Table 1.
Representative examples of radiolabeled PSMA inhibitors used for TAT of mCRPCa in preclinical and clinical settings
| Radioisotope | Radiolabeled agent used | Type of study (Preclinical/clinical) | Prostate cancer type | Treatment response | Reference |
|---|---|---|---|---|---|
| 211At | (2S)-2-(3-(1-carboxy-5-(4-211At-astatobenzamido) pentyl)ureido)-pentanedioic acid | Preclinical | (PSMA+) PC3 PIP xenograft | Caused significant delay in tumor growth. | [127] |
| 225Ac | 225Ac-PSMA-617 | Clinical | mCRPCa | Experienced PSA decline to below the measurable level and showed complete response on PET imaging. | [96] |
| 213Bi | 213Bi-PSMA I&T | Preclinical | PSMA+ LNCaP xenografts | Caused DNA double strand breaks in tumors. | [132] |
| 213Bi | 213Bi-PSMA-617 | Clinical | mCRPCa | Experienced decrease in PSA level from 237 μg/L to 43 μg/L and showed complete response on PET imaging. | [133] |