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Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases

Institute of Nuclear Chemistry, Johannes Gutenberg University Mainz, Fritz-Strassmann-Weg 2, 55128 Mainz, Germany
Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Bautzner Landstrasse 400, 01328 Dresden, Germany
University Cancer Center (UCC) Carl Gustav Carus, Tumorimmunology, Technical University Dresden, Fetscherstr. 74, 01307 Dresden, Germany
Department of Nuclear Medicine & PET, All India Institute of Medical Sciences, Ansari Nagar, New Delhi 110029, India
Department of Nuclear Medicine, University of Pretoria & Steve Biko Academic Hospital, Private Bag X169, Pretoria 0001, South Africa
Diagnostisch Therapeutisches Zentrum, DTZ am Frankfurter Tor, Kadiner Straße 23, 10243 Berlin, Germany
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
Pharmaceuticals 2017, 10(2), 45;
Received: 14 February 2017 / Revised: 3 May 2017 / Accepted: 5 May 2017 / Published: 18 May 2017
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.

AMA Style

Pfannkuchen N, Meckel M, Bergmann R, Bachmann M, Bal C, Sathekge M, Mohnike W, Baum RP, Rösch F. Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases. Pharmaceuticals. 2017; 10(2):45.

Chicago/Turabian Style

Pfannkuchen, Nina, Marian Meckel, Ralf Bergmann, Michael Bachmann, Chandrasekhar Bal, Mike Sathekge, Wolfgang Mohnike, Richard P. Baum, and Frank Rösch. 2017. "Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases" Pharmaceuticals 10, no. 2: 45.

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