PMID: 9428603Jan 15, 1998Paper

Synthesis, biodistribution and renal handling of various chelate-somatostatin conjugates with metabolizable linking groups

Nuclear Medicine and Biology
P M Smith-JonesC Bruns

Abstract

A series of DTPA-octreotide conjugates, with various linking groups, were synthesised to investigate the effect of different metabolizable linkers on the renal retention of radioactivity. All these newly synthesised octreotide conjugates retained the high binding affinity of octreotide for the somatostatin (SRIF) receptors either when unlabeled or radiolabeled with 111In. Some of the metabolizable linkers were rapidly degraded in vitro when incubated with a kidney homogenate. However, in vivo, all these conjugates displayed a significantly lower uptake in SRIF receptor-positive tissue compared to two conjugates with short, stable linkers. Additionally, the compounds with a potentially metabolizable linker had a higher whole-body retention of activity as opposed to the three metabolically stable compounds. Several of the linkers gave evidence of cleavage while in circulation in the blood, and it is probable that the lower tumour accumulation of most of the compounds tested was low due to the high enzymatic nature of the exocrine pancreatic tumour model used. In short, no increase in the tumour-to-kidney ratio was achieved with the analogues containing a metabolizable linker. The highest target-to-nontarget tissue ratios were obt...Continue Reading

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Citations

Oct 18, 2002·Biopolymers·Sylvie Froidevaux, Alex N Eberle
Apr 27, 2001·Nuclear Medicine and Biology·J E BugajA Srinivasan
Jan 27, 2004·Nuclear Medicine and Biology·Qin WangWalter Mier
May 30, 2008·Advanced Drug Delivery Reviews·Hiromichi AkizawaYasushi Arano
Jan 15, 2005·Journal of Receptor and Signal Transduction Research·Alex N EberleSylvie Froidevaux
Jun 13, 2009·Journal of Receptor and Signal Transduction Research·Alex N Eberle, Gabriele Mild
Dec 22, 2007·Journal of Receptor and Signal Transduction Research·Jean-Philippe BapstAlex N Eberle
Dec 26, 2001·Chemical Reviews·S Liu, D S Edwards
Jun 18, 2010·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Erik VegtOtto C Boerman

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