Positron Emission Tomography (PET) Imaging with [11C]-Labeled Erlotinib: A Micro-PET Study on Mice with Lung Tumor Xenografts

Abstract

Erlotinib (Tarceva) targets the epidermal growth factor receptor (EGFR), which is commonly overexpressed in human cancers, including lung cancer. We show that erlotinib can be labeled with [11 C] by reacting the normethyl precursor with [ 11

Strategies for Molecular Imaging of Epidermal Growth Factor Receptor Tyrosine Kinase in Cancer

“…2). In contrast to A549 and NC1358 cells, HCC827 cells have high expression of EGFR but, more important, harbor an in-frame deletion mutation (delE746-A750) in exon 19 (phosphorylated form) (21).…”

Preparation and Evaluation of 99mTc-Epidermal Growth Factor Receptor (EGFR)-Peptide Nucleic Acid for Visualization of EGFR Messenger RNA Expression in Malignant Tumors

“…Several modalities using PET, SPECT, and MR imaging have been introduced to noninvasively evaluate EGFR. Some noninvasive molecular agents, such as 11 Cerlotinib, 11 C-labeled 4-N-(3-bromoanilino)-6, 7-dimethoxyquinazoline, 177 Lu-nimotuzumab, 18 F-labeled Affibody protein, or anti-EGFR monoclonal antibodies using contrast-enhanced MR imaging, have been developed as molecular imaging biomarkers for evaluating tumor EGFR status (17)(18)(19)(20)(21). Although these EGFR-specific imaging probes have been investigated, they all have been directed either at an external ligand binding domain using antibodies and Affibody molecules or at the internal adenosine triphosphate binding domain with small organic reversible and irreversible inhibitors (22).…”

Multiplexed imaging for diagnosis and therapy

“…For instance, PET generally informs on tissue phenotypes or processes (such as receptor expression [11][12][13][14][15][16] , microenvironment 17,18 , metabolism 16,[19][20][21][22][23] or perfusion) with outstanding sensitivity, but it is hampered by low resolution, scarcity of anatomic detail and dosimetric stipulations 24 . In contrast, MR provides anatomic detail with exquisite resolution, but lacks the sensitivity offered by radionuclide imaging; specific aspects of individual modalities are indicated in Table 3 (refs 24-31 ).…”

“…In this setting, 11 C-choline-PET and, more recently, 68 Ga-PSMA-PET have been found to be superior to anatomical imaging with MRI or CT, using laparoscopic extended lymph-node dissection as the reference standard, including the detection of sub-centimetre lesions 6,157 . Diffusion weighted MRI (DWI) has similarly low-to-moderate sensitivity and high specificity as the aforementioned PET methods 158 , and it is envisaged that the combined use of a PET-MR scanner may lead to improvements in both sensitivity and specificity; however, methodological challenges exist and will need resolving in order to achieve optimal outcome.…”

“…179 with permission from AACR. c i-iv, Physiologic use of multiplexing PET demonstrated in the determination of the mechanism of action of temozolomide in glioma patients with 11 C-HCO3 -followed by 11 C-temozolomide in the same visit. Labelling temozolomide with carbon-11 as 4-11 C-carbonyl-temozolomide relative to 3-N-11 C-methyl-temozolomide leads to the generation of 11 C-CO2 in plasma of glioma patients, which is corrected by determining mathematically the unit impulse response function of 11 C-HCO3 in plasma.…”