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Radiopharmaceuticals for Therapy

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Molecular Imaging and Targeted Therapy

Abstract

Radionuclide therapy or targeted radionuclide therapy (TRT) is designed to selectively deliver cytotoxic radiation to cancer cells that causes minimal toxicity to surrounding healthy tissues, using optimized targeting vehicles (such as small organic molecules, peptides, and proteins) that deliver beta (β−) or alpha (α) emitting radionuclides to specific biological targets (such as receptors and tumor-specific proteins) in cancer tissue. Therapeutic radiopharmaceuticals may be structurally simple ions (131I−, 89Sr2+, and 223Ra2+), small molecules (131I-MIBG and 153Sm-EDTMP), complex molecules (177Lu-Dotatate, 177Lu-DOTA-PSMA-617, and 90Y-ibritumomab tiuxetan), colloids (32P chromic phosphate), or even particles (90Y labeled microspheres). Twelve approved therapeutic radiopharmaceuticals are in clinical use and many more are in active clinical investigation. Theranostics has the potential to develop patient-specific radiation dosimetry strategies based on molecular imaging (MI) studies and cell-killing radiation strategies to deliver the optimal therapeutic dose to the right patient at the right time. The success of the theranostic approach has been well established in patients with neuroendocrine tumors and prostate cancer with the approval of 18F-, 68Ga-, and 64Cu-labeled PET radiopharmaceuticals for MI studies, and 177Lu-labeled somatostatin receptor (SSTR) agonists and small-molecule prostate-specific membrane antigen (PSMA) inhibitors. This chapter provides a broad overview of therapeutic radiopharmaceuticals, clinical indications, and mechanisms of tumor localization.

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  1. Emeritus of Radiochemistry and Radiopharmacy in Radiology, Weill Cornell Medicine, Cornell University, New York, NY, USA

    Shankar Vallabhajosula

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Vallabhajosula, S. (2023). Radiopharmaceuticals for Therapy. In: Molecular Imaging and Targeted Therapy. Springer, Cham. https://doi.org/10.1007/978-3-031-23205-3_17

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