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. 2019 May 14;10:510. doi: 10.3389/fphar.2019.00510

Table 1.

Comprehensive overview of potential targeted “always-on” FIGS tracers.

Tracer type Compound name Molecular target Imaging target Reporter fluorophore(s) References Remarks
Antibodies/Antibody fragments Antibody Girentuximab CAIX Renal cancerC, Ev IRDye800CW Hekman et al., 2016, 2018 Multimodal, Clinical trial
MabCAIX Breast cancerO IRDye800CW Van Brussel et al., 2013
YY146 CD146 Hepatocellular cancerS, O ZW800-1 Hernandez et al., 2016 Multimodal
BIWA CD44v6 Head and Neck cancerO IRDye800CW Odenthal et al., 2018 Multimodal
MN-14 CEA Colorectal cancerS, Ip IRDye800CW Rijpkema et al., 2014 Multimodal
SGM-ch511 (SGM-101) Colorectal cancerC, O, Ip, M, Pancreatic cancerC, O BM104 Gutowski et al., 2017; Boogerd et al., 2018; Hoogstins et al., 2018 Clinical trial
Labetuzumab Colorectal cancerS, O IRDye800CW Hekman et al., 2017 Multimodal
hM5A Pancreatic cancerS, O, Pdx IRDye800CW Lwin et al., 2018b,c
Cetuximab EGFR Breast cancerS, Head and Neck cancerC, S, O, Pancreatic cancerC, FibrosarcomaS IRDye800CW Day et al., 2013b; Korb et al., 2014; De Boer et al., 2015; Warram et al., 2015, 2016; Rosenthal et al., 2016, 2017; Moore et al., 2017; Gao et al., 2018a; Prince et al., 2018; Tummers et al., 2018b Clinical trial
Panitumumab Breast cancerS, Colorectal cancerS, Head and Neck cancerC, O, gliomaS, O, Skin cancerS, O IRDye800CW, FNIR-Z-759 (Heath et al., 2012; Day et al., 2013a,b; Gong et al., 2014; Korb et al., 2014; Sato et al., 2016a,b; Gao et al., 2018a,b; Marston et al., 2019; van Keulen et al., 2019) Clinical trial
mAb 7.4 EpCAM Prostate cancerO IRDye800CW Zhu et al., 2013
323/A3 Colorectal cancerO, Breast cancerO, Ip, Head and Neck cancerO IRDye800CW van Driel et al., 2016
Trastuzumab HER2 Breast cancerS, Gastric cancerIp, Ovarian cancerS IRDye800CW Terwisscha van Scheltinga et al., 2011; Korb et al., 2014
Tocilizumab IL-10 Breast cancer, MelanomaS, M IRDye800CW Day et al., 2013a; Korb et al., 2014
mAb62 Kv10.1 MelanomaS Cy5.5 Napp et al., 2016
D2B PSMA Prostate cancerS, Colorectal cancerM IRDye800CW Lütje et al., 2014a Multimodal
Bevacizumab VEGF-A Breast cancerC, S, Colorectal cancerC, Gastric cancer, Ovarian cancerS, Skin cancerS, O IRDye800CW Terwisscha van Scheltinga et al., 2011; Day et al., 2013a; Korb et al., 2014; Harlaar et al., 2016; Lamberts et al., 2017 Clinical trial
DC101 VEGFR-2 FibrosarcomaS IRDye800CW Prince et al., 2018
ATN-658 uPAR Colorectal cancerS, O, Head and Neck cancerO ZW800-1 Boonstra et al., 2015c, 2017 Multimodal
(Fab)2 TRC-105 & ALT-836 heterodimer CD105/TF Pancreatic cancerS ZW800-1 Luo et al., 2017
Minibody A11 (c)Mb PSCA Prostate cancerS, O, M, Im Cy5.5, IRDye800CW Tsai et al., 2018; Zhang et al., 2018 Multimodal
Diabody anti-HER3 diabody HER3 Pharyngeal cancerS IRDye800CW Alam et al., 2018
A2cDb PSCA Prostate cancerS, Pancreatic cancerPdx Cy5, IRDye800CW Sonn et al., 2016; Zettlitz et al., 2018, 2019 Multimodal
Fab anti-CEA CEA Colorectal cancerS Dy676 Lisy et al., 2008
VB5-845d EpCAM Colorectal cancerS, Breast cancerO IRDye800CW Boogerd et al., 2019
ScFv ssSM3E CEA Colorectal cancerS, O, Pancreatic cancerO IRDye800CW Boonstra et al., 2015b
ScFvEGFR EGFR Breast cancerO IRDye800CW Yang et al., 2014
scFvD2B PSMA Prostate cancerO XenoLight 770CF Mazzocco et al., 2016
3E8.scFv.Cys TAG-72 Colorectal cancerO IRDye800CW Gong et al., 2018
Nanobody B9 CAIX Breast cancerO IRDye800CW Kijanka et al., 2016
7D12, 7D12-9G6 EGFR Head & Neck cancerO IRDye800CW Van Driel et al., 2014
2Rs15d HER2 Ovarian cancerS, Ip IRDye800CW, IRDye680RD Debie et al., 2017, 2018
11A1 Breast cancerS IRdye800CW Kijanka et al., 2013, 2016
Protein Scaffolds Centyrin 83v2Cys EGFR Lung cancerS S0456 Mahalingam et al., 2017
Affibody Z03115-Cys EGFR GliomaO IRDye800CW Sexton et al., 2013; de Souza et al., 2017; Ribeiro de Souza et al., 2018
ZEGFR:1907 Skin cancerS Cy5.5, AF680, IRDye800CW Miao et al., 2011; Qi et al., 2012
ZHER2 HER2 Breast cancerS DyLight-750 Zielinski et al., 2012
Cystine knottin R01-MG Integrin αvβ6 Pancreatic cancerS, O, Tg IRDye800CW Tummers et al., 2018a
Chlorotoxin ANXA2, MMP-2 Breast cancerC, GliomaS, O, Head and Neck cancerO, Spontaneous canine tumors ICG, Cy5.5 Veiseh et al., 2007; Butte et al., 2014; Kittle et al., 2014; Fidel et al., 2015; Baik et al., 2016; Dintzis et al., 2018 Clinical trial
Peptides cRGD Integrins αvβ3, αvβ5 and αvβ6 Breast cancerO, Colorectal cancerS, O, Gastric cancerS, Ip, GliomaS, O, Head and Neck cancerO, Lung cancerM, Skin cancerS, Pancreatic cancerO ICG, Cy5, Cy5.5, ZW800-1, IRDye800CW, CH1055* Huang et al., 2012; Choi et al., 2013; Verbeek et al., 2014; Cheng et al., 2016; Handgraaf et al., 2017; Liu et al., 2018; Sun et al., 2018 *NIR-II, Multimodal
NGR CD13 GliomaS, O, fibrosarcomaS Cy5.5 Li et al., 2014; Liu et al., 2018
Ac-TZ14011 CXCR4 Breast cancerS CyAL-5.5b Kuil et al., 2011; Buckle et al., 2013 Multimodal
EGF EGFR Head and Neck cancerO, gliomaS IRDye800CW Keereweer et al., 2012; Gong et al., 2014
TM1 GRPR Head and Neck cancerO IRDye680RD Suganya et al., 2016
G-pip-Sta-BBN, GSG-Sta-BBN,6Ahx-Sta-BBN Prostate cancerS AF750 Xu et al., 2018
BBN[7-14]NH2 GliomaC, O, Prostate cancerO AF680, IRDye800CW Cai et al., 2013; Li et al., 2018 Multimodal Clinical trial
BBN[6-14]NH2 Prostate cancerS IRDye650 Zhang et al., 2017a Multimodal
OTL78 (DUPA) PSMA Prostate cancerS S0456 Kularatne et al., 2018
KuE Prostate cancerS Cy5, ZW800+3C Bao et al., 2017; Schottelius et al., 2018 Multimodal
Glu-urea-Lys-HBED-CC Prostate cancerS IRDye800CW, DyLight800 Baranski et al., 2017 Multimodal
PSMA-1 Prostate cancerS, O Cy5.5, IRDye800CW Wang et al., 2014
AE105 uPAR GliomaO, Head and Neck cancerO ICG, CH1055 Christenen et al., 2017; Kurbegovic et al., 2018
ATF Breast cancerO, Pancreatic cancerO Cy5.5, NIR-830 Yang et al., 2014
Small molecules Hypoxyfluor-1 CAIX Colorectal cancerS S0456 Mahalingam et al., 2018a
Z-360 CCK2R, CCK2i4svR Transfected HEK 293TS, M LS288 Wayua and Low, 2014
OTL38 FR Cervical cancerS, Lung cancerC, Ovarian cancerC S0456 Hoogstins et al., 2016; Keating et al., 2017; Mahalingam et al., 2018b; Predina et al., 2018 Clinical trial
EC17 Breast cancerC, Ovarian cancerC, Renal cancerS, C Fluorescein van Dam et al., 2011; Guzzo et al., 2016; Tummers et al., 2016 Clinical trial
2-DG GLUT1 Head and Neck cancerO IRDye800CW Keereweer et al., 2012
BOEPL LHRH-R Breast cancerS, Endometrial cancerS, Ovarian cancerS S0456 Roy et al., 2019
L-733,060 NK1R Transfected HEK 293TS LS288 Kanduluru et al., 2016
YC-27 PSMA Prostate cancerS, O IRDye800CW Chen et al., 2009; Neuman et al., 2015
IY-IY TrkC Breast cancerS ZWCC Yang et al., 2018
*

C, In clinical trial; Ev, Ex vivo human tumor samples; Ip, small animal intraperitoneally disseminated tumor model; M, small animal metastatic tumor model; O, small animal orthotopic tumor model; Pdx, small animal patient-derived xenograft tumor model; S, small animal subcutaneous tumor model; Tg, small animal transgenic spontaneous tumor model.

ANXA2, annexin a2; CAIX, carbonic anhydrase 9; CCK2R, cholecystokinin 2 receptor (CCKi4svR is a splice variant); CEA, carcinoembryonic antigen; CXCR4, C-X-C chemokine receptor type 4; EGFR, epidermal growth factor receptor; EpCAM, epithelial cell adhesion molecule; FR, folate receptor; GLUT1, glucose transporter 1; GRPR, gastrin releasing peptide receptor; HER2/3, human epidermal growth factor receptor 2/3; LHRH-R, Luteinizing hormone releasing hormone receptor; IL-10, interleukin 10; MMP-2, matrix metalloproteinase 2; NK1R, neurokinin 1 receptor; PSCA, prostate stem cell antigen; PSMA, prostate specific membrane antigen; TAG-72, tumor-associated glycoprotein 72; TF, tissue factor; TrkC, tropomyosin receptor kinase C; uPAR, urokinase plasminogen activator receptor; VEGF-A, vascular endothelial growth factor A; VEGFR-2, Vascular endothelial growth factor receptor 2.