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Nectin-4-Targeting Radiotracers: Novel Theranostic Agents for Precision Oncology in Cancer
Giorgia Speltri1, Ilham Badrane2,3, Rebecca Napolitano4
1Department of Chemical, Pharmaceutical, and Agricultural Sciences, University of Ferrara, Via L. Borsari, 46-44121, Ferrara, Italy.
Abstract:
Nectin cell adhesion molecule 4 (Nectin-4) is specifically overexpressed in most cancers of epithelial origin but downregulated in normal tissue, representing an ideal target for positron emission tomography imaging. The development of positron emission tomography imaging probes targeting Nectin-4 has gained significant attention in recent years, especially after the approval in December 2019 by the US Food and Drug Administration of enfortumab vedotin-an antibody drug conjugate targeting Nectin-4-in patients with locally advanced or metastatic bladder cancer. This article aims to comprehensively review original research articles discussing preclinical development or early translational clinical applications of radiolabeled probes targeting Nectin-4. The main radioactive compounds investigated belong to two classes, antibody-based radiopharmaceuticals and peptide-drug conjugates, in particular novel bicyclic peptides. While monoclonal antibody-based probes have demonstrated theranostic potential in preclinical studies, their clinical application has been hindered by their slow pharmacokinetic properties. However, peptide-based positron emission tomography/computed tomography tracers offer several advantages, such as ease of handling in synthesis, a more favorable biodistribution, and lower immunogenicity and have been tested in preliminary clinical experiences.
Insights
Nectin-4 targeted imaging probes show promise for epithelial cancers. Peptide-based tracers offer advantages over antibodies for positron emission tomography/computed tomography imaging.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Nectin cell adhesion molecule 4 (Nectin-4) is overexpressed in epithelial cancers, making it a target for imaging.
- Enfortumab vedotin, an Nectin-4 targeting agent, was approved for bladder cancer in 2019, increasing interest in Nectin-4 probes.
Purpose of the Study:
- To review preclinical and early translational research on radiolabeled probes targeting Nectin-4.
- To compare antibody-based and peptide-based radiopharmaceuticals for Nectin-4 imaging.
Main Methods:
- Literature review of original research articles.
- Analysis of radiolabeled probes including antibody-drug conjugates and peptide-drug conjugates.
- Evaluation of preclinical and early clinical data.
Main Results:
- Both antibody-based and peptide-based probes targeting Nectin-4 have shown theranostic potential.
- Antibody-based probes face pharmacokinetic limitations for clinical use.
- Peptide-based positron emission tomography/computed tomography tracers exhibit favorable properties like easier synthesis, better biodistribution, and lower immunogenicity.
Conclusions:
- Peptide-based tracers are promising for Nectin-4 targeted positron emission tomography/computed tomography imaging due to their advantages.
- Further clinical evaluation of peptide-based tracers is warranted.
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