Nuclear Medicine and Molecular Imaging

The Korean Society of Nuclear Medicine (대한핵의학회)
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Radiotracer Methods for Targeted Imaging of the Epidermal Growth Factor Receptor

Epidermal Growth factor 수용체 영상을 위한 방사성추적자 기술

  • Jung, Kyung-Ho (Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine) ;
  • Lee, Kyung-Han (Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine)
  • 정경호 (성균관대학교 의과대학 삼성서울병원 핵의학과) ;
  • 이경한 (성균관대학교 의과대학 삼성서울병원 핵의학과)
  • Published : 2008.06.30
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Abstract

While indirect targeting strategies using reporter-genes are taking center stage in current molecular imaging research, another vital strategy has long involved direct imaging of specific receptors using radiolabeled ligands. Recently, there is renewal of immense interest in this area with particular attention to the epidermal growth factor receptor (EGFR), a transmembrane glycoprotein critically involved in the regulation of many cellular functions and malignancies. Recently, two novel classes of EGFR-targeting anticancer drugs have entered clinical trials with great expectations. These are monoclonal antibodies such as cetuximab that target the extracellular domain, and small molecule tyrosine kinase inhibitors such as gefitinib (lressa) and erlotinib (Tarceva) that target the catalytic domain of the receptor. However, early results have showed disappointing survival benefits, disclosing a major challenge for this therapeutic strategy; namely, the need to identify tumors that are most likely to respond to the agents. To address this important clinical issue, several noninvasive imaging techniques are under investigation including radiolabeled probes based on small molecule tyrosine kinase inhibitors, anti-EGFR antibodies, and EGF peptides. This review describes the current status, limitations, and future prospects in the development of radiotracer methods for EGFR imaging.

Keywords

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