Abstract
In the era of personalized medicine, “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 pathway-targeted 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 (223Ra-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.
Abbreviations
- [211At]SAPC:
-
N-succinimidyl 5-[211At]astato-3-pyridinecarboxylate
- ALP:
-
Alkaline phosphatase
- BBN:
-
Bombesin
- BsMAb:
-
Bispecific monoclonal antibody
- CAIX:
-
Carbonic anhydrase isoenzyme 9
- ccRCC:
-
Clear-cell renal carcinoma
- CEA:
-
Carcinoembryonic antigen
- CI:
-
Confidence interval
- DOTA:
-
2-(4-isothiocyanatobenzyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (macrocyclic coupling agent to label compounds of biological interest with metal radionuclides)
- EBRT:
-
External beam radiation therapy
- ECM:
-
Extracellular matrix
- EMEA:
-
European Medicines Agency
- ETDMP:
-
Ethylenediamine tetra(methylene phosphonic acid)
- FDA:
-
Food and Drug Administration of the United States of America
- FN:
-
Fibronectin
- GA:
-
Arabic glycoprotein
- HA:
-
Hydroxyapatite
- HAMA:
-
Human anti-mouse antibody
- HER2:
-
Human epidermal growth factor receptor 2, also known as receptor tyrosine-protein kinase erbB-2, or HER2/neu
- HSG:
-
Histaminesuccinyl-glutamine hapten
- L-19 SIP:
-
Small immunoreactive protein, (scFv)2, derived from monoclonal antibody L19
- L-19:
-
Monoclonal antibody recognizing the EDB domain of fibronectin
- MAA:
-
Macroaggregated albumin
- mAb:
-
Monoclonal antibody
- mCRPC:
-
Metastatic castrate-resistant prostate cancer
- MIBG:
-
Metaiodobenzyilguanidine
- MTA-1:
-
Metastasis-associated protein encoded by the MTA1 gene
- MTC:
-
Medullary thyroid cancer
- MTD:
-
Maximum tolerated dose
- MTRD:
-
Maximum tolerated radiation dose
- MX35:
-
A monoclonal antibody recognizing the sodium dependent phosphate transport protein 2b
- NaPi2b:
-
Sodium-dependent phosphate transport protein 2b
- NCA:
-
No-carrier-added
- NHL:
-
Non-Hodgkin’s lymphoma
- PAI2-uPAR:
-
Proteases, members of the urokinase-type plasminogen activator family
- PCa:
-
Prostatic carcinoma
- PET:
-
Positron emission tomography
- PRRT:
-
Peptide receptor radionuclide therapy
- PSA:
-
Prostate-specific antigen
- PSMA:
-
Prostate-specific membrane antigen
- RE:
-
Radioembolization
- RIT:
-
Radioimmunotherapy
- SCID:
-
Severe combined immunodeficiency
- SPECT:
-
Single-photon emission computed tomography
- SRE:
-
Skeletal-related event
- TAT:
-
Targeted alpha therapy
- TCMC:
-
2-(4-isothiocyanatobenzyl-1,4,7,10-tetraaza-1,4,7,10-tetra-(2-carbamonylmetyl)-cyclododecane (macrocyclic coupling agent to label compounds of biological interest with metal radionuclides)
- Theranostic:
-
An agent with both diagnostic and therapeutic capabilities (e.g., 131I-iodide – in low activity it is a diagnostic agent, in high activity it is a therapeutic agent)
- TROP-2:
-
Cell-surface glycoprotein overexpressed in adenocarcinomas, correlated with tumor aggressiveness
- TRT:
-
Targeted radionuclide therapy
- VGEF:
-
Vascular endothelial growth factor
- WHO:
-
World Health Organization
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Guidoccio, F., Mazzarri, S., Orsini, F., Erba, P.A., Mariani, G. (2016). Novel Radiopharmaceuticals for Therapy. In: Strauss, H., Mariani, G., Volterrani, D., Larson, S. (eds) Nuclear Oncology. Springer, Cham. https://doi.org/10.1007/978-3-319-26067-9_36-1
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Novel Radiopharmaceuticals for Therapy- Published:
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DOI: https://doi.org/10.1007/978-3-319-26067-9_36-2
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DOI: https://doi.org/10.1007/978-3-319-26067-9_36-1