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Table 1 uPAR targeting imaging agents

From: Molecular imaging of the urokinase plasminogen activator receptor: opportunities beyond cancer

Agent Classification Targeting epitope Imaging modality Imaging window Notes Translation stage Ref
Cy5.5-mATF-IO ATF-based NP uPA-binding region MRI, optical 24-48 h Mouse ATF In vivo preclinical [198, 199]
hATF-Cy5.5-IO-Nos ATF-based NP uPA-binding region MRI, optical n.v.t. Human ATF In vitro preclinical [200]
ATF-I125 ATF-based uPA-binding region n.a. n.v.t.   In vitro preclinical [201]
NIR-830-mATF-IONP ATF-based NP uPA-binding region PA, optical 24 h Mouse ATF In vivo preclinical [202]
ATF-IONP-Gem ATF-based NP uPA-binding region MRI 48 h Mouse and human ATF In vivo preclinical [203]
NIR-830-hATF-IONP ATF-based NP uPA-binding region Optical 24 h Human ATF In vivo preclinical [204]
NAc-dD-CHA-F-dS-dR-Y-L-W-S-βAla)2-K-K(DOTA)-NH2-111In Peptide uPA-binding region n.a. n.v.t.   In vitro preclinical [201]
99mTc-Hynic-PEG-AE105 Peptide uPA-binding region SPECT 4-6 h   In vivo preclinical [205]
64Cu-DOTA-AE105 Peptide uPA-binding region PET 24 h   Phase I clinical [13, 219,220,221,222, 224]
68Ga-NOTA-AE105 Peptide uPA-binding region PET 10 min-1 h   Phase I clinical [14, 206]
ICG-Glu-Glu-AE105 Peptide uPA-binding region Optical 6-24 h   In vivo preclinical [207,208,209]
CH1055-4Glu-AE105 Peptide uPA-binding region Optical 72-96 h   In vivo preclinical [210]
AF680-2G10 Antibody uPA-binding region Optical 48-96 h Recombinant antibody with trastuzumab Fc region In vivo preclinical [211, 212]
111ln-2G10 Antibody uPA-binding region SPECT 48-120 h Recombinant antibody with trastuzumab Fc region In vivo preclinical [211, 212]
AF680-3C6 Antibody β1-binding region Optical 48-96 h Recombinant antibody with trastuzumab Fc region In vivo preclinical [211]
111ln-3C6 Antibody β1-binding region SPECT 48-96 h Recombinant antibody with trastuzumab Fc region In vivo preclinical [211]
111In-ZW800-1-ATN-658 (Hybrid ATN-658) Antibody Domain 3, amino acids 268-275 Optical, SPECT 24-72 h Mouse antibody In vivo preclinical [213, 214]
  1. NP nanoparticle, MRI magnetic resonance imaging, PET positron emission tomography, SPECT single photon-emission computed tomography, h hours, min minute, n.a. not applicable, ATF amino-terminal fragment