Radiometals for Combined Imaging and Therapy

Cutler, Cathy S.; Hennkens, Heather M.; Sisay, Nebiat; Huclier‐Markai, Sandrine; Jurisson, Silvia S.

doi:10.1021/cr3003104

Cited by 346 publications

(281 citation statements)

References 171 publications

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“…Over the last several years, the 177 Lu radionuclide has attracted considerable attention and exhibited great promise in the research, commercial and clinical communities for use in a variety of therapeutic procedures [1][2][3][4][5][6][7][8]. Despite being a late entrant, 177 Lu has not only consolidated its potential, but also established a strong foothold at the forefront of TRT.…”

Section: Introductionmentioning

confidence: 99%

“…The in vivo applications of key 177 Lu radiopharmaceuticals for a variety of therapeutic procedures include peptide receptor radionuclide therapy [11][12][13][14][15][16][17][18][19][20][21][22][23][24][25][26], bone pain palliation [27][28][29][30][31][32][33], radiation synovectomy [34][35][36][37][38][39] and radioimmonutherapy [40][41][42][43][44][45][46]. There is a steadily expanding list of 177 Lu-labeled radiopharmaceuticals that is currently being evaluated at the preclinical research or at product development stages; these may potentially be used in vivo in humans for evaluation for radionuclide therapy [1][2][3]. A summary of key 177 Lu-labeled radiopharmaceuticals currently used in TRT is depicted in Table 1.…”

Section: Introductionmentioning

confidence: 99%

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Production of 177Lu for Targeted Radionuclide Therapy: Available Options

Dash

Pillai²,

Knapp

2015

Nucl Med Mol Imaging

239

166

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Background: This review provides a comprehensive summary of the production of 177 Lu to meet expected future research and clinical demands. Availability of options represents the cornerstone for sustainable growth for the routine production of adequate activity levels of 177 Lu having the required quality for preparation of a variety of 177 Lu-labeled radiopharmaceuticals. The tremendous prospects associated with production of 177 Lu for use in targeted radionuclide therapy (TRT) dictate that a holistic consideration should evaluate all governing factors that determine its success. Methods: While both "direct" and "indirect" reactor production routes offer the possibility for sustainable 177 Lu availability, there are several issues and challenges that must be considered to realize the full potential of these production strategies. Results: This article presents a mini review on the latest developments, current status, key challenges and possibilities for the near future. Conclusion: A broad understanding and discussion of the issues associated with 177 Lu production and processing approaches would not only ensure sustained growth and future expansion for the availability and use of 177 Lu-labeled radiopharmaceuticals, but also help future developments.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Production of 177Lu for Targeted Radionuclide Therapy: Available Options

Dash

Pillai²,

Knapp

2015

Nucl Med Mol Imaging

239

166

View full text Add to dashboard Cite

show abstract

“…I-131 tositumomab or Y-90 ibritumomab), as well as diagnostic agents for non-invasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging (e.g. In-111 Capromab pendetide or In-111 pentetreotide) [9,10] and playing an important role in cancer management as a form of personalized medicine [9,11].…”

Section: Introductionmentioning

confidence: 99%

Analytical characterization of NOTA-modified somatropins

Bracke

Wynendaele

D׳Hondt

et al. 2014

Journal of Pharmaceutical and Biomedical Analysis

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Highlights• NOTA-labeled somatropins were synthesized using different NOTA:protein ratios.• Direct LC-MS and CE-MS approaches indicated multiple substitution degrees.• Bottom-up approaches gave structural insights and information on the labeling yield.• Lys-70 (in silico calculated pKa of 8.3) is the NOTA-modification hotspot.• We report a synthesis procedure for the production of target-specific radiopharmaceuticals.

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“…For non-metal isotope F-18 (t 1/2 1.8 h), as well as C-11 (t 1/2 20.4 min), bifunctional prosthetic groups are installed on the peptide allowing conjugation to the biologically relevant peptide [15][16][17][18][19]. Present peptide radiolabeling techniques require structural modification of the lead structure, consequently influencing the pharmacokinetics, receptor affinity, and/or selectivity, usually in a negative manner [12,16].…”

Section: Introductionmentioning

confidence: 99%

From Carbon-11-Labeled Amino Acids to Peptides in Positron Emission Tomography: the Synthesis and Clinical Application

et al. 2018

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Radiolabeled amino acids, their derivatives and peptides have a broad scope of application and can be used as receptor ligands, as well as enzyme substrates for many different diseases as radiopharmaceutical tracers. Over the past few decades, the application of molecular imaging techniques such as positron emission tomography (PET) has gained considerable importance and significance in diagnosis in today's advanced health care. Next to that, the availability of cyclotrons and state-of-the-art radiochemistry facilities has progressed the production of imaging agents enabling the preparation of many versatile PET radiotracers. Due to many favorable characteristics of radiolabeled amino acids and peptides, they can be used for tumor staging and monitoring the progress of therapy success, while aromatic amino acids can be employed as PET tracer to study neurological disorders. This review provides a comprehensive overview of radiosynthetic and enzymatic approaches towards carbon-11 amino acids, their analogues and peptides, with focus on stereoselective reactions, and reflects upon their clinical application.

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Radiometals for Combined Imaging and Therapy

Cited by 346 publications

References 171 publications

Production of 177Lu for Targeted Radionuclide Therapy: Available Options

Production of 177Lu for Targeted Radionuclide Therapy: Available Options

Analytical characterization of NOTA-modified somatropins

From Carbon-11-Labeled Amino Acids to Peptides in Positron Emission Tomography: the Synthesis and Clinical Application

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