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Preparation and bio-distribution of bone tumor therapeutic agent (188)~Re-TCTMP

Jiang Shu

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Abstract

TCTMP (1,4,8,11-tetraaza cyclotetradecyl-1,4,8,11-tetramethylene phosphonate) was synthesized and coupled with 188Re. The 188Re-TCTMP’s coupling condition, stability and bio-distribution in mice were investigated. The results showed that satisfactory yield of 188Re could be obtained under the conditions of media pH=2.0, 0.8~1.6 mg of SnCl2 and 50 mg of ligand. 188Re-TCTMP was stable (complexation yield 95%) in 8 d without pro- tection of N2. The result of bio-distribution indicated that188Re-TCTMP had a strong affinity to skeleton and very low non-target tissue’s uptake, and the amount of 188Re-TCTMP in blood was (0.06±0.02)%ID/g 6 h after injection, whereas the concentration of 188Re-HEDP (1-hydroxy-ethylidene diphosphonate) in blood was (0.28±0.05)%ID/g 6 h after injection. Compared with 188 Re-HEDP, 188Re-TCTMP exhibits better potential for the treatment of metastases.

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What this paper is about

TCTMP (1,4,8,11-tetraaza cyclotetradecyl-1,4,8,11-tetramethylene phosphonate) was synthesized and coupled with 188Re. The 188Re-TCTMP’s coupling condition, stability and bio-distribution in mice were investigated. The results showed that satisfactory yield of 188Re could be obtained under the conditions of media pH=2.0, 0.8~1.6 mg of SnCl2 and 50 mg of ligand. 188Re-TCTMP was stable (complexation yield 95%) in 8 d without pro- tection of N2. The result of bio-distribution indicated that188Re-TCTMP had a strong affinity to skeleton and very low non-target tissue’s uptake, and the amount of 188Re-TCTMP in blood was (0.06±0.02)%ID/g 6 h after injection, whereas the concentration of 188Re-HEDP (1-hydroxy-ethylidene diphosphonate) in blood was (0.28±0.05)%ID/g 6 h after injection. Compared with 188 Re-HEDP, 188Re-TCTMP exhibits better potential for the treatment of metastases.

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Available abstract

TCTMP (1,4,8,11-tetraaza cyclotetradecyl-1,4,8,11-tetramethylene phosphonate) was synthesized and coupled with 188Re. The 188Re-TCTMP’s coupling condition, stability and bio-distribution in mice were investigated. The results showed that satisfactory yield of 188Re could be obtained under the conditions of media pH=2.0, 0.8~1.6 mg of SnCl2 and 50 mg of ligand. 188Re-TCTMP was stable (complexation yield 95%) in 8 d without pro- tection of N2. The result of bio-distribution indicated that188Re-TCTMP had a strong affinity to skeleton and very low non-target tissue’s uptake, and the amount of 188Re-TCTMP in blood was (0.06±0.02)%ID/g 6 h after injection, whereas the concentration of 188Re-HEDP (1-hydroxy-ethylidene diphosphonate) in blood was (0.28±0.05)%ID/g 6 h after injection. Compared with 188 Re-HEDP, 188Re-TCTMP exhibits better potential for the treatment of metastases.

Key concepts: Yield (engineering), Chemistry, Phosphonate, Ligand (biochemistry), Distribution (mathematics), Radiochemistry, Nuclear chemistry, Biochemistry

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