Journal
PHARMACEUTICALS
Volume 15, Issue 4, Pages -Publisher
MDPI
DOI: 10.3390/ph15040450
Keywords
EGFR; PET tracer; evaluation
Categories
Funding
- European Union [675417]
- Marie Curie Actions (MSCA) [675417] Funding Source: Marie Curie Actions (MSCA)
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This review analyzes the historical development of in vivo evaluation approaches for EGFR PET tracers and discusses the challenges faced by each tracer, as well as the requirements for driving progress in this field.
Multiple small molecule PET tracers have been developed for the imaging of the epidermal growth factor receptor (EGFR). These tracers target the tyrosine kinase (TK) domain of the receptor and have been used for both quantifying EGFR expression and to differentiate between EGFR mutational statuses. However, the approaches for in vivo evaluation of these tracers are diverse and have resulted in data that are hard to compare. In this review, we analyze the historical development of the in vivo evaluation approaches, starting from the first EGFR TK PET tracer [C-11]PD153035 to tracers developed based on TK inhibitors used for the clinical treatment of mutated EGFR expressing non-small cell lung cancer like [C-11]erlotinib and [F-18]afatinib. The evaluation of each tracer has been compiled to allow for a comparison between studies and ultimately between tracers. The main challenges for each group of tracers are thereafter discussed. Finally, this review addresses the challenges that need to be overcome to be able to efficiently drive EGFR PET imaging forward.
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