A PSMA-targeted peptide derivative for radiotherapy, which is a novel structural molecule developed for diagnosis or treatment of prostate cancer, and prostate-specific membrane antigen (PSMA) is a protein present on the surface of healthy prostate cells, which is often at a high level of expression on the surface of prostate cancer cells, and the molecular composition of PSMA inhibitor is mainly composed of glutamic acid, urea and lysine, in addition to the linker of the present invention, PSMA inhibitor can be combined with a chelating agent and truncated Evans Blue, which can be labeled with radionuclides Ga-67, Ga-68, In-111, Lu-177, Cu-64 and Y-90, used for image analysis and analysis of human prostate cancer tumor pattern as a new PSMA-targeted peptide receptor radionuclide therapy (PRRT), and which has a longer half-life in vivo and is featured by specific binding of prostate-specific membrane antigens for radiotherapy diagnosis or treatment.一種PSMA靶向放射性診療之胜肽衍生物，係為應用於前列腺癌診斷或治療藥物所開發的新型結構分子；前列腺特異性膜抗原（PSMA）是一種存在於健康前列腺細胞表面的蛋白，其往往在前列腺癌細胞表面處於較高的表達水準，該PSMA抑制劑主要是由麩氨酸、尿素及離氨酸三個分子組成，加上本發明連接基後可與螯合劑及截斷的伊文思藍 (truncated Evans Blue) 結合，該螯合劑可標誌放射性核種Ga-67、Ga-68、In-111、Lu-177、Cu-64、Y-90，用以進行人類前列腺癌腫瘤模式影像分析評估，並作為前列腺癌疾病之新標靶胜肽受體放射治療藥物 (peptide receptor radionuclide therapy，PRRT)，其具有生物體內長半衰期，且針對前列腺特異性膜抗原之專一性結合與放射性治療診斷等特點。
