前列腺癌具有病程长且呈多阶段渐进发展的特点，其病灶异质性大，易发生淋巴结及骨转移。寻求早期精准检测前列腺癌的方法、开发针对晚期转移患者的新型治疗方法具有十分重要的意义。前列腺特异性膜抗原（prostate-specific membrane antigen，PSMA）在前列腺癌肿瘤细胞高表达，大量靶向PSMA的放射性药物已被开发进入临床使用。[68Ga]Ga-P16-093是一种血液清除快、膀胱背景低、肿瘤摄取高且保留时间长的新型PSMA显像剂，P17-079是拥有P16-093核心结构及膦酸盐双靶向基团的新型双靶点诊疗一体化放射性药物，[177Lu]Lu-P17-087和[177Lu]Lu-P17-088是在P16-093基础上改构的新型PSMA放射性靶向治疗药物。本研究从①“PSMA显像剂[68Ga]Ga-P16-093与骨显像剂[68Ga]Ga-P15-041的头对头比较”、②“新型双靶点显像剂[68Ga]Ga-P17-079的首次人体生物分布及剂量学研究”以及③“[177Lu]Lu-P17-087和[177Lu]Lu-P17-088靶向治疗去势抵抗性前列腺癌的首次人体剂量学研究”三方面入手，开展系列前列腺癌精准诊疗新型放射性药物的初步临床转化研究。结果显示显像剂[68Ga]Ga-P16-093 PET/CT和骨显像剂[68Ga]Ga-P15-041 PET/CT对不同类型的前列腺癌转移灶检出能力有差异，PSMA和双膦酸盐双靶点显像剂[68Ga]Ga-P17-079能够同时检出前列腺癌原发灶、淋巴结转移及骨转移病灶，其在非靶器官的低摄取、在血液中一定的保留能力及较高的肿瘤摄取，具有作为诊疗一体化放射性药物的潜力；[177Lu]Lu-P17-087和[177Lu]Lu-P17-088的药代动力学表现不同，具有良好的PSMA靶向给药效果，二者都具有作为治疗药物的潜力。本研究为初步研究了系列新型放射性药物的体内性质及疾病诊疗效率，为优化前列腺癌的临床诊疗策略、促进前列腺癌精准诊疗技术的进一步发展奠定基础。

Prostate cancer has the characteristics of long course and multi-stage progressive development, the heterogeneity of the lesions is large, and the lymph node and bone metastasis are easy to occur. It is of great significance to seek for early and accurate detection of prostate cancer and to develop new therapeutic methods for patients with advanced metastasis. Prostate-specific membrane antigen (PSMA) is highly expressed in prostate cancer tumor cells, and a large number of radiopharmaceutics targeting PSMA have been developed for clinical use. [68Ga]Ga-P16-093 is a novel PSMA imaging agent with rapid blood clearance, low bladder background, high tumor uptake and long retention time, and P17-079 is a novel dual-target integrated radiopharmaceutics for diagnosis and treatment with P16-093 core structure and phosphonate double-targeted groups. [177Lu]Lu-P17-087 and [177Lu]Lu-P17-088 are novel radio-targeted therapies for PSMA modified from P16-093. This study includes: (1) "Head-to-head comparison of PSMA imaging agent [68Ga]Ga-P16-093 and bone imaging agent [68Ga]Ga-P15-041", (2) "First human biodistribution and dosimetry study of a novel dual-target imaging agent [68Ga]Ga-P17-079" and (3) "[177Lu]Lu-P17-08. 7 and the First human dosimetry Study of [177Lu]Lu-P17-088 Targeted Therapy for castration-resistant prostate cancer "three aspects, to carry out a series of preliminary clinical transformation of new radiopharmaceutical precision diagnosis and treatment of prostate cancer. The results showed that the detection ability of [68Ga]Ga-P16-093 PET/CT and [68Ga]Ga-P15-041 PET/CT for different types of prostate cancer metastases was different. PSMA and bisphosphonate dual-target imaging agent [68Ga]Ga-P17-079 can simultaneously detect the primary focus of prostate cancer, lymph node metastasis and bone metastasis, and its low uptake in non-target organs, certain retention ability in blood and high tumor uptake have the potential to be used as theranostics agent for diagnosis and treatment. The pharmacokinetics of [177Lu]Lu-P17-087 and [177Lu]Lu-P17-088 are different, and they have good PSMA targeted drug delivery effect, and both of them have potential as therapeutic drugs. This study is a preliminary study of the in vivo properties and disease diagnosis and treatment efficiency of a series of novel radiopharmaceuticals, which lays a foundation for optimizing the clinical diagnosis and treatment strategy of prostate cancer and promoting the further development of precision diagnosis and treatment technology for prostate cancer.