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Table 1 Summary of potential PET tracers for TAMs, evaluated in preclinical or clinical studies

From: Potential PET tracers for imaging of tumor-associated macrophages

Target

Macrophage phenotype

Radiotracer

Species

Disease (model)

References

CD206

M2

[18F]FDM

Rabbit

Atherosclerosis model

Tahara et al. (2014)

[18F]FB-anti-MMR-sdAb

Mouse

Lung cancer xenograft model

Blykers et al. (2015)

[68Ga]NOTA-MSA

Mouse

Atherosclerosis model

Kim et al. (2016)

[68Ga]NOTA-anti-MMR-Nb

Mouse

Atherosclerosis model

Varasteh et al. (2019)

[68Ga]Ga-NOTA-anti-MMR-sdAb

Mouse

Lung cancer xenograft model

Xavier et al. (2019)

CD163

M2

[68Ga]ED2

Rat

Arthritis model

Eichendorff et al. (2015)

Arginase

M2

[18F]FMARS

Mouse

Prostate cancer xenograft model

Clemente et al. (2021)

[18F]FBMARS

Mouse

Prostate cancer xenograft model

Clemente et al. (2021)

CSF-1R

M1 and M2

[11C]AZ683

Rat, non-human primate

Healthy

Tanzey et al. (2018)

[11C]CPPC

Mouse, non-human primate

Neuroinflammation model (LPS)

Horti et al. (2019), Zhou et al. (2021)

[11C]GW2580

Mouse, non-human primate

Neuroinflammation mouse model (LPS) and health non-human primates

Zhou et al. (2021)

CD68

M1 and M2

[64Cu]CD68-Fc

Mouse

Atherosclerosis model

Bigalke et al. (2014)

CCR2

M1 and M2

[64Cu]-DOTA-ECLi

Rat

Abdominal aortic aneurysm model

English et al. (2020)

[64Cu]Cu@CuOx-ECLi

Mouse

Pancreatic ductal adenocarcinoma model

Zhang et al. (2021)

[18F]6b

Mouse

Healthy

Wagner et al. (2021)

Folate receptor

M1 and M2

[68Ga]NOTA-folate

Mouse

KB xenograft model

Brand et al. (2017)

[18F]AlF-NOTA-folate-PEG12

Mouse

KB xenograft model

Chen et al. (2017)

[18F]fluoro-PEG-folate

Mouse

Rheumatoid arthritis model

Chandrupatla et al. (2018)

Human

Rheumatoid arthritis

Verweij et al. (2020)

[18F]AlF-NOTA-folate

Mouse

Atherosclerosis model

Silvola et al. (2018)

[18F]AzaFol

Mouse

Lung fibrosis model

Schniering et al. (2019)

  

Human

Ovarian and lung cancer

(https://clinicaltrials.gov/ct2/show/NCT03242993)

  1. sdAb: single-domain antibody; Nb: nanobody; CSF-1R: Colony stimulating factor 1 receptor; CD: cluster of differentiation; CCR2: C–C chemokine receptor type 2; KB: human epithelial cancer cell; Fc: fragment crystallizable region; LPS: lipopolysaccharides; 6b: 2-[4-(5-Fluoropentoxy)phenyl]-N-{4-[N-methyl-N-(tetrahydro-2H-pyran-4-yl)aminomethyl]phenyl}-6,7-dihydro-5H-benzo[7]annulene-8-carboxamide