Glycomimetic
drugs have attracted increasing interest as unique
targeting vectors or surrogates for endogenous biomolecules. However,
it is generally difficult to determine the in vivo pharmacokinetic profile of these compounds. In this work, two galectin-3
inhibitors were radiolabeled with fluorine-18 and used as surrogate
PET tracers of TD139 and GB1107. Both compounds are promising drugs
for clinical applications. In vivo evaluation revealed
that both surrogates strongly differed with respect to their biodistribution
profile. The disaccharide (TD139 surrogate) was rapidly eliminated
from blood while the monosaccharide (GB1107 surrogate) showed no sign
of excretion. The data obtained allowed us to infer the different in vivo fate of TD139 and GB1107 and rationalize how different
administration routes could boost efficacy. Whereas the fast excretion
profile of the TD139 surrogate indicated that systemic application
of disaccharides is unfavorable, the extended biological half-life
of the GB1107 surrogate indicated that systemic administration is
possible for monosaccharides.
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