The present disclosure relates to gastrin-releasing peptide receptor (GRPR) targeting radiopharmaceuticals and uses thereof. In particular, the present disclosure relates to a pharmaceutical composition comprising radiolabeled GRPR-antagonist and a surfactant. The present disclosure also relates to radiolabeled GRPR-antagonist for use in treating or preventing a cancer.本發明係關於標靶胃泌素釋放肽受體(gastrin-releasing peptide receptor;GRPR)的放射性藥物及其用途。特定言之,本發明係關於一種醫藥組合物,其包含放射性標記GRPR拮抗劑及界面活性劑。本發明亦關於放射性標記GRPR拮抗劑,其用於治療或預防癌症。