In an animal study with 129I-labeled EPO in Han-Wistar rats, an increase of 129I-EPO is observed after dose administration. The half-life was found to be 2 and 5.5 h for two different EPOs. These results are in accordance with expected values. [Conclusion]: Although further research is required, 129I-labeling of proteins seems a feasible method for AMS microdose studies with peptide and protein drugs, such as biosimilars. © 2013 Future Science Ltd.
Identifiersdoi: 10.4155/bio.12.297
issn: 1757-6180
Appears in Collections:(CNA) Artículos
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