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Novel Positron-Emitting Radiopharmaceuticals

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Nuclear Oncology

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Abstract

In recent decades, radiopharmaceuticals – particularly those for PET imaging – have become vital clinical tools in oncology. In this chapter, we seek to provide a bird’s-eye view of the current landscape of emergent PET radiopharmaceuticals, specifically those that have been the subject of multiple clinical trials but have yet to be approved by regulatory agencies for routine use. We will begin with a brief discussion of the fundamental anatomy of radiopharmaceuticals and then embark upon detailed examinations of several agents designed to facilitate the imaging of the aberrant amino acid transport, cellular metabolism, lipid biosynthesis, and cell surface receptors of malignant tissues. Particular focus will be dedicated to the early phase clinical trials in which these radiopharmaceuticals have been employed. This chapter will conclude with an examination of a particularly exciting recent trend in nuclear medicine: the advent of radiotheranostics.

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Abbreviations

AACD:

Aromatic amino acid decarboxylase

AR:

Androgen receptor

ASCT:

Alanine-serine-cysteine transporter

BB2:

Bombesin receptor subtype-2

BB2r:

Bombesin receptor subtype-2

ChoK:

Choline kinase

CNS:

Central nervous system

COMT:

Catechol-o-methyl transferase

CT:

X-ray computed tomography

64Cu-ATSM:

64Cu-diacetyl-bis(N4-methylsemicarbazone)

DOTA:

1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid

DTPA:

Diethylenetriaminepentaacetic acid

ER:

Estrogen receptor

FAS:

Fatty acid synthase

[18F]DCFBC:

N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-4-[18F]fluorobenzyl-L-cysteine

[18F]FACBC:

anti-1-amino-3-18F-fluorocyclobutane-1-carboxylic acid

[18F]FDG:

2-[18F]fluoro-2-deoxyglucose

[18F]FDHT:

16ß-[18F]fluoro-5-dihydrotestosterone

[18F]FDOPA:

L-3,4-dihydroxy-6-[18F]fluorophenylalanine

[18F]FES:

16a-[18F]fluoro-17ß-estradiol

[18F]FET:

O-(2-18F-fluoroethyl)-L-tyrosine

[18F]FGln:

4-[18F]-(2S,4R)fluoroglutamine

[18F]FLT:

3′-deoxy-3′-[18F]fluorothymidine

[18F]FMISO:

[18F]-fluoromisonidazole, 1-fluoro-3-(2-nitroimidazol-1-yl)-propan-2-ol

[18F]RGD-K5:

[18F]flotegatide-RGD

18F-AH111585:

[18F]fluciclatide

18F-alfatide II:

[18F]AlF-NOTA-E[PEG4-c(RGDfk)]2

68Ga-PSMA-ligand:

Glu-urea-Lys-(Ahx)-[68Ga(HBED-CC)]

GRPr:

Gastrin-releasing peptide receptor

[123I]MIBG:

[123I]-meta-iodobenzylguanidine

IMRT:

Intensity-modulated radiation therapy

LAT1:

L-type amino acid transporter 1

MRI:

Magnetic resonance imaging

MTC:

Medullary thyroid cancer

mTOR:

Mammalian target of rapamycin

NET:

Neuroendocrine tumor

NSCLC:

Non-small cell lung cancer

OC:

Octreotide

PEG:

Polyethylene glycol

PET:

Positron emission tomography

PET/MRI:

Positron emission tomography/magnetic resonance imaging

PSA:

Prostate-specific antigen

PSMA:

Prostate-specific membrane antigen

RGD:

Arginine-glycine-aspartic acid

SHBG:

Steroid hormone-binding globulin

SPECT:

Single photon emission computed tomography

SSR:

Somatostatin receptor

SST:

Somatostatin

SSTr:

Somatostatin receptor

SUV:

Standardized uptake value

TATE:

Octreotate

TCA:

Tricarboxylic acid

TK:

Thymidine kinase

TOC:

Tyr3-octreotide

TTPmin:

Minimum time to peak

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Authors and Affiliations

  1. Department of Chemistry, Hunter College of the City University of New York, New York, NY, USA

    Outi Keinänen, Aaron G. Nash, Samantha M. Sarrett & Brian M. Zeglis

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

    Outi Keinänen, Aaron G. Nash, Samantha M. Sarrett, Jason S. Lewis & Brian M. Zeglis

  3. Department of Chemistry, University of Helsinki, Helsinki, Finland

    Outi Keinänen & Mirkka Sarparanta

  4. Ph.D. Program in Biochemistry, Graduate Center of the City University of New York, New York, NY, USA

    Samantha M. Sarrett & Brian M. Zeglis

  5. Program in Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, NY, USA

    Jason S. Lewis

  6. Department of Radiology, Weill Cornell Medical College, New York, NY, USA

    Jason S. Lewis & Brian M. Zeglis

  7. Department of Pharmacology, Weill Cornell Medical College, New York, NY, USA

    Jason S. Lewis

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  1. Outi Keinänen
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Editors and Affiliations

  1. Associate Professor and Director of Nuclear Medicine, University of Pisa, Pisa, Italy

    Duccio Volterrani

  2. Translational Research, Pisa University, PISA, Pisa, Italy

    Paola A. Erba

  3. Attending Emeritus, Memorial Sloan-Kettering Cancer Center Dept. Radiology, New York, NY, USA

    H. William Strauss

  4. Professor Emeritus, University of Pisa, Pisa, Italy

    Giuliano Mariani

  5. Attending Physician, Memorial Sloan-Kettering Cancer Center, New York, NY, USA

    Steven M. Larson

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Keinänen, O., Nash, A.G., Sarrett, S.M., Sarparanta, M., Lewis, J.S., Zeglis, B.M. (2022). Novel Positron-Emitting Radiopharmaceuticals. In: Volterrani, D., Erba, P.A., Strauss, H.W., Mariani, G., Larson, S.M. (eds) Nuclear Oncology. Springer, Cham. https://doi.org/10.1007/978-3-319-26067-9_87-3

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  • DOI: https://doi.org/10.1007/978-3-319-26067-9_87-3

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  1. Latest

    Novel Positron-Emitting Radiopharmaceuticals
    Published:
    16 July 2022

    DOI: https://doi.org/10.1007/978-3-319-26067-9_87-3

  2. Novel Positron Emitting Radiopharmaceuticals
    Published:
    23 November 2016

    DOI: https://doi.org/10.1007/978-3-319-26067-9_87-2

  3. Original

    Emerging Radiopharmaceuticals in Clinical Oncology
    Published:
    12 September 2016

    DOI: https://doi.org/10.1007/978-3-319-26067-9_87-1

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