Clinical translation of a PSMA inhibitor for 99m Tc-based SPECT

Ferro-Flores, Guillermina; Luna-Gutiérrez, Myrna; Ocampo‐García, Blanca; Santos-Cuevas, Clara; Azorín-Vega, Erika; Jiménez-Mancilla, Nallely; Orocio-Rodríguez, Emmanuel; Davanzo, Jenny; García-Pérez, Francisco O.

doi:10.1016/j.nucmedbio.2017.01.012

Cited by 57 publications

(40 citation statements)

References 20 publications

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“…The technology of 99m Tc-hydrazinonicotinyl was also applied in the development of a PSMA inhibitor for 99m Tc-based SPECT. Ferro-Flores et al [70] reported in vitro and in vivo studies of 99m Tc-EDDA-HYNIC-iPSMA demonstrating that this radiopharmaceutical could detect tumour and metastases of PCa as well as 68 Ga-PSMA-617. 99m Tc-EDDA-HYNIC-iPSMA was quickly prepared from a kit with radiochemical yield >95%.…”

Section: The Metal Fragments Approach In the Development Of New 99m Tmentioning

confidence: 99%

A Picture of Modern Tc-99m Radiopharmaceuticals: Production, Chemistry, and Applications in Molecular Imaging

2019

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Even today, techentium-99m represents the radionuclide of choice for diagnostic radio-imaging applications. Its peculiar physical and chemical properties make it particularly suitable for medical imaging. By the use of molecular probes and perfusion radiotracers, it provides rapid and non-invasive evaluation of the function, physiology, and/or pathology of organs. The versatile chemistry of technetium-99m, due to its multi-oxidation states, and, consequently, the ability to produce a variety of complexes with particular desired characteristics, are the major advantages of this medical radionuclide. The advances in technetium coordination chemistry over the last 20 years, in combination with recent advances in detector technologies and reconstruction algorithms, make SPECT’s spatial resolution comparable to that of PET, allowing 99mTc radiopharmaceuticals to have an important role in nuclear medicine and to be particularly suitable for molecular imaging. In this review the most efficient chemical methods, based on the modern concept of the 99mTc-metal fragment approach, applied to the development of technetium-99m radiopharmaceuticals for molecular imaging, are described. A specific paragraph is dedicated to the development of new 99mTc-based radiopharmaceuticals for prostate cancer.

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Section: The Metal Fragments Approach In the Development Of New 99m Tmentioning

confidence: 99%

A Picture of Modern Tc-99m Radiopharmaceuticals: Production, Chemistry, and Applications in Molecular Imaging

2019

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“…The first, 99m Tc-EDDA/HYNIC-iPSMA, developed by Ferro-Flores et al utilized ethylenediamine-N, N ″ -diacetic acid (EDDA) as a coligand for complexation. 141 They showed specific binding to PSMA on LNCaP cells by comparing blocked versus nonblocked settings and assessed their compound in a biodistribution study. The biodistribution study was carried out in athymic mice bearing LNCaP and PC-3 tumors.…”

Section: Technetium-99mmentioning

confidence: 99%

Targeting prostate cancer: Prostate‐specific membrane antigen based diagnosis and therapy

Wüstemann

Haberkorn

Babich

et al. 2018

Medicinal Research Reviews

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The high incidence rates of prostate cancer (PCa) raise demand for improved therapeutic strategies. Prostate tumors specifically express the prostate-specific membrane antigen (PSMA), a membrane-bound protease. As PSMA is highly overexpressed on malignant prostate tumor cells and as its expression rate correlates with the aggressiveness of the disease, this tumor-associated biomarker provides the possibility to develop new strategies for diagnostics and therapy of PCa. Major advances have been made in PSMA targeting, ranging from immunotherapeutic approaches to therapeutic small molecules. This review elaborates the diversity of PSMA targeting agents while focusing on the radioactively labeled tracers for diagnosis and endoradiotherapy. A variety of radionuclides have been shown to either enable precise diagnosis or efficiently treat the tumor with minimal effects to nontargeted organs. Most small molecules with affinity for PSMA are based on either a phosphonate or a urea-based binding motif. Based on these pharmacophores, major effort has been made to identify modifications to achieve ideal pharmacokinetics while retaining the specific targeting of the PSMA binding pocket. Several tracers have now shown excellent clinical usability in particular for molecular imaging and therapy as proven by the efficiency of theranostic approaches in current studies. The archetypal expression profile of PSMA may be exploited for the treatment with alpha emitters to break radioresistance and thus to bring the power of systemic therapy to higher levels.

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“…Molar activity for the above compounds was between 25 and 333.3 MBq/nmol. 28,44 In a recent study, a similar approach was followed by coupling the iPSMA (PSMA inhibitor) (2-Nal-Lys-CO-Glu-OH) 55 with DOTA (1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid) (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and combining it with the Lys 3 -(1-14), agonist, (iPSMA-BN) 6 (Scheme 2). 46,47,56 The Lys 3 -BN peptide was conjugated to the N-γmaleimidobutyl-oxysuccinimidyl ester moiety at the Lys 3 and then coupled to Glu-CO-Lys-2-Nal-Cys-DOTA through the formation of a thioether with the Cys residue.…”

Section: Synthesis and Radiolabelingmentioning

confidence: 99%

Bispecific radioligands targeting prostate‐specific membrane antigen and gastrin‐releasing peptide receptors on the surface of prostate cancer cells

Liolios

Sachpekidis

Schäfer

et al. 2019

Labelled Comp Radiopharmac

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Metastases of prostate cancer usually show highly heterogeneous or partly lost prostate-specific membrane antigen (PSMA) expression. In order to image and treat both PSMA positive and negative tissues, the extension of PSMA tracer specificity to other receptors, also highly expressed on the surface of prostate cancer cells, has been suggested. Prostate cancer cells usually express both PSMA and gastrin-releasing peptide (GRP) receptors; thus, bispecific heterodimeric molecules, addressing both targets at the same time, may significantly improve prostate cancer imaging and therapy. This article summarizes preclinical data regarding low-molecular weight molecules targeting PSMA and GRP receptors.

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Clinical translation of a PSMA inhibitor for 99m Tc-based SPECT

Cited by 57 publications

References 20 publications

A Picture of Modern Tc-99m Radiopharmaceuticals: Production, Chemistry, and Applications in Molecular Imaging

A Picture of Modern Tc-99m Radiopharmaceuticals: Production, Chemistry, and Applications in Molecular Imaging

Targeting prostate cancer: Prostate‐specific membrane antigen based diagnosis and therapy

Bispecific radioligands targeting prostate‐specific membrane antigen and gastrin‐releasing peptide receptors on the surface of prostate cancer cells

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