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Table 6 Current state of pre-clinical studies performed on scandium radionuclides

From: Production of scandium radionuclides for theranostic applications: towards standardization of quality requirements

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)