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- W2166796054 abstract "The BB2 receptor subtype, of the bombesin family of receptors, has been shown to be highly overexpressed in a variety of human tumors, including prostate cancer. Bombesin (BBN), a 14-amino acid peptide, has been shown to target the BB2 receptor with high affinity. <sup>64</sup>Cu (half-life = 12.7 h, β<sup>+</sup>: 18%, E<sub>β+max</sub> = 653 keV; β<sup>−</sup>: 37%, E<sub>β−max</sub> = 578 keV) is a radioisotope that has clinical potential for application in both diagnostic imaging and radionuclide therapy. Recently, new chelation systems such as 1,4,8,11-tetraazabicyclo[6.6.2]hexadecane-4,11-diacetic acid (CB-TE2A) have been reported to significantly stabilize the <sup>64</sup>Cu radiometal in vivo. The increased stability of the <sup>64</sup>Cu-CB-TE2A chelate complex has been shown to significantly reduce nontarget retention compared with tetraazamacrocycles such as 1,4,7,10-tetraazacyclodoadecane-<i>N,N′,N″,N‴-</i>tetraacetic acid (DOTA). The aim of this study was to determine whether the CB-TE2A chelation system could significantly improve the in vivo stability of <sup>64</sup>Cu bombesin analogs. The study directly compares <sup>64</sup>Cu bombesin analogs using the CB-TE2A and DOTA chelation systems in a prostate cancer xenograft SCID (severely compromised immunodeficient) mouse model. <b>Methods:</b> The CB-TE2A-8-AOC-BBN(7–14)NH<sub>2</sub> and DOTA-8-AOC-BBN(7–14)NH<sub>2</sub> conjugates were synthesized and radiolabeled with <sup>64</sup>Cu. The receptor-binding affinity and internalization profile of each metallated conjugate was evaluated using PC-3 cells. Pharmacokinetic and small-animal PET/CT studies were performed using female SCID mice bearing PC-3 xenografts. <b>Results:</b> In vivo BB2 receptor targeting was confirmed by tumor uptake values of 6.95 ± 2.27 and 4.95 ± 0.91 %ID/g (percentage injected dose per gram) at the 15-min time point for the <sup>64</sup>Cu-CB-TE2A and <sup>64</sup>Cu-DOTA radioconjugates, respectively. At the 24-h time point, liver uptake was substantially reduced for the <sup>64</sup>Cu-CB-TE2A radioconjugate (0.21 ± 0.06 %ID/g) compared with the <sup>64</sup>Cu-DOTA radioconjugate (7.80 ± 1.51 %ID/g). The <sup>64</sup>Cu-CB-TE2A-8-AOC-BBN(7–14)NH<sub>2</sub> radioconjugate demonstrated significant clearance, 98.60 ± 0.28 %ID, from the mouse at 24 h after injection. In contrast, only 67.84 ± 5.43 %ID of the <sup>64</sup>Cu activity was excreted using the <sup>64</sup>Cu-DOTA-8-AOC-BBN(7–14)NH<sub>2</sub> radioconjugate because of nontarget retention. <b>Conclusion:</b> The pharmacokinetic and small-animal PET/CT studies demonstrate significantly improved nontarget tissue clearance for the <sup>64</sup>Cu-CB-TE2A8-AOC-BBN(7–14)NH<sub>2</sub>. This is attributed to the improved in vivo stability of the <sup>64</sup>Cu-CB-TE2A chelate complex as compared with the <sup>64</sup>Cu-DOTA chelate complex." @default.
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- W2166796054 date "2007-08-01" @default.
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- W2166796054 title "In Vivo Evaluation and Small-Animal PET/CT of a Prostate Cancer Mouse Model Using 64Cu Bombesin Analogs: Side-by-Side Comparison of the CB-TE2A and DOTA Chelation Systems" @default.
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- W2166796054 doi "https://doi.org/10.2967/jnumed.107.039487" @default.
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