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Advances in Radiotherapy
& Nuclear Medicine Role of PET/CT in exploring tumor heterogeneity
Table 1. Mechanism of action and indications of various positron emission tomography (PET) radiopharmaceuticals 24,25
PET radiopharmaceutical Mechanism of localization Oncological indication
18 F-fluorodeoxyglucose (FDG) Enters the cell through GLUT 1 and 3 Staging, restaging, and response
transporter, phosphorylated and trapped assessment of a wide range of tumors,
inside the cell including breast, lung, GI tumors,
melanoma, etc.
68 Ga-DOTA -peptides Binds to somatostatin receptors on tumor Staging and restaging of neuroendocrine
cells tumors
18
18 F-fluoro-L DOPA ( F-DOPA) Transported into the cell by large neutral Diagnosis, staging, and follow-up
amino acid transporters L-type (LAT) of neural crest tumors, for example,
and stored in secretory vesicles neuroblastoma, paraganglioma,
brain tumors, and congenital
hyperinsulinemia
18 F-metafluorobenzylguanidine (mFBG) Norepinephrine analog transported Detection and staging of neural crest
by norepinephrine transporters tumors
overexpressed on tumor cells
68 Ga/ F/ Cu-prostate-specific Binds to PSMA (type II transmembrane Staging and detection of recurrence in
64
18
membrane antigen (PSMA) protein) on prostate cancer cells prostate cancer
68 Ga-fibroblast activation protein Binds to FAP in the stroma of tumor Diagnosis and staging of various
inhibitor (FAPI) microenvironment tumors, for example, pancreas,
cholangiocarcinoma, breast, etc.
18 F-fluoroestradiol (FES) Binds to estrogen receptors in the nucleus Diagnosis and follow-up of
of ER-expressing cells hormone-positive breast cancer
Various Zirconium labeled tracers
89
89 Zr-trastuzumab Labeled antibodies (immune-PET); Diagnosis and staging of HER2-positive
monoclonal antibody that binds to breast cancers
89 Zr-cituximab HER2; targets EGFR; binds to VEGFA; Diagnosis of cancers with overexpression
antibodies act against PD-L1; targets of EGFR
CD38 antigen expressed on myeloma
89 Zr-bevacizumab cells Diagnosis of cancers with overexpression
of VEGF
89 Zr-atezolizumab Detection of PD-L1-positive tumors
89 Zr-DFO-daratumumab Diagnosis of multiple myeloma
68 Ga-RGD/trivehexin Binds with integrins expressed on tumor Diagnosis of cancers, for example,
cells or angiogenic blood vessels pancreas, head and neck, etc.
18
18 F-fluoroethyl-l-tyrosine ( F-FET); Amino acid analogs transported in cells Diagnosis and grading of brain tumors
11 C-methyl-l-methionine ( C-MET) by overexpressed transmembrane LAT on
11
tumor cells
18 F-fluciclovine Amino acid analog enters the cell by Diagnosis of biochemically recurrent
neutral amino acid transporter prostate cancer and other tumors
11 C-acetate/palmitate Converted to acetyl CoA in cells Diagnosis of prostate, renal, brain, and
for cholesterol and fatty acid HCC cancers
synthesis, which are integrated into
the cell membrane or oxidized in
mitochondria
18 F/ C-choline Phosphorylated to phosphorylcholine Diagnosis of the brain, prostate, lung,
11
within cells and integrated into bladder cancers, etc.
phospholipids in the cell membrane
18 F-FLT (thymidine) Enters cell by facilitated diffusion through Diagnosis and response assessment of
nucleoside transporters and is trapped in cancers, for example, lung, breast, colon,
the cell lymphoma
18 F-misonidazole Nitroimidazole compound that enters the Detects hypoxia in tumors, for example,
cell through blood flow and gets trapped lung, head and neck, and brain tumors
in hypoxic cells
(Cont'd...)
Volume 3 Issue 2 (2025) 5 doi: 10.36922/ARNM025040005
