Table 2.
An overview of the targets available on cellular TME components, with a number of their corresponding radioligands
| Source | Target | Compound | Research phase | Reference |
|---|---|---|---|---|
| Cancer-associated fibroblasts | FAP |
FAPI-04 FAPI-46 FAPI-74 FAPI-2286 OncoFAP BiOncoFap DOTA-2P(FAPI)2 DOTAGA.(SA.FAPi)2 |
Clinical trial Clinical trial Clinical trial Clinical trial Clinical trial Preclinical Preclinical Preclinical |
[92, 95, 100, 104, 106–108] |
| Tumor-associated macrophages | MMR (CD206) |
γ-Tilmanocept NOTA-anti-MMR-sdAb Man-LIPs |
Approved Clinical trial Preclinical |
[113, 115, 133] |
| TSPO |
PBR28 DPA-714 GE-180 DPA-713 |
Clinical trial Clinical trial Clinical trial Clinical trial Preclinical |
[122, 123, 125] | |
| Folate receptor β |
DTPA-folate EC20 |
Clinical trial Clinical trial |
[129, 130] | |
| Elevated endocytosis |
Al-HDL PL-HDL |
Preclinical Preclinical |
[134, 135] | |
| CD163 | Anti-CD163 mAbb | n/a | [137] | |
| Neo-angiogenic endothelial cells | Perfusion | 15O-water | Approved | [140] |
| αvβ3 Integrin |
Galacto-RDG FPPRGD2 Fluciclatide Alfatide Alfatide II NOTA-RGD2 DOTA-RGD2 |
Clinical trial Clinical trial Clinical trial Clinical trial Clinical trial Clinical trial Clinical trial |
[145, 152] | |
| APN/CD13 |
DOTA-NGR1/2 cNGR NGRyk |
Preclinical Preclinical Preclinical |
[154, 155] | |
| VEGF/VEGF-R |
VEGF165 VEGF121 Bevacizumab |
Clinical trial Preclinical Preclinical |
[160, 163] | |
| PSMA |
PSMA-11 PSMA-I&T PSMA-617 |
Approvedc Clinical trial Clinical trial |
[165, 166] | |
| Tumor-infiltrating immune cells |
PDL1 (tumor/stromal cells) |
Atezolizumab Avelumab NM-01 BMS-986192 |
Clinical trial Clinical trial Clinical trial Clinical trial |
[174, 176, 177] |
|
PD1 (immune cells) |
Nivolumab Pembrolizumab |
Clinical trial Clinical trial |
[175] | |
| CXCR4/CXCL12 |
Pentixather/Pentixafor NOTA-NFB AMD3100 AMD3465 |
Clinical trial Clinical trial Preclinical Preclinical |
[185–187, 190] | |
| Cancer-associated adipocytes | FABP4 |
TAP1 BMS-309403 |
Preclinical Preclinical |
[194–196] |
| FASN | Acetate | Preclinical | [198] |
bAffinity for rat CD163, tested in arthritis, not cancer. cFDA-approved for treatment of prostate cancer, not in angiogenesis setting