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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