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

Liolios, Christos; Sachpekidis, Christos; Schäfer, Martin; Kopka, Klaus

doi:10.1002/jlcr.3749

Cited by 13 publications

(13 citation statements)

References 66 publications

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“…However, in order to overcome this limitation, and increase specificity and sensitivity of the imaging method, the heterodimers approach has been described for a combination of various targets [ 169 , 170 ]. Specifically, heterodimers (Hd) targeting PSMA/GRPr have been recently reviewed by Liolios et al [ 171 ]. The first reported heterodimer targeting both PSMA and GRPr consisted of the acyclic chelator HBED-CC, which was linked to either side via its two carboxylic groups not participating at the complexation of the radiometal with the Lys-CO-Glu-OH PSMA binding motif and the GRPr agonist H 2 N-PEG 2 -[ D -Tyr 6 , beta -Ala 11 ,Thi 13 ,Nle 14 )BN(6–14) [ 172 ].…”

Section: Multitargeted Psma Inhibitorsmentioning

confidence: 99%

Radiolabeled PSMA Inhibitors

Neels

Kopka

Liolios

et al. 2021

Cancers

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PSMA has shown to be a promising target for diagnosis and therapy (theranostics) of prostate cancer. We have reviewed developments in the field of radio- and fluorescence-guided surgery and targeted photodynamic therapy as well as multitargeting PSMA inhibitors also addressing albumin, GRPr and integrin αvβ3. An overview of the regulatory status of PSMA-targeting radiopharmaceuticals in the USA and Europe is also provided. Technical and quality aspects of PSMA-targeting radiopharmaceuticals are described and new emerging radiolabeling strategies are discussed. Furthermore, insights are given into the production, application and potential of alternatives beyond the commonly used radionuclides for radiolabeling PSMA inhibitors. An additional refinement of radiopharmaceuticals is required in order to further improve dose-limiting factors, such as nephrotoxicity and salivary gland uptake during endoradiotherapy. The improvement of patient treatment achieved by the advantageous combination of radionuclide therapy with alternative therapies is also a special focus of this review.

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Section: Multitargeted Psma Inhibitorsmentioning

confidence: 99%

Radiolabeled PSMA Inhibitors

Neels

Kopka

Liolios

et al. 2021

Cancers

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“…Within the last 10 to 15 years, the approach to combine different receptor-specific peptides to one heterodimeric radioligand to improve tumor targeting emerged, yielding several agents with improvable tumor imaging characteristics but also other ones demonstrating high potential [69][70][71][72][73]. Over the last five years, the number of agents considerably increased, showing the growing interest in the field of heterobivalent peptides for tumor targeting.…”

Section: Radiolabeled Peptidic Heterodimers Developed For Improved Tumentioning

confidence: 99%

Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy

et al. 2020

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Over the past few years, an approach emerged that combines different receptor-specific peptide radioligands able to bind different target structures on tumor cells concomitantly or separately. The reason for the growing interest in this special field of radiopharmaceutical development is rooted in the fact that bispecific peptide heterodimers can exhibit a strongly increased target cell avidity and specificity compared to their corresponding monospecific counterparts by being able to bind to two different target structures that are overexpressed on the cell surface of several malignancies. This increase of avidity is most pronounced in the case of concomitant binding of both peptides to their respective targets but is also observed in cases of heterogeneously expressed receptors within a tumor entity. Furthermore, the application of a radiolabeled heterobivalent agent can solve the ubiquitous problem of limited tumor visualization sensitivity caused by differential receptor expression on different tumor lesions. In this article, the concept of heterobivalent targeting and the general advantages of using radiolabeled bispecific peptidic ligands for tumor imaging or therapy as well as the influence of molecular design and the receptors on the tumor cell surface are explained, and an overview is given of the radiolabeled heterobivalent peptides described thus far.

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“…Generally, with β − emitters, it necessitates the specific attachment of several hundred radiotracers to the targeted cell in order to be able to destroy it, whereas α-emitters, due to their high radiotoxicity, only need a few of them. Since several different receptors are likely to be conjointly overexpressed on cancer cells, multitargeting might be an elegant method for enhanced targeting [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

Clinical Advances and Perspectives in Targeted Radionuclide Therapy

Lepareur,

Ramée,

Mougin-Degraef

et al. 2023

Pharmaceutics

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Targeted radionuclide therapy has become increasingly prominent as a nuclear medicine subspecialty. For many decades, treatment with radionuclides has been mainly restricted to the use of iodine-131 in thyroid disorders. Currently, radiopharmaceuticals, consisting of a radionuclide coupled to a vector that binds to a desired biological target with high specificity, are being developed. The objective is to be as selective as possible at the tumor level, while limiting the dose received at the healthy tissue level. In recent years, a better understanding of molecular mechanisms of cancer, as well as the appearance of innovative targeting agents (antibodies, peptides, and small molecules) and the availability of new radioisotopes, have enabled considerable advances in the field of vectorized internal radiotherapy with a better therapeutic efficacy, radiation safety and personalized treatments. For instance, targeting the tumor microenvironment, instead of the cancer cells, now appears particularly attractive. Several radiopharmaceuticals for therapeutic targeting have shown clinical value in several types of tumors and have been or will soon be approved and authorized for clinical use. Following their clinical and commercial success, research in that domain is particularly growing, with the clinical pipeline appearing as a promising target. This review aims to provide an overview of current research on targeting radionuclide therapy.

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

Cited by 13 publications

References 66 publications

Radiolabeled PSMA Inhibitors

Radiolabeled PSMA Inhibitors

Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy

Clinical Advances and Perspectives in Targeted Radionuclide Therapy

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