Table 2.
GRPR-antagonist-based peptide radioligands tested in the clinic. BBN(7–14), H-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2.
| Radioligand | Radioconjugate Sequence | Clinical Indication | Ref. |
|---|---|---|---|
| SPECT Tracers | |||
| [99mTc]Tc-DB15 | [99mTc]Tc-N4-AMA‡-DGA†-[DPhe6,Sar11,Leu13-NHEt]BBN(6–13) | Advanced BC⇈ | [28] |
| PET Tracers | |||
| [68Ga]Ga-SB3 | [68Ga]Ga-DOTA-AMA‡-DGA†-[DPhe6,Leu13-NHEt]BBN(6–13) | Disseminated PC⇊, BC⇈ | [21,29] |
| [68Ga]Ga-RM2 | [68Ga]Ga-DOTA-Pip§-[DPhe6,Sta13,Leu14-NH2]BBN(6–14) | PC⇊, BC⇈ | [30,31] |
| [68Ga]Ga-RM26 | [68Ga]Ga-NOTA-PEG3-[DPhe6,Sta13,Leu14-NH2]BBN(6–14) | PC⇊, BC⇈ | [32,33] |
| [68Ga]Ga-NeoBOMB1 | [68Ga]Ga-DOTA-AMA‡-DGA-[DPhe19,Gln20,His25-NHR]GRP(20–25)€ | Different malignancies |
[34,35] |
| [64Cu]Cu-CB-TE2A | [64Cu]Cu-CB-TE2A-PEG4-[DPhe6,Sta13,Leu14-NH2]BBN(6–14)# | Newly diagnosed PC⇊ |
[36] |
| PRRT Agents | |||
| [177Lu]Lu-RM2 | [177Lu]Lu-DOTA-Pip§-[DPhe6,Sta13,Leu14-NH2]BBN(6–14) | castration-resistant PC⇊ | [37] |
| [177Lu]Lu-NeoBOMB1 | [177Lu]Lu-DOTA-AMA‡-DGA†-[DPhe19,Gln20,His25-NHR]GRP(20–25)€ | Advanced solid tumors |
(NCT03872778) |
‡ AMA, p-aminomethylaniline; †DGA, diglycolic acid; §Pip, 4-amino-1-carboxymethyl-piperidine; €R, -CH(CH2CH(CH3)2)2; ⇊PC, prostate cancer; #CB-TE2A, 4,11-bis(carboxymethyl)-1,4,8,11-tetraazabicyclo(6.6.2)hexadecane; ⇈ BC, breast cancer.