From:  Translocator protein (TSPO) in glioma: implications for diagnosis, disease progression monitoring, and targeted therapies

TSPO-targeted therapies and imaging in gliomas

TherapyMeritsMOAClinical usesReference(s)
[11C]PK11195The high specificity for TSPO allows for tumor detection.Binds to TSPO in the outer mitochondrial membrane, enabling PET imaging.Imaging of TSPO-positive glioblastoma.[86, 99]
[18F]DPA-714It enhances imaging techniques and may reduce tumor growth.TSPO antagonist, inhibiting tumor cell proliferation and inducing apoptosis.Potential in clinical trials for therapy.[36, 100, 101]
[18F]FEPPAHigh sensitivity and specificity for TSPO allow the monitoring of treatment responses.Selectively binds to TSPO in the outer mitochondrial membrane, enabling PET imaging.Detection of TSPO-expressing gliomas and monitoring therapies.[102, 103]
[18F]PBR111Non-invasive imaging and quantification of TSPO expression.Binds to TSPO and enables PET imaging of tumor viability.Used in glioma diagnosis and assessment of treatment efficacy.[104]
[11C]PBR-28Selectively eliminates TSPO-positive glioma cells.Induces apoptosis in TSPO-expressing cells.Targeted chemotherapy for treating TSPO-positive gliomas.[102, 105]
Ro5-4864Anti-proliferative effects in glioma cells promote apoptosis.It inhibits TSPO, disrupting cellular metabolism and leading to cell death.Preclinical studies focusing on glioma treatment.[51, 106]
[18F]GE180High binding affinity to TSPO and a better signal-to-noise ratio make it useful for distinguishing tumor types.Binding to TSPO allows visualization of activated cells, specifically within tumor areas contributing to the glioma pathology.Imaging of glioma to assess tumor viability and differentiate between types of gliomas based on TSPO expression.[36, 66, 107]
Return to article view

[11C]PBR-28: N-(2-[¹¹C]methoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide; [11C]PK11195: [11C]N-butan-2-yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide; [18F]DPA-714: [18F]N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide; [18F]FEPPA: [¹⁸F]N-(2-(2-fluoroethoxy)benzyl)-N-(4-phenoxypyridin-3-yl)acetamide; [18F]GE180: [18F]3-(2-fluoroethyl)-2-[(4-methoxyphenyl)thiomethyl]-8-methylquinazolin-4-one; [18F]PBR111: 2-(6-chloro-2-(4-(3-[¹⁸F]fluoropropoxy)phenyl)imidazo[1,2-a]pyridin-3-yl)-N,N-diethylacetamide; MOA: mechanisms of action; PET: positron emission tomography; Ro5-4868: 4'-chlorodiazepam; TSPO: translocator protein