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BZM055, a SPECT tracer candidate for studying FTY720 brain distribution and myelin imaging

Orain, David and Beerli, Christian and Billich, Andreas and Streiff, Markus and Bigaud, Marc and Auberson, Yves and Briard, Emmanuelle (2011) BZM055, a SPECT tracer candidate for studying FTY720 brain distribution and myelin imaging. ChemMedChem, 6 (4). pp. 667-677.

Abstract

FTY720 (fingolimod, Gilenya®) is a sphingosine 1-phosphate (S1P) receptor modulator that showed significant therapeutic efficacy after oral administration to multiple sclerosis patients. We propose here an imaging tracer to study the pharmacokinetics and organ distribution of FTY720 in patients and, since this drug accumulates in myelin sheaths, for myelin imaging.
FTY720 does not contain any atom whose PET or SPECT radioisotope would have a half-life compatible with its pharmacokinetic properties. We hence searched for a radiolabeled derivative that would be an adequate surrogate of the drug, mimicking its pharmacokinetics and organ distribution, but also its affinity, selectivity for S1P receptors, phosphorylation kinetics, and overall physicochemical properties. We selected a close mimic of the drug, BZM055 (2a), for radiolabeling and further characterization

Item Type: Article
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Keywords: SPECT, myelin, imaging agents, iodine
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Date Deposited: 26 Apr 2016 23:46
Last Modified: 26 Apr 2016 23:46
URI: https://oak.novartis.com/id/eprint/3985

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