Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases

Pfannkuchen, Nina; Meckel, Marian; Bergmann, Ralf; Bachmann, Michael; Bal, Chandrasekhar; Sathekge, Mike; Mohnike, Wolfgang; Baum, Richard P.; Rösch, Frank

doi:10.3390/ph10020045

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Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases

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^1,*

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

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

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

Received: 14 February 2017 / Revised: 3 May 2017 / Accepted: 5 May 2017 / Published: 18 May 2017

(This article belongs to the Special Issue Emerging Theranostic Tracers in the Context of Radiopharmaceutical Drug Development)

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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

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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. https://doi.org/10.3390/ph10020045

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. https://doi.org/10.3390/ph10020045

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. https://doi.org/10.3390/ph10020045

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Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases

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