Table 2.
Comprehensive overview of potential activatable FIGS tracers.
| Tracer type | Compound name | Molecular target | Imaging target | Reporter fluorophore(s) | References | Remarks | |
|---|---|---|---|---|---|---|---|
| Activatables; Cell-binding based | Antibody | Cetuximab | EGFR | Pancreatic cancerO | AF660 | (Obaid et al., 2017) | IRDye QC-1 quencher |
| Trastuzumab | HER2 | Lung cancerS | ATTO680 | (Kim et al., 2017) | Molecular switch | ||
| J591 | PSMA | Prostate cancerS | ICG | (Nakajima et al., 2011) | |||
| Minibody | PSMA-Mb | PSMA | Prostate cancerS | ICG | (Watanabe et al., 2014) | ||
| Diabody | PSMA-Cys-Db | PSMA | Prostate cancerS | ICG | (Sano et al., 2013) | ||
| Peptide | EGF | EGFR | Breast cancerS, Skin cancerS | ATTO655, Cy5.5 | (Ryu et al., 2013; Kim et al., 2019) | BHQ3 Quencher (Cy5.5) | |
| Activatables; enzyme-activated | HMRef-bGal | β-Galactosidase | Ovarian cancerIp | HMRef | (Asanuma et al., 2015) | Spirocyclic | |
| 6QCNIR | Cathepsins | Breast cancerO, Lung cancerTg | DyLight780-B1 | (Ofori et al., 2015) | IRDye QC-1 quencher | ||
| BMV109 | Cathepsins | Colorectal cancerTg | Cy5 | (Segal et al., 2015) | QSY21 quencher | ||
| GB119 | Cathepsins | GliomaO, Skin cancerEv | Cy5 | (Cutter et al., 2012; Walker et al., 2017) | QSY21 quencher | ||
| LUM015 | Cathepsins | Breast cancerC, O, Soft tissue sarcomaC, O | Cy5 | (Whitley et al., 2016; Smith et al., 2018) | Clinical trial, QSY21 quencher | ||
| Z-Phe-Arg-HMRG | Cathepsins | Ovarian CancerIp | Hydroxymethyl rhodamine green | (Fujii et al., 2014) | Spirocyclic | ||
| ANPFAP | FAP-α | GliomaS | Cy5.5 | (Li et al., 2012) | QSY21 quencher | ||
| gGlu-HMRG | GGT | Breast cancerEv, Colorectal cancerEv, Head and Neck cancerO | Hydroxymethyl rhodamine green | (Urano et al., 2011; Sato et al., 2015; Ueo et al., 2015; Slooter et al., 2018) | Spirocyclic | ||
| HMRef-βGlcNAc | Hexosaminidase | Colorectal cancerEv, Ip | HMRef | (Matsuzaki et al., 2016) | Spirocyclic | ||
| Q3STCy | hNQO1 | Ovarian cancerEv, Ip | TCy | (Shen et al., 2017) | Q3 is target specific, and quencher | ||
| AVB-620 | MMP-1,9, … | Breast cancerO, Pancreatic cancerO | Cy5 | (Metildi et al., 2015; Miampamba et al., 2017; Unkart et al., 2017) | Clinical trial, Cy7 quencher |
*C, In clinical trial; Ev, Ex vivo human tumor samples; Ip, small animal intraperitoneally disseminated tumor model; O, small animal orthotopic tumor model; S, small animal subcutaneous tumor model; Tg, small animal transgenic spontaneous tumor model.
EGFR, epidermal growth factor receptor; EpCAM, epithelial cell adhesion molecule; FAP-α, fibroblast activation protein alpha; GGT, gamma-glutamyltransferase; hNQO1, human NAD(P)H:quinone oxidoreductase type I; MMP-1/9, matrix metalloproteinase 1/9; PSMA, prostate specific membrane antigen.