放射性核素标记前列腺特异性膜抗原小分子抑制剂靶向前列腺癌的显像与治疗

Targeted imaging and therapy of prostate cancer by radionuclide labeled small molecule inhibitors of prostate specific membrane antigen

前列腺特异性膜抗原（PSMA）在大多数前列腺癌（PCa）病灶中过表达，在PCa的早期诊断、术前分期、治疗指导、复发和转移的探查以及靶向治疗中具有重要的临床价值。放射性核素（尤其68Ga与177Lu）标记的多种PSMA小分子抑制剂在PCa SPECT和PET显像中的应用得到了临床的广泛关注，同时也在转移性去势抵抗性前列腺癌（mCRPC）的治疗中发挥了重要的作用。该文总结了相关研究进展。

Prostate specific membrane antigen （PSMA） overexpresses in most prostate cancer （PCa） lesions and plays an important role in the early diagnosis and preoperative staging, clinical decision making, recurrence and metastasis detection as well as targeted therapy. Radionuclide （especially 68Ga and 177Lu） labeled multiple small molecule inhibitors of PSMA have been wildly used in SPECT, PET imaging on PCa, and play an important role in the treatment of metastatic castration resistant prostate cancer （mCRPC）. This review summarizes the development in these fields.