Further characterization of the epidermal growth factor receptor ligand 11C-PD153035
- Author:
- No author available
- Journal Title:
- CHINESE MEDICAL JOURNAL
- Issue:
- 11
- DOI:
- No doi available
- Key Word:
- 4-N-( 3-bromoanilino )-6,7-dimethoxyquinazoline;epidermal growth factor receptor;tyrosine kinase;positron emission tomography
Abstract： Background 11C-4-N-(3-bromoanilino)-6,7-dimethoxyquinazoline (11C-PD153035) has been reported as a tracer for imaging human tumors that overexpress epidermal growth factor receptor (EGFR). However it is still unclear whether 11C-PD153035 uptake correlates with EGFR expression levels. The objective of this study was to investigate the relationship between 11C-PD153035 accumulation and EGFR expression levels.Methods Synthesis of 11C-PD153035 was performed in the Tracerlab FXc system. Accumulation of 11C-PD153035 by MDA-MB-468, A549 and MDA-MB-231 cells was measured in vitro. There were six tumor-bearing mice in each group.11C-PD153035 uptake in tumors was determined by positron emission tomography/computed tomography (PET/CT).Tumor/normal muscle tissue (T/NT) analysis in PET images was applied to quantify the PET data. Sixty minutes after PET/CT scanning, the nude mice were sacrificed and the tumors were excised. The 11C-PD153035 accumulation in different tumors was determined by a gamma counter.Results Close correlation existed between the uptake and the level of EGFR expression both in vitro and ex vivo (r2=0.72, P＜0.001; r2=0.63, P=0.003). When the static T/NT analysis method was applied to analyze the PET data, the observed correlation was again excellent (r2=0.70, P=0.001).Conclusions The uptake of PET tracer 11C-PD153035 closely correlates with the EGFR expression levels in tumor cells. 11C-PD153035 has the potential to yield useful information for both cancer diagnosis and therapy.
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