Thematische Bibliographien / Peptide receptor radiolabelled therapy

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Auswahl der wissenschaftlichen Literatur zum Thema „Peptide receptor radiolabelled therapy“

Autor: Grafiati

Veröffentlicht am 22. Februar 2025

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Zeitschriftenartikel zum Thema "Peptide receptor radiolabelled therapy"

Chakraborty, Kushal, Jagannath Mondal, Jeong Man An, Jooho Park und Yong-Kyu Lee. „Advances in Radionuclides and Radiolabelled Peptides for Cancer Therapeutics“. Pharmaceutics 15, Nr. 3 (17.03.2023): 971. http://dx.doi.org/10.3390/pharmaceutics15030971.

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Radiopharmaceutical therapy, which can detect and treat tumours simultaneously, was introduced more than 80 years ago, and it has changed medical strategies with respect to cancer. Many radioactive radionuclides have been developed, and functional, molecularly modified radiolabelled peptides have been used to produce biomolecules and therapeutics that are vastly utilised in the field of radio medicine. Since the 1990s, they have smoothly transitioned into clinical application, and as of today, a wide variety of radiolabelled radionuclide derivatives have been examined and evaluated in various studies. Advanced technologies, such as conjugation of functional peptides or incorporation of radionuclides into chelating ligands, have been developed for advanced radiopharmaceutical cancer therapy. New radiolabelled conjugates for targeted radiotherapy have been designed to deliver radiation directly to cancer cells with improved specificity and minimal damage to the surrounding normal tissue. The development of new theragnostic radionuclides, which can be used for both imaging and therapy purposes, allows for more precise targeting and monitoring of the treatment response. The increased use of peptide receptor radionuclide therapy (PRRT) is also important in the targeting of specific receptors which are overexpressed in cancer cells. In this review, we provide insights into the development of radionuclides and functional radiolabelled peptides, give a brief background, and describe their transition into clinical application.

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Allott, Louis, Suraiya Dubash und Eric O. Aboagye. „[18F]FET-βAG-TOCA: The Design, Evaluation and Clinical Translation of a Fluorinated Octreotide“. Cancers 12, Nr. 4 (02.04.2020): 865. http://dx.doi.org/10.3390/cancers12040865.

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The success of Lutathera™ ([177Lu]Lu-DOTA-TATE) in the NETTER-1 clinical trial as a peptide receptor radionuclide therapy (PRRT) for somatostatin receptor expressing (SSTR) neuroendocrine tumours (NET) is likely to increase the demand for patient stratification by positron emission tomography (PET). The current gold standard of gallium-68 radiolabelled somatostatin analogues (e.g., [68Ga]Ga-DOTA-TATE) works effectively, but access is constrained by the limited availability and scalability of gallium-68 radiopharmaceutical production. The aim of this review is three-fold: firstly, we discuss the peptide library design, biological evaluation and clinical translation of [18F]fluoroethyltriazole-βAG-TOCA ([18F]FET-βAG-TOCA), our fluorine-18 radiolabelled octreotide; secondly, to exemplify the potential of the 2-[18F]fluoroethylazide prosthetic group and copper-catalysed azide-alkyne cycloaddition (CuAAC) chemistry in accessing good manufacturing practice (GMP) compatible radiopharmaceuticals; thirdly, we aim to illustrate a framework for the translation of similarly radiolabelled peptides, in which in vivo pharmacokinetics drives candidate selection, supported by robust radiochemistry methodology and a route to GMP production. It is hoped that this review will continue to inspire the development and translation of fluorine-18 radiolabelled peptides into clinical studies for the benefit of patients.

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Krenning, E. P., M. de Jong, P. P. M. Kooij, W. A. P. Breeman, W. H. Bakker, W. W. de Herder, C. H. J. van Eijck et al. „Radiolabelled somatostatin analogue(s) for peptide receptor scintigraphy and radionuclide therapy“. Annals of Oncology 10 (1999): S23—S30. http://dx.doi.org/10.1093/annonc/10.suppl_2.s23.

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Bodei, Lisa, Chiara M. Grana, Mirco Bartolomei, Silvia M. Baio, Maribel Lopera Sierra und Giovanni Paganelli. „Peptide receptor radionuclide therapy with radiolabelled somatostatin analogues: ten years experience“. Biomedicine & Pharmacotherapy 62, Nr. 8 (Oktober 2008): 524. http://dx.doi.org/10.1016/j.biopha.2008.07.082.

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Laudicella, Riccardo, Domenico Albano, Salvatore Annunziata, Diletta Calabrò, Giovanni Argiroffi, Elisabetta Abenavoli, Flavia Linguanti et al. „Theragnostic Use of Radiolabelled Dota-Peptides in Meningioma: From Clinical Demand to Future Applications“. Cancers 11, Nr. 10 (22.09.2019): 1412. http://dx.doi.org/10.3390/cancers11101412.

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Meningiomas account for approximately 30% of all new diagnoses of intracranial masses. The 2016 World Health Organization’s (WHO) classification currently represents the clinical standard for meningioma’s grading and prognostic stratification. However, watchful waiting is frequently the chosen treatment option, although this means the absence of a certain histological diagnosis. Consequently, MRI (or less frequently CT) brain imaging currently represents the unique available tool to define diagnosis, grading, and treatment planning in many cases. Nonetheless, these neuroimaging modalities show some limitations, particularly in the evaluation of skull base lesions. The emerging evidence supporting the use of radiolabelled somatostatin receptor analogues (such as dota-peptides) to provide molecular imaging of meningiomas might at least partially overcome these limitations. Moreover, their potential therapeutic usage might enrich the current clinical offering for these patients. Starting from the strengths and weaknesses of structural and functional neuroimaging in meningiomas, in the present article we systematically reviewed the published studies regarding the use of radiolabelled dota-peptides in surgery and radiotherapy planning, in the restaging of treated patients, as well as in peptide-receptor radionuclide therapy of meningioma.

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Van Essen, Martijn, Eric P. Krenning, Marion De Jong, Roelf Valkema und Dik J. Kwekkeboom. „Peptide Receptor Radionuclide Therapy with radiolabelled somatostatin analogues in patients with somatostatin receptor positive tumours“. Acta Oncologica 46, Nr. 6 (Januar 2007): 723–34. http://dx.doi.org/10.1080/02841860701441848.

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Reismann, Péter, Zoltán Kender, Gabriella Dabasi, Lídia Sréter, Károly Rácz und Péter Igaz. „Somatostatin receptor endoradiotherapy of neuroendocrine tumors: experience in Hungarian patients“. Orvosi Hetilap 152, Nr. 10 (März 2011): 392–97. http://dx.doi.org/10.1556/oh.2011.29057.

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Beside conventional therapies for the treatment of neuroendocrine tumors, a new therapeutical approach, peptide receptor radionuclide therapy has been developed recently. There are two important features which make this therapy feasible: somatostatin receptors are strongly over-expressed in most neuroendocrine tumors resulting in a high tumor-to-background ratio and internalization of the somatostatin-receptor complex in neuroendocrine cells. Due to these features, neuroendocrine tumors can be treated with radiolabelled somatostatin analogues. For peptide receptor radionuclide therapy, somatostatin analogues are conjugated to a chelator that can bind a radionuclide. The most frequently used radionuclides for neuroendocrine tumor treatment are the β-emitter Yttrium-90 (90Y) and the β+γ emitter Lutetium-177 (177Lu). Candidates for somatostatin receptor endoradiotherapy are patients with progressive, metastatic, somatostatin-receptor positive neuroendocrine tumors. Many patients have been successively treated with this approach: according to international results major remission can be achieved in 25% of the cases. Although this therapy is still unavailable in Hungary, Hungarian patients can be treated with somatostatin receptor endoradiotherapy with financial support from the National Health Fund in a co-operation with the University of Basel since 2005. During the past 5 years, 51 Hungarian patients have been treated with this therapy. This review briefly summarizes the theoretical background, indications, effectiveness and side effects of somatostatin receptor endoradiotherapy and the authors present the first data obtained from Hungarian patients. Orv. Hetil., 2011, 152, 392–397.

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Judmann, Benedikt, Diana Braun, Björn Wängler, Ralf Schirrmacher, Gert Fricker und Carmen Wängler. „Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy“. Pharmaceuticals 13, Nr. 8 (30.07.2020): 173. http://dx.doi.org/10.3390/ph13080173.

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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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Pattison, David A., und Rodney J. Hicks. „Molecular imaging in the investigation of hypoglycaemic syndromes and their management“. Endocrine-Related Cancer 24, Nr. 6 (Juni 2017): R203—R221. http://dx.doi.org/10.1530/erc-17-0005.

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There has been recent progress in molecular imaging using a variety of cellular targets for the investigation of adult non-diabetic hypoglycaemic syndromes and its integration into patient management. These targets include peptide receptors (somatostatin receptors (SSTRs) and glucagon-like peptide-1 receptor (GLP-1R)) the amine precursor uptake and decarboxylation system utilising the diphydroxyphenylaline (DOPA) analogue 6-[18F]-l-fluoro-l-3,4-dihydroxyphenylalanine (18F-FDOPA), and glycolytic metabolism with 2-[18F]fluoro-2-deoxy-d-glucose (FDG). Accurate preoperative localisation and staging is critical to enable directed surgical excision or enucleation with minimal morbidity and preservation of residual pancreatic function. Benign insulinoma has near ubiquitous dense GLP-1R expression enabling accurate localisation with radiolabelled-exendin-4 compounds (e.g.68Ga-NOTA-exendin-4 PET/CT), whilst the rarer and more difficult to manage metastatic insulinoma typically express SSTR and is preferably imaged with radiolabelled-SSTR analogues such as68Ga-DOTA-octreotate (DOTATATE) PET/CT for staging and assessment of suitability for peptide receptor radionuclide therapy (PRRT). Similar to other metastatic neuroendocrine tumours, FDG PET/CT is used in the setting of higher-grade metastatic insulinoma to provide important prognostic information that can guide treatment and determine suitability for PRRT. Interestingly, these three tracers appear to represent a spectrum of differentiation, which we conceptually describe as the ‘triple-flop’ phenomenon, with GLP-1R > SSTR > FDG in benign insulinoma and the opposite in higher-grade disease. This paper will review the clinical syndromes of adult hypoglycaemia (including a practical overview of the differential diagnoses to be considered), comparison of techniques for insulinoma localisation with emphasis on molecular imaging before discussing its implications for management of metastatic insulinoma.

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Trindade, Victoria, und Henia Balter. „Oxidant and Antioxidant Effects of Gentisic Acid in a 177Lu-Labelled Methionine-Containing Minigastrin Analogue“. Current Radiopharmaceuticals 13, Nr. 2 (03.08.2020): 107–19. http://dx.doi.org/10.2174/1874471012666190916112904.

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Background: The radiolabelling of receptor-binding peptides for therapy is a challenge since the peptide itself is exposed (during labelling, storage and transport) to radiation-induced damage, directly or indirectly, in aqueous solution. Hence, the use of radiostabilizers seems to be mandatory, especially in peptide molecules that contain radiation-sensitive amino acids. Objective: The aim of this study was to investigate the effect of two stabilizers, gentisic acid and methionine, to delve into how each of them affects the radiolabelling and stability of the minigastrin analogue [177Lu]Lu-DOTA-His-His-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 through the analysis of the 22 species distinguished over time by an optimized HPLC system. Methods: The stabilizers, in different combinations, were present from the beginning of the labelling process carried out at 96 °C for 15 min. The stability was studied for up to 7 days. Results: The unexpected selective oxidation of the methionine residue of the radiolabelled peptide, promoted by gentisic acid, led to studying the effect of pH, from 3.5 to 6.0, in the presence of only this stabilizer. A pH-dependent antioxidant behaviour was revealed, showing a decrease in peptide impurities but an increase in the selective oxidation as the pH was increased. Conclusion: The selective oxidation of the methionine residue could be induced by oxidizing species probably produced in the reaction between gentisic acid and free radicals of water, during the protection of the radiolabelled peptide from the attack of these harmful species. Therefore, the addition of methionine becomes necessary to effectively decrease this selective oxidation in the methioninecontaining peptide.

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Dissertationen zum Thema "Peptide receptor radiolabelled therapy"

Tran, Sophie. „Evaluation de la radiothérapie interne vectorisée augmentée par ultrasons et optimisation de son efficacité par imagerie TEP“. Electronic Thesis or Diss., université Paris-Saclay, 2024. http://www.theses.fr/2024UPAST183.

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Depuis plusieurs années, la radiothérapie interne vectorisée (RIV) est devenue une thérapie efficace dans la prise en charge des cancers de la prostate métastatique résistant à la castration, forme rare au pronostic très péjoratif. Cette approche théranostique se repose sur l'administration d'un médicament radiopharmaceutique (MRP), molécule vectrice radiomarquée qui cible spécifiquement l'antigène membranaire spécifique de la prostate (PSMA) surexprimée à la surface des cellules cancéreuses. Le MRP peut être à visée diagnostique permettant une imagerie TEP (tomographie par émission de positons) ou à visée thérapeutique délivrant localement un rayonnement ionisant, initiant des dégâts irréversibles au niveau de l'ADN des cellules tumorales et induisant leur mort. Malgré des résultats cliniques prometteurs, l'accès à la RIV reste limité et son application est réservé à des patients porteurs de tumeurs à un stade avancé de la pathologie. De plus, une accumulation non négligeable du MRP dans les organes d'élimination (e.g., rein, foie) et les organes du système immunitaire induit des effets indésirables impactant le bien être du patient. L'un des défis consiste à assurer une diffusion rapide dans toute la tumeur des agents de liaison tout en maintenant ou améliorant la fixation spécifique à la tumeur, afin de réduire les doses injectées. L'émission d'ondes ultrasonores combinée à l'injection intravasculaire de microbulles de gaz fournit des alternatives sans précédent comme méthode adjuvante pour la délivrance locale de molécules thérapeutiques. En effet, la vibration des microbulles sous l'effet des ultrasons entraîne une perméabilisation transitoire des barrières biologiques (e.g., barrière hémato-tumorale). Cette technique, appelée sono-perméabilisation potentialise l'extravasation de molécules thérapeutiques dans la région d'intérêt en augmentant leur biodisponibilité uniquement dans la zone où les ondes sont focalisées. L'objectif de la thèse est d'optimiser par TEP, la délivrance locale du MRP au sein de la tumeur de la prostate par sono-perméabilisation. Cette approche permettra de répondre aux questions cruciales de la diminution de la dose d'injection et donc de la radiotoxicité sur les organes sains pour aller vers une médecine du futur personnalisée et moins délétère pour le patient. Pour cela, des études in vitro ont été réalisées afin d'évaluer l'impact de la sono-perméabilisation sur la perméabilité membranaire. Les protocoles ultrasonores ont ainsi été validées sur deux modèles cellulaires : un modèle en suspension de cancer de la prostate métastatique (LNCaP) et un modèle perméabilité épithéliale (MDCKII-MDR1). L'impact de la sono- perméabilisation a été ensuite évaluée dans un modèle préclinique murin sous cutanée du cancer de la prostate. Cette étude in vivo a permis d'évaluer la biodistribution d'un MRP à usage diagnostique dans un premier temps ([¹⁸F]F-PSMA-1007), utilisé en routine clinique au sein de notre laboratoire par imagerie TEP/tomodensitométrie (TDM). Le dernier axe actuellement en cours est d'évaluer l'efficacité thérapeutique de la sono-perméabilisation combinée avec le MRP thérapeutique ([¹⁷⁷Lu]Lu-PSMA-617). Cet axe permettra de calculer par la suite la posologie optimale afin d'atteindre la dose thérapeutique efficace tout en minimisant l'accumulation du MRP dans les tissus sains. Ce projet pourrait ouvrir la voie à des études combinant la sono-perméabilisation avec d'autres traitements comme l'immunothérapie sur les tumeurs prostatiques ou encore des études cliniques pour évaluer l'efficacité de cette technique chez les patients
For several years, peptide receptor radiolabelled therapy (PRRT) has become an effective therapy for managing metastatic castration-resistant prostate cancer, a rare form with a very poor prognosis. This theranostic approach relies on the administration of a radiopharmaceutical (RP), a radiolabelled vector molecule that specifically targets the prostate-specific membrane antigen (PSMA) overexpressed on the surface of cancer cells. The RP can be diagnostic, allowing for PET imaging (positron emission tomography), or therapeutic, delivering ionizing radiation locally, causing irreversible damage to the DNA of tumor cells and inducing their death. Despite promising clinical results, access to VIRT remains limited, and its application is reserved for patients with advanced-stage tumors. Additionally, a significant accumulation of the RP in elimination organs (e.g., kidneys, liver) and immune system organs induces adverse effects impacting the patient's well-being. One challenge is ensuring rapid diffusion of binding agents throughout the tumor while maintaining or improving specific tumor binding to reduce injected doses. The emission of ultrasound waves combined with the intravascular injection of gas microbubbles provides unprecedented alternatives as an adjunctive method for the local delivery of therapeutic molecules. Indeed, the vibration of microbubbles under ultrasound induces transient permeabilization of biological barriers (e.g., the blood-tumor barrier). This technique, called sonopermabilization, enhances the extravasation of therapeutic molecules in the region of interest by increasing their bioavailability only where the waves are focused. The aim of the thesis is to optimize the local delivery of the RP within the prostate tumor using sonopermabilization through PET. This approach will address crucial questions regarding the reduction of injected doses and thus radiotoxicity to healthy organs, moving towards a future of personalized medicine that is less harmful to the patient. To achieve this, in vitro studies were conducted to evaluate the impact of sonopermabilization on membrane permeability. Ultrasound protocols were validated on two cellular models: a suspension model of metastatic prostate cancer (LNCaP) and an epithelial permeability model (MDCKII-MDR1). The impact of sonopermabilization was then evaluated in a preclinical murine subcutaneous model of prostate cancer. This in vivo study allowed for the assessment of the biodistribution of a diagnostic RP initially ([¹⁸F]F- PSMA-1007), routinely used in our laboratory for PET/computed tomography (CT) imaging. The latest focus is to evaluate the therapeutic efficacy of sonopermabilization combined with the therapeutic RP ([¹⁷⁷Lu]Lu-PSMA-617). This will subsequently allow for the calculation of the optimal dosage to achieve an effective therapeutic dose while minimizing accumulation of RP in healthy tissues. This project could pave the way for studies combining sonopermabilization with other treatments such as immunotherapy for prostate tumors, or clinical studies to evaluate the effectiveness of this technique in patients

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Yang, Liying. „Targeting Interleukin-4 Receptor α with Hybrid Peptide for Effective Cancer Therapy“. Kyoto University, 2014. http://hdl.handle.net/2433/188669.

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Teunissen, Jacobus Johannes Maria. „Endocrine tumours molecular radiation on target peptide receptor radionuclide therapy with lutetium-octreotate“. [S.l.] : Rotterdam : [The Author] ; Erasmus University [Host], 2008. http://hdl.handle.net/1765/14119.

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Wilson, Darren Jonathan. „Studies of the seven transmembrane domain thrombin receptor on human platelets and megakaryocytic cells“. Thesis, University College London (University of London), 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.264966.

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Kanai, Yugo. „Circulating osteocrin stimulates bone growth by limiting C-type natriuretic peptide clearance“. Kyoto University, 2018. http://hdl.handle.net/2433/232097.

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Woodbine, Donna-Beth. „Biological effects of anti-peptide antibodies against the her-2/neu receptor tyrosine kinase : implications for therapy of human breast cancer /“. The Ohio State University, 1997. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487948807587924.

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Smith, Simon Matthew Giles. „Investigations into the genetic basis of platelet responsiveness to adenosine diphosphate and thrombin receptor activating peptide, and the variable response to clopidogrel therapy“. Thesis, University of Sheffield, 2007. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.444830.

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Silva, Jefferson de Jesus. „Radiomarcação de inibidor de PSMA com 177Lu e avaliação biológica do potencial para aplicação no tratamento do câncer de próstata“. Universidade de São Paulo, 2017. http://www.teses.usp.br/teses/disponiveis/85/85131/tde-07122017-110519/.

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O câncer de próstata é considerado o segundo mais comum na população masculina em todo o mundo e ocupa a 15ª posição em mortes por câncer, em homens, representando cerca de 6% do total de mortes por câncer no mundo. O antígeno de membrana prostático específico (PSMA) é uma glicoproteína tipo II transmembrânica superexpressa no câncer de próstata, suas metástases e em neovascularizações relacionadas a tumores sólidos, que tem estimulado o desenvolvimento de pequenas moléculas inibidoras do receptor de PSMA, que carreguem agentes terapêuticos. Este trabalho pretendeu estudar de forma inédita a marcação e estabilidade radioquímica do Glu-NH-CO-NH-Lys(Ahx)-DOTA com 177Lu (PSMA-DOTA-177Lu) e avaliar seu potencial para a terapia do câncer de próstata. O radiofármaco foi obtido com pureza radioquímica elevada (PR > 95%) em todas as condições estudadas e permaneceu inalterada em ≤ - 20 °C até 48 horas, mesmo em atividade específica alta (74 MBq/μg). O ensaio de ligação específica do PSMADOTA- 177Lu mostrou que a fração do peptídeo que se ligou às células LNCaP de tumor de próstata foi de 1,79 ± 0,21 %, 2,47 ± 0,03 %, 3,07 ± 0,01 % e 4,13 ± 0,27%, para as concentrações de 0,15 x 106, 0,3 x 106, 0,5 x 106 e 1 x 106 células, respectivamente. O ensaio de internalização do PSMA-DOTA-177Lu sugere que o maior percentual da ligação específica do radiofármaco às células LNCaP corresponde à fração da ligação de superfície (99,03 ± 0,84 %). Os parâmetros farmacocinéticos determinados no estudo in vivo em camundongos Balb/c são compatíveis com o rápido clareamento sanguíneo e excreção renal, além de apresentar apreciável captação tumoral in vivo (2,76 ± 1,21 % Al/g) após 4 horas de administração do radiofármaco. Os estudos em estabilidade em soro humano demonstram estabilidade alta do radiofármaco PSMA-DOTA-177Lu por um período de até 24 horas, que foi confirmada pela baixa captação óssea demonstrada nos estudos in vivo de biodistribuição. O estudo de variação da atividade possibilitou estabelecer a atividade específica ideal (MBq/μg), que será extrapolada para um piloto de produção do radiofármaco. Os resultados favoráveis deste estudo encorajam a perspectiva de realização de ensaio clínico controlado deste novo radiofármaco, avaliando seu potencial para aplicação no tratamento do câncer de próstata.
Prostate cancer is the second most frequently worldwide diagnosed cancer among males and ranks the 15th common cause of death from cancer in men, comprising 6% of the world\'s total cancer deaths. The prostate specific membrane antigen (PSMA) is a type II transmembrane glycoprotein, which is overexpressed in prostate cancer as well as in the neovasculature of solid tumors and metastasis. These features render PSMA an ideal target for developing small molecules inhibitors of PSMA and therapeutic approaches to targeted drugs delivery. This work intended to study in an unprecedented way the radiochemical labeling and stability of Glu-NHCO- NH-Lys (Ahx)-DOTA with 177Lu (177Lu-PSMA-DOTA) and its potential anti-tumor effects in prostate cancer. The radiopharmaceutical PSMA-177Lu was obtained with high radiochemical purity (RP > 95%) under all studied conditions and remained unchanged up to 48 hours (high at ≤ -20 °C), even at high specific activity (74 MBq / μg). The cellular uptake of PSMA-DOTA-177Lu was determined using PSMAexpressing LNCaP cells and showed a binding of 1.79 ± 0.21%, 2.47 ± 0.03%, 3.07 ± 0.01% and 4.13 ± 0.27%, to 0.15 × 106, 0.3 × 106, 0.5 × 106 and 1 × 106 LNCaP cells, respectively. The PSMA-DOTA-177Lu internalization assay revealed that the membrane-bound activity (non-internalized peptide) to LNCap cells, was 99.03 ± 0.84%. Moreover, the pharmacokinetic in vivo studies performed in Scid mice resulted in a rapid blood clearance and renal excretion, and showed significant tumor uptake (2.76 ± 1.21% lA/g) 4 hours after PSMA-DOTA-177Lu administration. Stability studies in human serum demonstrated high PSMA-DOTA-177Lu stability over 24 hours, which is in agreement with the low bone uptake obtained in the in vivo biodistribution studies. Furthermore, the comparative study aiming to establish the ideal PSMA-DOTA-177Lu specific activity (MBq / μg) will be considered for further radiopharmaceutical production. The pre-clinical data obtained from this study suggested a great potential for PSMA-DOTA-177Lu to be included in clinical trials and to make a major contribution to the treatment of prostate cancer.

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Jiménez, Franco Luis David [Verfasser], und Frederik [Akademischer Betreuer] Wenz. „Development of a treatment planning algorithm for peptide-receptor radionuclide therapy considering multiple tumour lesions and organs at risk / Luis David Jiménez Franco ; Betreuer: Frederik Wenz“. Heidelberg : Universitätsbibliothek Heidelberg, 2018. http://d-nb.info/1177044692/34.

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Jin, Xifeng [Verfasser], und Christoph [Akademischer Betreuer] Auernhammer. „Novel strategies for targeted therapy in NETs : inhibition of Wnt signaling in neuroendocrine tumors and improving peptide receptor chemoradionuclide therapy (PRCRT) by a combination of 5-fluorouracil and epigenetic modifiers / Xifeng Jin ; Betreuer: Christoph Auernhammer“. München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2019. http://d-nb.info/1192663365/34.

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Bücher zum Thema "Peptide receptor radiolabelled therapy"

IAEA. Practical Guidance on Peptide Receptor Radionuclide Therapy (PRRNT) for Neuroendocrine Tumours. International Atomic Energy Agency, 2013.

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Wójcik-Gładysz, Anna. Ghrelin – hormone with many faces. Central regulation and therapy. The Kielanowski Institute of Animal Physiology and Nutrition, Polish Academy of Sciences, 2020. http://dx.doi.org/10.22358/mono_awg_2020.

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Discovered in 1999, ghrelin, is one of the peptides co-creating the hypothalamicgastrointestinal axis, otherwise known as the brain-gut axis. Ghrelin participates in many physiological processes and spectrum of its activity is still being discovered. This 28 amino acid peptide ‒ a product of the ghrl gene, was found in all vertebrates and is synthesized and secreted mainly from enteroendocrine X/A cells located in the gastric mucosa of the stomach. Expression of the ghrelin receptor has been found in many nuclei of the hypothalamus involved in appetite regulation. Therefore it’s presumed that ghrelin is one of the crucial hormones deciphering the energy status required for the maintenance of organism homeostasis. Ghrelin acts as a signal of starvation or energy insufficiency and its level in plasma is reduced after the meal. Neuropeptide Y (NPY) and agouti-related peptide (AgRP; NPY/AgRP) neurons located in the arcuate nucleus (ARC) area are the main target of ghrelin in the hypothalamus. This subpopulation of neurons is indispensable for inducing orexigenic action of ghrelin. Moreover ghrelin acting as a neurohormone, mainly in the hypothalamus area, plays an important role in the regulation of growth and reproduction processes. Indeed, ghrelin action on reproductive processes has been observed in the systemic effects exerted at both hypothalamus-pituitary and gonadal levels. Similarly the GH-releasing ghrelin action was observed both on the hypothalamus level and directly on the somatotrophic cells in the pituitary and this dose-related GH releasing activity was found in in vitro as well as in in vivo experiments. In recent years, numerous studies revealed that ghrelin potentially takes part in the treatment of diseases associated with serious disturbances in the organism energy balance and/or functioning of the gastrointestinal tract. It was underlined that ghrelin may be a hormone with a broad spectrum of therapeutic effect on obesity and anorexia nervosa, as well as may also have protective effect on neurodegenerative diseases, inflammatory disorders or functional changes in the body caused by cancers. In overall, ghrelin treatment has been tested in over 100 preclinical studies with healthy volunteers as well as patients with various types of cancer, eating disorders such as anorexia nervosa and bulimia nervosa. It was observed that ghrelin has an excellent clinical safety profile and emerging side effects occurred only in 3–10% of patients and did not constitute a sufficient premise to discontinue the therapy. In general, it can be concluded that ghrelin may be sufficiently used as a prescription drug.

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Macdougall, Iain C. Erythropoiesis-stimulating agents in chronic kidney disease. Herausgegeben von David J. Goldsmith. Oxford University Press, 2015. http://dx.doi.org/10.1093/med/9780199592548.003.0124.

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The advent of recombinant human erythropoietin (epoetin) in the late 1980s transformed the management of renal anaemia, liberating many dialysis patients from lifelong regular blood transfusions, in turn causing severe iron overload and human leucocyte antigen sensitization. Epoetin can be administered either intravenously or subcutaneously, but the half-life of the drug is fairly short at around 6–8 hours, necessitating frequent injections. To circumvent this problem, two manipulations to the erythropoietin molecule were engineered. The first of these was to attach an extra two carbohydrate chains to the therapeutic protein hormone (to make darbepoetin alfa), and the second was to attach a large pegylation chain to make continuous erythropoietin receptor activator. Both of these strategies prolonged the circulating half-life of the erythropoietin analogue. The next erythropoietic agent to be produced was peginesatide, a peptide-based agent which had no structural homology with native or recombinant erythropoietin, but shared the same biological and functional characteristics. Future strategies include stabilization of hypoxia-inducible factor, by orally active inhibitors of the prolyl hydroxylase enzyme, and advanced clinical trials are underway. In the meantime, several large randomized controlled trials have highlighted the potential harm in targeting a near normal haemoglobin of 13–14 g/dL (with an increased risk of cardiovascular complications), and sub-normal correction of anaemia is now advised. Some patients may show mild or severe resistance to erythropoiesis-stimulating agent (ESA) therapy, and common causes include iron insufficiency, infection, and underlying inflammation. Very rarely, patients may produce antibodies against their ESA, which neutralize not only the ESA, but also endogenous erythropoietin, causing pure red cell aplasia.

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Buchteile zum Thema "Peptide receptor radiolabelled therapy"

Wild, Damian. „Theranostics with Somatostatin Receptor Antagonists“. In Beyond Becquerel and Biology to Precision Radiomolecular Oncology: Festschrift in Honor of Richard P. Baum, 349–59. Cham: Springer International Publishing, 2024. http://dx.doi.org/10.1007/978-3-031-33533-4_35.

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AbstractSomatostatin receptors (SST), especially SST subtype 2 (SST2), are important targets for the management of patients with neuroendocrine tumours (NETs) or neuroendocrine neoplasias (NENs). Peptide receptor radionuclide therapy (PRRT) with 177Lu-labelled SST agonists, for example, 177Lu-DOTA-TOC or 177Lu-DOTA-TATE, is recommended by the European Neuroendocrine Tumour Society as second-line treatment after progression under treatment with somatostatin analogues in patients with metastatic, SST positive grade 1 and 2 midgut NETs. PET/CT imaging with 68Ga-labelled SST agonists, for example, 68Ga-DOTA-TOC or 68Ga-DOTA-TATE, plays an important role in staging and restaging NETs. Furthermore, SST PET/CT can identify those patients with highly 68Ga-DOTA-TOC or 68Ga-DOTA-TATE avid tumours. These are the patients who will benefit from PRRT. As a result, SST PET/CT can predict the treatment efficacy of 177Lu-DOTA-TOC or 177Lu-DOTA-TATE. This allows a personalized treatment approach, also called a therapeutic/diagnostic approach = theranostic approach. Until recently, it was thought that internalisation of the radiolabelled agonist was mandatory for SST-mediated imaging and therapy. It was Ginj et al. who proposed in 2006 the paradigm shift that radiolabelled SST antagonists may perform better than agonists despite lacking internalisation. In this chapter, the preclinical and clinical development, current status and possible future developments of radiolabelled SST antagonists are discussed.

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Buscombe, John. „Peptide Receptor Radionuclide Therapy Using Radiolabeled Somatostatin Analogues“. In Somatostatin Analogues, 207–13. Hoboken, NJ: John Wiley & Sons, Inc, 2015. http://dx.doi.org/10.1002/9781119031659.ch19.

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Bozkurt, Murat Fani. „Peptide Receptor Radionuclide Therapy“. In Neuroendocrine Tumours, 491–500. Berlin, Heidelberg: Springer Berlin Heidelberg, 2015. http://dx.doi.org/10.1007/978-3-662-45215-8_27.

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Yordanova, Anna. „Peptide Receptor Radionuclide Therapy“. In Clinical Nuclear Medicine, 867–98. Cham: Springer International Publishing, 2020. http://dx.doi.org/10.1007/978-3-030-39457-8_32.

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Stefańska, Agnieszka, Alicja Hubalewska-Dydejczyk, Agata Jabrocka-Hybel und Anna Sowa-Staszczak. „Peptide Receptor Radionuclide Therapy“. In Somatostatin Analogues, 282–90. Hoboken, NJ: John Wiley & Sons, Inc, 2015. http://dx.doi.org/10.1002/9781119031659.ch25.

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Teunissen, J. J. M., D. J. Kwekkeboom, M. de Jong, J. P. Esser, R. Valkema und E. P. Krenning. „Peptide Receptor Radionuclide Therapy“. In Clinical Nuclear Medicine, 443–55. Berlin, Heidelberg: Springer Berlin Heidelberg, 2007. http://dx.doi.org/10.1007/978-3-540-28026-2_24.

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Knapp, F. F., und Ashutosh Dash. „Peptide Receptor Radionuclide Therapy (PRRT)“. In Radiopharmaceuticals for Therapy, 185–207. New Delhi: Springer India, 2016. http://dx.doi.org/10.1007/978-81-322-2607-9_10.

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Rostene, William, und Gérard Le Fur. „Peptide Receptor Antagonists“. In Pharmacological Sciences: Perspectives for Research and Therapy in the Late 1990s, 29–36. Basel: Birkhäuser Basel, 1995. http://dx.doi.org/10.1007/978-3-0348-7218-8_4.

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Bodei, Lisa, und Giovanni Paganelli. „Peptide Receptor Radionuclide Therapy (PRRT)“. In Somatostatin Analogues, 252–63. Hoboken, NJ: John Wiley & Sons, Inc, 2015. http://dx.doi.org/10.1002/9781119031659.ch22.

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Bozkurt, Murat Fani. „Peptide Receptor Radionuclide Therapy (PRRT)“. In Neuroendocrine Tumours, 595–607. Cham: Springer International Publishing, 2024. http://dx.doi.org/10.1007/978-3-031-56968-5_28.

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Konferenzberichte zum Thema "Peptide receptor radiolabelled therapy"

Yordanova, A., H. Ahrens, H. Ahmadzadehfar, F. Gärtner, G. Feldmann, C. Fottner, M. Miederer und M. Essler. „Peptide receptor radionuclide therapy combined with chemotherapy“. In NuklearMedizin 2019. Georg Thieme Verlag KG, 2019. http://dx.doi.org/10.1055/s-0039-1683540.

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Adorján, Afrodité Emese, Szilvia Bósze, Ildikó Szabó und Gábor Mezó. „Structure-activity relationship of HER2 receptor targeting peptide and its derivatives in targeted tumor therapy“. In 35th European Peptide Symposium. Prompt Scientific Publishing, 2018. http://dx.doi.org/10.17952/35eps.2018.320.

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Kertels, O., M. Breun, H. Hänscheid, M. Kircher, P. Hartrampf, A. Schirbel, CM Monoranu et al. „Peptide Receptor Radionuclide Therapy in Patients with Neurofibromatosis Type 2 – Initial Experience“. In NuklearMedizin 2020. © Georg Thieme Verlag KG, 2020. http://dx.doi.org/10.1055/s-0040-1708361.

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Jeremic, Marija, Milovan Matovic, Dragoslav Nikezic, Dragana Krstic, Tatjana Miladinovic und Suzana Pantovic. „Measurement of urinary excretion and blood clearance after peptide receptor radionuclide therapy“. In RAD Conference. RAD Centre, 2021. http://dx.doi.org/10.21175/rad.abstr.book.2021.18.3.

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Zhang, J., HR Kulkarni, A. Singh, K. Niepsch und RP Baum. „Peptide Receptor Radionuclide Therapy (PRRT) in Patients with Grade 3 Neuroendocrine Neoplasms (NEN)“. In NuklearMedizin 2019. Georg Thieme Verlag KG, 2019. http://dx.doi.org/10.1055/s-0039-1683734.

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Knop, Filip K., Shweta Urva, Mallikarjuna Rettiganti, Charles T. Benson, William C. Roell, Kieren J. Mather, Axel Haupt, Edward Pratt und Martin Füchtenbusch. „A long-acting glucose-dependent insulinotropic polypeptide receptor agonist improves gastrointestinal tolerability of glucagon-like peptide 1 receptor agonist therapy“. In Diabetes. Umwelt. Leben. Perspektiven aus allen Blickwinkeln. Georg Thieme Verlag KG, 2024. http://dx.doi.org/10.1055/s-0044-1785380.

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Zhang, J., D. Li, M. Q. Shi, V. Jakobsson, E. Zan, C. Schuchardt, X. Chen, H. R. Kulkarni und R. P. Baum. „Long-Term Efficacy, Survival, and Toxicity of Peptide Receptor Radionuclide Therapy in Patients with Refractory Meningioma“. In 61. Jahrestagung der Deutschen Gesellschaft für Nuklearmedizin. Georg Thieme Verlag, 2023. http://dx.doi.org/10.1055/s-0043-1766317.

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Mileva, Magdalena, Hugo Levillain, Gwennaëlle Marin, Gabriela Critchi, Clementine Marin, Patrick Flamen und Ioannis Karfis. „Quantitative PET Parameters for Outcome Prediction of Peptide Receptor Radionuclide Therapy in Patients with Gastroenteropancreatic Neuroendocrine Tumors (GEP-NETs)“. In 6th International Conference on Radiopharmaceutical Therapy (ICRT 2021) Abstracts. Thieme Medical and Scientific Publishers Pvt. Ltd., 2022. http://dx.doi.org/10.1055/s-0042-1749236.

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Liu, Q. X., H. R. Kulkarni, T. Z. Zhao, C. Schuchardt, X. Chen, Z. H. Zhu, J. Zhang und R. P. Baum. „Peptide Receptor Radionuclide Therapy in Patients with Advanced Progressive Medullary Thyroid Cancer: Efficacy, Safety and Survival Predictors“. In 61. Jahrestagung der Deutschen Gesellschaft für Nuklearmedizin. Georg Thieme Verlag, 2023. http://dx.doi.org/10.1055/s-0043-1766219.

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Wahba, Mona M., Jonathan Strosberg, Anca Avram und Carina Mari Aparici. „Abstract CT254: COMPETE Phase III Trial - Peptide Receptor Radionuclide Therapy (PRRT) with177Lu-Edotreotide vs. Everolimus in Progressive GEP-NET“. In Proceedings: AACR Annual Meeting 2021; April 10-15, 2021 and May 17-21, 2021; Philadelphia, PA. American Association for Cancer Research, 2021. http://dx.doi.org/10.1158/1538-7445.am2021-ct254.

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Berichte der Organisationen zum Thema "Peptide receptor radiolabelled therapy"

Reddy, Sakamuri V. Measles Virus Nucleocapsid (MJVNP) Gene Expression and RANK Receptor Signaling in Osteoclast Precursors. Osteoclast Inhibitors Peptide Therapy for Pagets Disease. Fort Belvoir, VA: Defense Technical Information Center, Oktober 2005. http://dx.doi.org/10.21236/ada484715.

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Reddy, Sakamuri V. Measles Virus Nucleocapsid (MVNP) Gene Expression and RANK Receptor Signaling in Osteoclast Precursors, Osteoclast Inhibitors Peptide Therapy for Pagets Disease. Fort Belvoir, VA: Defense Technical Information Center, Oktober 2008. http://dx.doi.org/10.21236/ada500887.

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Reddy, Sakamuri V. Measles Virus Nucleocapsid (MVNP) Gene Expression and RANK Receptor Signaling in Osteoclast Precursors,Osteoclast Inhibitors Peptide Therapy for Pagets Disease. Fort Belvoir, VA: Defense Technical Information Center, Oktober 2004. http://dx.doi.org/10.21236/ada482539.

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Deo, Salil, David McAllister, Naveed Sattar und Jill Pell. The time-varying cardiovascular benefits of glucagon like peptide-1 agonist (GLP-RA)therapy in patients with type 2 diabetes mellitus: A meta-analysis of multinational randomized trials. INPLASY - International Platform of Registered Systematic Review and Meta-analysis Protocols, Juli 2021. http://dx.doi.org/10.37766/inplasy2021.7.0097.

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Review question / Objective: P - patients with type 2 diabetes melllitus already receiving routine medical therapy; I - patients receiving glucagon like peptide 1 receptor agonist (GLP1 receptor agonist) therapy (semaglutide, dulaglutide, liraglutide, exenatide, lixisenatide, efpeglenatide, abiglutide); C - patients receiving standard therapy for diabetes mellitus but not receiving GLP1 agonist therapy; O - composite end point as per invididual trial, cardiovascular mortality, all-cause mortality, myocardial infarction, stoke. Condition being studied: Type 2 diabetes mellitus. Study designs to be included: Randomised controlled trials which enroll a large number of patients (defined as > 500) and are multinational in origin. Studies included will need to have published Kaplan and Meier curves for the end-points presented in the manuscript.

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Xie, Yunhui, und Peng Pang. A Systematic Review and Network Meta-Analysis: Effect of of GLP-1 drugs on weight loss in obese people. INPLASY - International Platform of Registered Systematic Review and Meta-analysis Protocols, Juni 2022. http://dx.doi.org/10.37766/inplasy2022.6.0074.

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Review question / Objective: 1、Whether GLP-1 drugs have weight loss effect on obese people ? 2、Which GLP-1 drugs are most effective in weight loss among obese people ? Condition being studied: Obesity is an important public health issue that has been on the rise over the last decades. It calls for effective prevention and treatment. Bariatric surgery is the most effective medical therapy for weight loss in morbid obesity, but we are in need for less aggressive treatments. Glucagon-like-peptide-1 receptor agonists are a group of incretin-based drugs that have proven to be productive for obesity treatment. Through activation of the GLP-1 receptor they not only have an important role stimulating insulin secretion after meals, but with their extrapancreatic actions, both peripheral and central, they also help reduce body weight by promoting satiety and delaying gastric emptying.

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