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Pharmaceuticals 2017, 10(2), 45; doi:10.3390/ph10020045

Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases

1
Institute of Nuclear Chemistry, Johannes Gutenberg University Mainz, Fritz-Strassmann-Weg 2, 55128 Mainz, Germany
2
Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, 01328 Dresden, Germany
3
University Cancer Center (UCC) Carl Gustav Carus, Tumorimmunology, Technical University Dresden, Fetscherstr. 74, 01307 Dresden, Germany
4
Department of Nuclear Medicine & PET, All India Institute of Medical Sciences, Ansari Nagar, New Delhi 110029, India
5
Department of Nuclear Medicine, University of Pretoria & Steve Biko Academic Hospital, Private Bag X169, Pretoria 0001, South Africa
6
Diagnostisch Therapeutisches Zentrum, DTZ am Frankfurter Tor, Kadiner Straße 23, 10243 Berlin, Germany
7
Department of Nuclear Medicine, Center for PET/CT, Zentralklinik Bad Berka, Robert-Koch-Allee 9, 99438 Bad Berka, Germany
*
Author to whom correspondence should be addressed.
Academic Editors: Klaus Kopka and Elisabeth Eppard
Received: 14 February 2017 / Revised: 3 May 2017 / Accepted: 5 May 2017 / Published: 18 May 2017
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Abstract

Bone metastases, often a consequence of breast, prostate, and lung carcinomas, are characterized by an increased bone turnover, which can be visualized by positron emission tomography (PET), as well as single-photon emission computed tomography (SPECT). Bisphosphonate complexes of 99mTc are predominantly used as SPECT tracers. In contrast to SPECT, PET offers a higher spatial resolution and, owing to the 68Ge/68Ga generator, an analog to the established 99mTc generator exists. Complexation of Ga(III) requires the use of chelators. Therefore, DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), NOTA (1,4,7-triazacyclododecane-1,4,7-triacetic acid), and their derivatives, are often used. The combination of these macrocyclic chelators and bisphosphonates is currently studied worldwide. The use of DOTA offers the possibility of a therapeutic application by complexing the β-emitter 177Lu. This overview describes the possibility of diagnosing bone metastases using [68Ga]Ga-BPAMD (68Ga-labeled (4-{[bis-(phosphonomethyl))carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl)acetic acid) as well as the successful application of [177Lu]Lu-BPAMD for therapy and the development of new diagnostic and therapeutic tools based on this structure. Improvements concerning both the chelator and the bisphosphonate structure are illustrated providing new 68Ga- and 177Lu-labeled bisphosphonates offering improved pharmacological properties. View Full-Text
Keywords: bisphosphonates; bone metastases; diagnosis; therapy; 68Ga; 177Lu bisphosphonates; bone metastases; diagnosis; therapy; 68Ga; 177Lu
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MDPI and ACS Style

Pfannkuchen, N.; Meckel, M.; Bergmann, R.; Bachmann, M.; Bal, C.; Sathekge, M.; Mohnike, W.; Baum, R.P.; Rösch, F. Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases. Pharmaceuticals 2017, 10, 45.

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