In the era of personalizedmedicine, "target radionuclide therapy" (TRT) is designed to damage only the cancerous cells while sparing unnecessary damage to the adjacent healthy cells/tissues. Unlike conventional external beam radiation therapy, TRT is intended to cause less or no collateral damage to normal tissues, as it aims at achieving targeted drug delivery either to a clinically diagnosed cancer not amenable to surgery or to metastatic tumor cells and tumor cell clusters, thus providing systemic therapy of cancer. Currently there are hundreds of new pathwaytargeted anticancer agents undergoing phase II and phase III clinical trials. TRT is just one type within the domain of "targeted therapies." In addition to the effective targeted radiopharmaceuticals already well validated for routine clinical use, newer radiolabeled agents are still in the phase of either preclinical or clinical validation. This chapter describes the main physical and radiochemical characteristics of radionuclides that have potential or have already been employed to label biologically reactive molecules for the development of novel radiopharmaceuticals for therapy. Some of these agents have entered advanced clinical trials in tumor-bearing patients. Results of these clinical trials cover a wide spectrum of potential clinical usefulness. The chapter is divided into two main parts depending on the type of particle emission (α- or β-associated or not with the emission of either γ- or β+-radiation). Within each domain, there is some exchange of experience and shift of focus in the various phases of development, depending on the modalities of ascertaining efficient tumor targeting according to the principles of theranostics. The example of a novel α-emitting radiopharmaceutical that has most recently achieved approval by regulatory agencies for clinical use ( 223 Ra-dichloride) is presented in detail as the paradigm for an agent that is showing a survival advantage besides the original target of pain palliation from bone metastases.

Novel radiopharmaceuticals for therapy

Erba P. A.;
2017-01-01

Abstract

In the era of personalizedmedicine, "target radionuclide therapy" (TRT) is designed to damage only the cancerous cells while sparing unnecessary damage to the adjacent healthy cells/tissues. Unlike conventional external beam radiation therapy, TRT is intended to cause less or no collateral damage to normal tissues, as it aims at achieving targeted drug delivery either to a clinically diagnosed cancer not amenable to surgery or to metastatic tumor cells and tumor cell clusters, thus providing systemic therapy of cancer. Currently there are hundreds of new pathwaytargeted anticancer agents undergoing phase II and phase III clinical trials. TRT is just one type within the domain of "targeted therapies." In addition to the effective targeted radiopharmaceuticals already well validated for routine clinical use, newer radiolabeled agents are still in the phase of either preclinical or clinical validation. This chapter describes the main physical and radiochemical characteristics of radionuclides that have potential or have already been employed to label biologically reactive molecules for the development of novel radiopharmaceuticals for therapy. Some of these agents have entered advanced clinical trials in tumor-bearing patients. Results of these clinical trials cover a wide spectrum of potential clinical usefulness. The chapter is divided into two main parts depending on the type of particle emission (α- or β-associated or not with the emission of either γ- or β+-radiation). Within each domain, there is some exchange of experience and shift of focus in the various phases of development, depending on the modalities of ascertaining efficient tumor targeting according to the principles of theranostics. The example of a novel α-emitting radiopharmaceutical that has most recently achieved approval by regulatory agencies for clinical use ( 223 Ra-dichloride) is presented in detail as the paradigm for an agent that is showing a survival advantage besides the original target of pain palliation from bone metastases.
2017
Guidoccio, F.; Mazzarri, S.; Orsini, F.; Erba, P. A.; Mariani, G.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/995767
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