Abstract

Molecular imaging is an emerging strategy for in vivo visualization of cancer over time based on biological mechanisms of disease activity. Optical imaging methods offer a number of advantages for real-time cancer detection, particularly in the epithelium of hollow organs and ducts, by using a broad spectral range of light that spans from visible to near-infrared. Targeted ligands are being developed for improved molecular specificity. These platforms include small molecule, peptide, affibody, activatable probes, lectin, and antibody. Fluorescence labeling is used to provide high image contrast. This emerging methodology is clinically useful for early cancer detection by identifying and localizing suspicious lesions that may not otherwise be seen and serves as a guide for tissue biopsy and surgical resection. Visualizing molecular expression patterns may also be useful to determine the best choice of therapy and to monitor efficacy. A number of these imaging agents are overcoming key challenges for clinical translation and are being validated in vivo for a wide range of human cancers.

Highlights

  • Cancer is a worldwide health-care concern that is steadily growing

  • Targeted optical contrast agents have the potential to provide a molecular mechanism to complement the anatomical view of cancer provided by conventional imaging platforms. ey can be administered via different routes, including topically and systemically, to infiltrate the epithelium for effective binding to achieve high contrast images

  • E peptide ASYNYDA was found to localize to regions of high-grade dysplasia and esophageal adenocarcinoma in patients with Barrett’s esophagus using either confocal endomicroscopy or wide-field endoscopy (Figure 5(d)) [82, 83]. e pharmacology/toxicology study was performed in rats at 4 doses in escalation by oral gavage and showed no peptide-related acute adverse effects in clinical signs or chemistries or on necropsy up to 15 days after peptide administration up to 0.86 mg/kg. e receiver-operator characteristic (ROC) curve for in vivo imaging showed an optimum sensitivity of 75% and specificity of 97% at tumorto-background ratio (TBR) 4.2, with an area under curve (AUC) of 0.91. e performance of the peptide varied with threshold

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Summary

Introduction

Cancer is a worldwide health-care concern that is steadily growing. By 2030, an annual incidence and mortality of 21.7 and 13 million cases, respectively, are expected [1]. is increase is attributed to an aging population, greater prevalence of obesity, adoption of western diets by developing countries, and environmental factors [2,3,4]. Rapid progress has been made in the technical performance of whole-body imaging systems, Contrast Media & Molecular Imaging including computed tomography (CT), magnetic resonance imaging (MRI), and ultrasound (US) [19,20,21,22,23] While these platforms provide detailed images of tumor anatomy, they reveal little about the biology that drives cancer progression. 2-deoxy-2-18F-fluoro-Dglucose (18FDG) is used routinely with PET in clinical practice for cancer staging [24,25,26] While both modalities have the capability to image multiple targets using affinity probes labeled with different radioisotopes, this approach is limited by high cost, lack of widespread radiotracer availability, and radiotracer stability. Nonspecific dye retention can reduce diagnostic performance for ICG, and clinical utility is limited by high levels of binding to plasma proteins (98%), low stability in aqueous media, and concentration dependent shifts in wavelength [59]

Targeted Optical Imaging Agents
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