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Peptides as Vectors for Radiopharmaceutical Therapy

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Radiopharmaceutical Therapy

Abstract

Radiolabeled receptor-binding peptides enable the selective delivery of radionuclides to target tissues (e.g., tumor) while reducing radiation toxicity to peripheral organs. Peptide-based nuclear imaging and radiopharmaceutical therapy (RPT) have advanced significantly in recent years with the United States Food and Drug Administration’s approvals of 68Ga-labeled NETSPOT® for the positron emission tomography (PET) imaging of neuroendocrine tumors in 2016 and its 177Lu-labeled therapeutic twin LUTATHERA® in 2018. Peptides can be viewed as smaller fragments of proteins, typically composed of α-amino acids in the L-configuration. The high affinity of peptides for their molecular targets as well as their ease of synthesis, tolerance to structural modifications, and general lack of immunogenicity make them particularly attractive as vectors for RPT (or, more specifically, peptide receptor radionuclide therapy, PRRT). However, the properties that make peptides attractive tools for diagnostic imaging—such as their rapid clearance—can become liabilities in the context of RPT, where longer circulation times may be desirable to achieve high levels of accumulation in target tissue. This chapter describes strategies for the identification of promising peptide sequences, common structural modifications employed for the successful development of peptides for RPT, and widely used strategies for radiolabeling. We also describe particularly notable peptide receptor targets, their associated ligands, and the future of peptide-based RPT in the clinic.

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Authors and Affiliations

  1. Department of Biomedical Engineering, University of California, Davis, CA, USA

    Ryan A. Davis & Tanushree Ganguly

  2. Department of Internal Medicine, Division of Hematology/Oncology, University of California, Davis, CA, USA

    Sven H. Hausner

  3. Department of Biomedical Engineering, Department of Internal Medicine, Division of Hematology/Oncology and Center for Molecular and Genomic Imaging, University of California, Davis, CA, USA

    Julie L. Sutcliffe

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  1. Ryan A. Davis
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  2. Tanushree Ganguly
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  4. Julie L. Sutcliffe
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Correspondence to Julie L. Sutcliffe .

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Editors and Affiliations

  1. Memorial Sloan Kettering Cancer Center, New York, NY, USA

    Lisa Bodei

  2. Memorial Sloan Kettering Cancer Center, New York, NY, USA

    Jason S. Lewis

  3. Hunter College - CUNY, New York, NY, USA

    Brian M. Zeglis

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Davis, R.A., Ganguly, T., Hausner, S.H., Sutcliffe, J.L. (2023). Peptides as Vectors for Radiopharmaceutical Therapy. In: Bodei, L., Lewis, J.S., Zeglis, B.M. (eds) Radiopharmaceutical Therapy. Springer, Cham. https://doi.org/10.1007/978-3-031-39005-0_13

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