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J Nucl Med. 2008; 49 (Supplement 1):315P
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Oncology-Basic Science: Basic Science

Basic Science Posters

Study on pharmacokinetics and acute toxicity of 99mTc-radiolabeled antisense probe targeting hTERT mRNA

Rong Fu Wang1, Meng Liu1, Chun Li Zhang1, Ping Yan1, Ming Ming Yu1 and Yong Gang Cui1

1 Nuclear Medicine, Beijing University 1st Hospital, Beijing, China

1340

Objectives: The aim of this report is to study the pharmacokinetics and acute toxicity of 99mTc-radiolabeled antisense probe targeting hTERT mRNA.

Methods: One 18mer uniformly phosphorothioate-modified antisense oligonucleotide targeting hTERT mRNA was radiolabeled with 99mTc through bifunctional chelator. Biodistribution of 99mTc-hTERT ASON in KM mice was obtained. The compartment model and pharmacokinetics parameters of 99mTc-hTERT ASON in experimental rabbits were dealt with pharmacokinetics software DAS 2.0.1. The acute toxicity test was performed in KM mice according to the instruction of "Chinese Pharmacopoeia".

Results: The labeling efficiencies of 99mTc-hTERT ASON reached 76%±5%, the specific activity was up to 1850KBq/µg, and the radiochemical purity was above 96%. The biodistribution of 99mTc-hTERT ASON was characterized by quick blood clearance. It accumulated mainly in small intestine, liver, kidney and bladder. Radioactivity counts per minute(CPM) versus time profiles for 99mTc-hTERT ASON were biphasic, indicative of a three-compartment model. The pharmacokinetics parameters of half-life of distribution(T1/2{alpha}), half-life of elimination(T1/2β), total apparent volume of distribution(Vd) and total rate of clearance (CL) were 2.04min, 74.94min, 969.66ml, 28.85ml/min respectively. All KM mice were present well after injection of high dose of 99mTc-hTERT ASON, and no mice was dead during the period of 48hr.

Conclusions: These results demonstrate widespread tissue availability of 99mTc-hTERT ASON and suggest its development as a potential molecular imaging agent.

Research Support: The study was supported by National Natural Science Foundation of China (NSFC 30470498 and 30670583), National Basic Research Program (973 Program, 2006CB705705-1) and the second phase of National Education Ministry "985" Project (985-2-056).





This Article
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Right arrow Alert me to new issues of the journal
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Google Scholar
Right arrow Articles by Wang, R. F.
Right arrow Articles by Cui, Y. G.
PubMed
Right arrow Articles by Wang, R. F.
Right arrow Articles by Cui, Y. G.