Selected Characteristics of Radiohalogenated PSMA-Targeted Agents
| Full chemical name | Abbreviation used in this article | Ki for PSMA (nM) | IC50 for PSMA (nM) | Imaging or therapy | Current status |
| N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-S-3-125I-iodo-l-tyrosine (35) | 125I-DCIT | 1.5 | Imaging | Early preclinical agent | |
| N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-4-18F-fluorobenzyl-l-cysteine (38) | 18F-DCFBC | 13.9 | Imaging | Currently under investigation in clinical trials | |
| 2-(3-(1-Carboxy-5-[(6-18F-fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-pentanedioic acid (42) | 18F-DCFPyL | 1.1 | Imaging | Currently under investigation in clinical trials | |
| (2R,4S)-2-18F-fluoro-4-phosphonomethyl-pentanedioic acid (43) | BAY 1075553 | 1.4 (major stereoisomer) | Imaging | Currently under investigation in clinical trials | |
| 4-Bromo-2-18F-fluorobenzoyllysineoxypentanedioic acid (30) | 4-Bromo-2-18F-fluorobenzoyllysine OPA | 0.11 | Imaging | Undergoing preclinical development | |
| 4-Iodo-2-18F-fluorobenzoyllysineoxypentanedioic acid (30) | 4-Iodo-2-18F-fluorobenzoyllysine OPA | 0.21 | Imaging | Undergoing preclinical development | |
| (S)-2-(3-((S)-1-carboxy-5-(3-(4-123I/131I-iodophenyl)ureido)pentyl)ureido)pentanedioic acid (52) | MIP-1095 | 0.24 | Imaging and therapy | Currently under investigation in clinical trials | |
| 2-[3-[1-Carboxy-5-(4-125I-iodo-benzoylamino)-pentyl]-ureido]-pentanedioic acid (56) | 125I-DCIBzL | 0.01 | Therapy | Undergoing preclinical development | |
| (2S)-2-(3-(1-carboxy-5-(4-211At-astato-benzamido)pentyl)ureido)-pentanedioic acid (58) | 211At-DCAtBzL | Not reported | Not reported | Therapy | Undergoing preclinical development |
Ki = dissociation constant; IC50 = 50% maximal inhibitory concentration.