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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)