Article Figures & Data
Figures
- FIGURE 1.
Chemical structures of small-molecule inhibitors of PSMA.
- FIGURE 2.
Predominantly lytic bone metastasis (arrow) (A) that was occult on 68Ga-PSMA PET (B) and PET/CT (C) but readily apparent on 18F-DCFPyL PET (D) and PET/CT (E).
- FIGURE 3.
Detection of wide variety of PC lesions with 18F-DCFPyL. Locally recurrent PC (CT [A] and 18F-DCFPyL PET/CT [B]) and lymph node (CT [C] and 18F-DCFPyL PET/CT [D]) and bone (CT [E] and 18F-DCFPyL PET/CT [F]) lesions were visible as marked focal radiotracer uptake (arrows).
- FIGURE 4.
Auger electron–emitting (125I-DCIBzL) and α-particle–emitting (211At-DCAtBzL) radiohalogenated small-molecule inhibitors of PSMA.
Tables
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.
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