A comparative PET imaging study of 44gSc- and 68Ga-labeled bombesin antagonist BBN2 derivatives in breast and prostate cancer models

Ferguson, Simon; Wuest, Melinda; Richter, Susan; Bergman, Cody; Dufour, Jennifer; Krys, Daniel; Simone, Jennifer; Jans, Hans-Soenke; Riauka, Terence; Wuest, Frank

doi:10.1016/j.nucmedbio.2020.10.005

Cited by 13 publications

(54 citation statements)

References 48 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Last but not least, one should report recent breakthroughs in the production of clinically appealing therapeutic radionuclides, including the Tb and Sc therapeutic isotopes and alpha emitters (Ac-225 and Bi-213), dynamically entering radiopharmaceutical development, and expected to soon upgrade the arsenal of anti-GRPR therapeutics with new powerful molecular tools [ 118 , 119 , 120 ].…”

Section: Newer Trends In the Application Of Anti-grpr Theranostic Radiopeptidesmentioning

confidence: 99%

Radiolabeled Bombesin Analogs

Mansi

Nock

Dalm³

et al. 2021

Cancers

View full text Add to dashboard Cite

The gastrin-releasing peptide receptor (GRPR) is expressed in high numbers in a variety of human tumors, including the frequently occurring prostate and breast cancers, and therefore provides the rationale for directing diagnostic or therapeutic radionuclides on cancer lesions after administration of anti-GRPR peptide analogs. This concept has been initially explored with analogs of the frog 14-peptide bombesin, suitably modified at the N-terminus with a number of radiometal chelates. Radiotracers that were selected for clinical testing revealed inherent problems associated with these GRPR agonists, related to low metabolic stability, unfavorable abdominal accumulation, and adverse effects. A shift toward GRPR antagonists soon followed, with safer analogs becoming available, whereby, metabolic stability and background clearance issues were gradually improved. Clinical testing of three main major antagonist types led to promising outcomes, but at the same time brought to light several limitations of this concept, partly related to the variation of GRPR expression levels across cancer types, stages, previous treatments, and other factors. Currently, these parameters are being rigorously addressed by cell biologists, chemists, nuclear medicine physicians, and other discipline practitioners in a common effort to make available more effective and safe state-of-the-art molecular tools to combat GRPR-positive tumors. In the present review, we present the background, current status, and future perspectives of this endeavor.

show abstract

Section: Newer Trends In the Application Of Anti-grpr Theranostic Radiopeptidesmentioning

confidence: 99%

Radiolabeled Bombesin Analogs

Mansi

Nock

Dalm³

et al. 2021

Cancers

View full text Add to dashboard Cite

show abstract

“…The early study by Koumarianou et al (Koumarianou et al 2011) was conducted on "cold" complexes with natural scandium and gallium. The binding affinity of both nat Sc-DOTATATE and nat Ga-DOTATATE in AR42J cell line was in the sub- (Ferguson et al 2020). In more recent studies, the binding affinity of nat Sc-PSMA-617 was evaluated in comparison to nat Ga-PSMA-617, however using different methods and cell lines (PC-3 PIP cells and PSMA+ LNCaP cells, respectively) (Umbricht et al 2017;Eppard et al 2017).…”

Section: Pre-clinical Studiesmentioning

confidence: 99%

Production of scandium radionuclides for theranostic applications: towards standardization of quality requirements

Mikołajczak

Huclier‐Markai

Alliot

et al. 2021

EJNMMI radiopharm. chem.

View full text Add to dashboard Cite

In the frame of “precision medicine”, the scandium radionuclides have recently received considerable interest, providing personalised adjustment of radiation characteristics to optimize the efficiency of medical care or therapeutic benefit for particular groups of patients. Radionuclides of scandium, namely scandium-43 and scandium-44 (43/44Sc) as positron emitters and scandium-47 (47Sc), beta-radiation emitter, seem to fit ideally into the concept of theranostic pair. This paper aims to review the work on scandium isotopes production, coordination chemistry, radiolabeling, preclinical studies and the very first clinical studies. Finally, standardized procedures for scandium-based radiopharmaceuticals have been proposed as a basis to pave the way for elaboration of the Ph.Eur. monographs for perspective scandium radionuclides.

show abstract

“…18 F is a radionuclide that has had increased focus for SSTR-targeting peptides [ 37 , 40 ]. It should be noted that other novel radiometals are currently in use and are continuously being investigated due to their similar advantages over 68 Ga, such as 64 Cu, 44 Sc and 89 Zr, with 64 Cu-DOTATOC and 64 Cu-DOTATATE currently being in clinical use as 68 Ga-DOTATOC and 68 Ga-DOTATATE alternatives [ 70 , 71 , 72 , 73 , 74 , 75 , 76 , 77 , 78 , 79 , 80 ]. These radiometals also provide attractive alternatives to 68 Ga PET imaging, although they are beyond the scope of this review.…”

Section: Peptidesmentioning

confidence: 99%

Recent Advances in the Clinical Translation of Silicon Fluoride Acceptor (SiFA) 18F-Radiopharmaceuticals

et al. 2021

View full text Add to dashboard Cite

The incorporation of silicon fluoride acceptor (SiFA) moieties into a variety of molecules, such as peptides, proteins and biologically relevant small molecules, has improved the generation of 18F-radiopharmaceuticals for medical imaging. The efficient isotopic exchange radiofluorination process, in combination with the enhanced [18F]SiFA in vivo stability, make it a suitable strategy for fluorine-18 incorporation. This review will highlight the clinical applicability of [18F]SiFA-labeled compounds and discuss the significant radiotracers currently in clinical use.

show abstract

A comparative PET imaging study of 44gSc- and 68Ga-labeled bombesin antagonist BBN2 derivatives in breast and prostate cancer models

Cited by 13 publications

References 48 publications

Radiolabeled Bombesin Analogs

Radiolabeled Bombesin Analogs

Production of scandium radionuclides for theranostic applications: towards standardization of quality requirements

Recent Advances in the Clinical Translation of Silicon Fluoride Acceptor (SiFA) 18F-Radiopharmaceuticals

Contact Info

Product

Resources

About