Table 6.
Current state of pre-clinical studies performed on scandium radionuclides
| Type of vector | Radioisotope used | Tumor model or human | Bio-Distributions (BioD) PET images |
Main results | Reference |
|---|---|---|---|---|---|
|
DOTATATE DOTANOC DOTATOC |
natSc, 43Sc, 44Sc | AR42J cells, xxx | In vitro | (Walczak et al. 2015; Minegishi et al. 2016; Domnanich et al. 2017b; Pruszynski et al. 2012; Domnanich et al. 2017c; Koumarianou et al. 2011) | |
| DOTATOC | 47Sc | AR42J cells | In vitro | (Loveless et al. 2019a) | |
| DOTA - puromycin | 44Sc |
Walker carcinoma 256 (breast carcinoma) in rats AT1 carcinoma (prostate carcinoma) in rats |
BioD + PET | significant tumor uptake of [44Sc]Sc-DOTA puromycin and a clear-cut tumor visualization, cellular uptake of [44Sc]Sc-DOTA-puromycin could be suppressed by blocking protein synthesis | (Eigner et al. 2013) |
| DOTA-Bombesin | 44Sc, 68Ga |
PC3 cells, rats with Dunning R-3327-AT-1 prostate cancer tumor (GRP/BN receptor expression) MCF7 |
BioD + microPET |
68Ga- and [44Sc]Sc-DOTA-BN[2–14]NH2 showed no differences in tumor uptake in micro-PET images [68Ga]Ga- and [44gSc]Sc-DOTA-Ava-BBN showed similar accumulation and retention profiles in PC3 and MCF7 tumors |
(Koumarianou et al. 2012), (Ferguson et al. 2020) |
| DOTA-Folate | 44Sc |
KB cells KB tumor-bearing mice |
BioD + PET | Tissue accumulation is similar to [177Lu]Lu-folate = > 44Sc could serve for dosimetry prior to 177Lu-based therapy | (Muller et al. 2018; Muller et al. 2014) |
| 47Sc |
KB cells KB tumor-bearing mice |
BioD | Delay in tumor growth | (Muller et al. 2014; Siwowska et al. 2019) | |
| PSMA-617 | 44Sc, 177Lu, 68Ga | PC-3 PIP and PSMA-negative PC-3 flu prostate cancer cells | BioD + PET (2 h p.i.) | [44Sc]Sc-PSMA-617 almost identical biodistribution data compared to [177Lu]Lu-PSMA-617 | (Umbricht et al. 2017) |
| 43Sc, 47Sc, 44Sc |
LNCaP cells + human |
BioD + PET + SPECT (2 h p.i.) | Tumor to liver ratio between 2.5 and 8.8. | (Umbricht et al. 2017; Eppard et al. 2017) | |
| picagaDUPA | 44Sc | PC3 cells, Male NCr nude mice | BioD + PET (90 min p.i.) |
uptake 13.8 ± 0.6% ID/g enhanced binding affinity to the target for [44Sc]Sc(picaga)-DUPA, and possibly also from slower blood clearance. |
(Vaughn et al. 2020a; Vaughn et al. 2020b) |
|
DOTA-RGD NODAGA-RGD DOTA-NOC NODAGA-NOC |
44Sc, 68Ga | U87MG (human glioblatoma) and AR42J tumor-bearing mice |
BioD + PET/CT (0.5 to 5 h p.i.) |
44Sc stability using NODA-functionalized peptides was increased compared to the corresponding radiolabeled one with 68Ga | (Domnanich et al. 2017c; Hernandez et al. 2014) |
| DOTA-NAPamide | 44Sc, 68Ga | MC1-R positive (B16-F10) and negative (A375) melanoma cell lines. |
In cellulo, BioD + PET/CT (1 to 4 h p.i.) |
Uptake 2.61 ± 0.46% ID/g on B16-F10 and 0.21 ± 0.08% ID/g on A375 for 44Sc-DOTA-NAPamide | (Nagy et al. 2017b) |
| CHX-A”-DTPA-Fab fragment of Cetuximab | 44Sc | U87MG (human glioblastoma) in tumor- bearing mice) | PET + BioD (0.5 to 6 h p.i.) | rapid tumor uptake (max. Uptake of ∼12% ID/g at 4 h p.i.) of with excellent tumor-to-background ratio | (Chakravarty et al. 2014) |
| DOTA-ZHER2–2891 | 44Sc | HER2-SKOV3.ip (human ovarian cancer) in vitro and in xenografted mice |
BioD (6 h p.i.) |
Higher tumor-to-background contrast | (Honarvar et al. 2017) |
| DOTA-antiCD20 | 46Sc | Raji cells in wild rats |
BioD (72 h p.i.) |
similar biodistribution pattern compared to other radiolabeled anti-CD20 immunoconjugates | (Moghaddam-Banaem 2012) |