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DOI: 10.1055/s-0035-1553440
PET/CT Diagnostik des Prostatakarzinoms mit Bombesinanaloga
PET/CT diagnostics of prostata cancer using BombesinanalogaPublication History
Publication Date:
14 August 2015 (online)
Zusammenfassung
Humane Prostatakarzinome exprimieren häufig den Gastrin-Releasing Peptide receptor (GRPr), der auch als Bombesin-Typ 2-Rezeptor bekannt ist. In normalem und hyperplastischem Prostatagewebe ist die Binding von GRPr-Liganden hingegen niedrig. Mit Radiometallen markierte GRPr-Antagonisten zeigten im Modell sowohl eine hohe Aufnahme in GRPr-exprimierenden Tumoren, als auch eine schnelle Elimination aus dem Plasma/Normalgewebe. Diese vielversprechenden Charakteristika wurden in klinischen Studien bestätigt, die auch erste Daten zur Sensitivität von GRPr PET/CT zum Nachweis von primären und metastatierten Prostatakarzinomen erhoben. Diese Arbeit gibt einen kurzen Überblick über die Entwicklung von GRPr-basierten Liganden zur Diagnostik (und zur potentiellen Radionuklidtherapie) von Prostatakarzinomen.
Abstract
Human prostate cancers frequently express the gastrin releasing peptide receptor (GRPr), also known as Bombesin type-2 receptor. In contrast, expression levels of GRPr are low in normal and hyperplastic prostate tissue. Metabolically stable GRPr antagonists, labeled with radiometals have shown high tumor uptake in preclinical models of prostate cancer. Furthermore, these ligands demonstrated rapid clearance from normal tissues. Clinical studies have confirmed this favorable biodistribution of GRPr antagonists in patients. These studies have also provided first data on the sensitivity of GRPr PET for detection of primary and metastatic prostate cancer. This review provides a brief overview on the clinical development of GRPr ligands for PET imaging (and potentially also for radionuclide therapy) of prostate cancer.
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