Table 3.
Peptide-based radiopharmaceuticals targeting GRPR evaluated in prostate cancer, preclinical, and experimental study models.
| Radiopharmaceuticals | Target | Usage | Tumor | Tumor uptake | Tumor-to-muscle (T/M) ratios | Half time | References |
|---|---|---|---|---|---|---|---|
| Al(18)F-NOTA-4,7-lanthionine-BBN Al(18)F-NOTA-2,6-lanthionine-BBN |
GRPR | PET imaging | PC-3 | 0.82 ± 0.23% ID/g (2 h p.i.) 1.40 ± 0.81% ID/g (2 h p.i.) |
9.1 ± 1.2 (2 h p.i.) 14.6 ± 1.7 (2 h p.i.) |
Carlucci et al., 2015 | |
|
64Cu-NODAGA-BBN 64Cu-NODAGA-galto-BBN |
GRPR | Targeted radiotherapy | PC-3 | 1.62 ± 0.23% ID/g (1 h p.i.) 3.26 ± 0.53% ID/g (1 h p.i.) |
70.7 ± 43.71 h 29.2 ± 20.61 h |
Kim et al., 2015 | |
|
68Ga-DOTA-AMBA 177Lu-DOTA-AMBA 111In-AMBA |
GRPR | PET imaging Targeted radiotherapy SPECT imaging |
PC-3 | / 6.35 ± 2.23% ID/g (1 h p.i.) 2.24 ± 0.66% ID/g (1 h p.i.) |
/ / 3.89 (1 h p.i.) |
/ / 1.53 ± 0.69 h (t1/2α) 30.73 ± 8.56 h (t1/2β) |
Maddalena et al., 2009; Zhang-Yin et al., 2020
Ho et al., 2011 |
| 64Cu-NO2A-(8-Aoc)-BBN | GRPR | PET imaging | PC-3 | 3.59 ± 0.73% ID/g (1 h p.i.) | Lane et al., 2010 | ||
| 68Ga-NOTA-PEG3-RM26 | GRPR | PET imaging | PC-3 | 3.31 ± 0.68% ID/g (1 h p.i.) | 72.5 (1 h p.i.) | Cheng et al., 2018 | |
| 64Cu-DOTHA2-PEG-RM26 | GRPR | PET imaging | PC-3 | 4.14 ± 0.96% ID/g (1 h p.i.) | Mansour et al., 2018 | ||
| 68Ga-NODAGA-SCH1 | GRPR | PET imaging | 6.20 ± 0.53% ID/g (2 h p.i.) | 16.6 ± 1.5 (2 h p.i.) | Sun et al., 2016 | ||
| 111In-RM1 | GRPR | SPECT imaging | PC-3 | 14.24 ± 1.75% ID/g (1 h p.i.) | 75 (1 h p.i.) | Mansi et al., 2009 | |
| Al18F-JMV5132 68Ga-JMV5132 68Ga-JMV4168 |
GRPR | PET imaging | PC-3 | 4.96 ± 1.20% ID/g (1 h p.i.) 4.73 ± 0.68% ID/g (1 h p.i.) 4.46 ± 0.33% ID/g (1 h p.i.) |
Chatalic et al., 2014 | ||
|
177Lu-SB3 111In-SB3 |
GRPR | Targeted radiotherapy SPECT imaging |
PC-3 | 8.22 ± 1.61% ID/g (4 h p.i.) 8.78 ± 3.03% ID/g (4 h p.i.) |
Maina et al., 2016; Lymperis et al., 2018 | ||
|
68Ga-NeoBOMB1 111In-NeoBOMB1 177Lu-NeoBOMB1 |
GRPR | PET imaging SPECT imaging Targeted radiotherapy |
PC-3 | 30.7 ± 3.9% ID/g (4 h p.i.) 28.6 ± 6.0% ID/g (4 h p.i.) 42.4 ± 5.0% ID/g (4 h p.i.) |
Nock et al., 2017 | ||
| 18F-AmBF3-MJ9 | GRPR | SPECT imaging | PC-3 | 1.37 ± 0.2% ID/g (1 h p.i.) | Pourghiasian et al., 2015 |