PMID: 8961801Sep 1, 1996Paper

Small peptides radiolabeled with 99mTc

The Quarterly Journal of Nuclear Medicine : Official Publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology (IAR)
J Lister-JamesT Dean

Abstract

The pharmacokinetic characteristics of small peptides radiolabeled with technetium-99m, their physico-chemical properties and radiolabeling techniques are reviewed. Physical and chemical characteristics which affect pharmacokinetics are discussed with particular reference to lipophilicity, charge and resistance to peptidases. General biodistribution, pharmacokinetics, metabolism and excretion characteristics, as well as tissue uptake kinetics are described. Methods of radiolabeling small peptides with 99mTc are reviewed, including discussion of chelating groups for technetium. Specific examples drawn either from the literature or from the 99mTc labeled peptides under development by Diatide are presented. Although lipophilicity and charge have an impact, the degree of resistance to peptidases is a key determinant of pharmacokinetic behavior. In general, pharmacokinetics and rate of tissue uptake are fast and metabolism occurs mainly via peptidase activity in the liver and kidneys. Although the route depends on a number of factors, excretion also usually is rapid. Chelating groups for 99mTc in the (+5) oxidation state are preferred. Site specific incorporation of the chelating groups during peptide synthesis is also preferred. Ex...Continue Reading

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