PET imaging with small-molecule tyrosine kinase inhibitors: TKI-PET

Breast Cancer Resistance Protein and P-Glycoprotein Influence In Vivo Disposition of 11C-Erlotinib

“…Among several different radiolabeled reversible and irreversible TKIs tested for PET imaging of receptor tyrosine kinases, 11 C-erlotinib has emerged as a promising candidate tracer to distinguish responders from nonresponders to treatment with EGFR-targeted TKIs (e.g., gefitinib, erlotinib) (17). Preclinical as well as clinical data indicate that 11 C-erlotinib binds specifically to EGFR with activating mutations (e.g., delE746-A750, L858R), whereas it lacks specific binding to wild-type EGFR (2-6).…”

Imaging of Platelet-Derived Growth Factor Receptor β Expression in Glioblastoma Xenografts Using Affibody Molecule111In-DOTA-Z09591

“…Imaging of receptor tyrosine kinase expression might provide important additional diagnostic information that cannot be obtained from 18 F-FDG imaging. The development of radionuclide-labeled tracers for the visualization of receptor tyrosine kinases is therefore one focus in radiopharmaceutical research (16)(17)(18)(19). Radiolabeled TKIs have the potential advantage of enabling direct imaging of the therapeutic target.…”

Nodular Thyroid Disease and Thyroid Cancer in the Era of Precision Medicine

“…These findings have prompted the development of peptide receptor radionuclide therapy with yttriumor lutetium-labelled somatostatin analogues to treat advanced DTC tumours [60][61][62] . Additionally TKI-PET tracers have shown encouraging results [63] . Finally, 124 I-PET has demonstrated clinical and functional value in the analysis of DTC metastases [64,65] .…”