One-step labelling of a novel small-molecule peptide with astatine-211: preliminary evaluation in vitro and in vivo

In this paper, VP2, a novel small molecule fusion peptide, was labelled with 211At through a one-step method (coupled with bifunctional intermediate SPC first and then labelled) with a radiochemical yield of about 45%. The radiochemical purity was still > 95% after 24 h at room temperature. Specificity studies in vitro indicated that 211At-SPC-VP2 has a high affinity for several tumour cells. Additionally, biodistribution in KM mice showed that 211At-SPC-VP2 has sufficient stability in vivo. This research suggested that 211At–SPC-VP2 produced by the convenient method has the potential to be a novel targeted drug for cancer radiotherapy.