Pre vivo, ex vivo and in vivo evaluations of [68Ga]-EDTMP

Mitterhauser, Markus; Toegel, Stefan; Wadsak, Wolfgang; Lanzenberger, Rupert R.; Mien, Leonhard-Key; Kuntner, Claudia; Wanek, Thomas; Eidherr, Harald; Ettlinger, Dagmar E.; Viernstein, Helmut; Kluger, Rainer; Dudczak, Robert; Kletter, Kurt

doi:10.1016/j.nucmedbio.2007.03.002

« Previous Next »Nuclear Medicine and Biology
Volume 34, Issue 4 , Pages 391-397, May 2007

Pre vivo, ex vivo and in vivo evaluations of [⁶⁸Ga]-EDTMP

Markus Mitterhauser
- Department of Nuclear Medicine, Medical University of Vienna, Vienna 1090, Austria
- Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna 1090, Austria
- Hospital Pharmacy, General Hospital of Vienna, Vienna 1090, Austria
- Corresponding author. Department of Nuclear Medicine, AKH Wien, A-1090 Vienna, Austria. Tel.: +43 1 40400 1557; fax: +43 1 40400 1559.
Stefan Toegel
- Department of Nuclear Medicine, Medical University of Vienna, Vienna 1090, Austria
- Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna 1090, Austria
Wolfgang Wadsak
- Department of Nuclear Medicine, Medical University of Vienna, Vienna 1090, Austria
- Department of Inorganic Chemistry, University of Vienna, Vienna 1090, Austria
Rupert R. Lanzenberger
- Department of Psychiatry, Medical University of Vienna, Vienna 1090, Austria
Leonhard-Key Mien
- Department of Nuclear Medicine, Medical University of Vienna, Vienna 1090, Austria
- Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna 1090, Austria
Claudia Kuntner
- Department of Radiopharmaceuticals, Austrian Research Centers, Seibersdorf 2443, Austria
Thomas Wanek
- Department of Radiopharmaceuticals, Austrian Research Centers, Seibersdorf 2443, Austria
Harald Eidherr
- Department of Nuclear Medicine, Medical University of Vienna, Vienna 1090, Austria
- Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna 1090, Austria
Dagmar E. Ettlinger
- Department of Nuclear Medicine, Medical University of Vienna, Vienna 1090, Austria
Helmut Viernstein
- Department of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna 1090, Austria
Rainer Kluger
- Department of Orthopedics, Donauspital, Vienna 1220, Austria
Robert Dudczak
- Department of Nuclear Medicine, Medical University of Vienna, Vienna 1090, Austria
Kurt Kletter
- Department of Nuclear Medicine, Medical University of Vienna, Vienna 1090, Austria

Received 22 January 2007; received in revised form 23 February 2007; accepted 3 March 2007.

Abstract

Introduction

The objectives of this study were to develop a simple preparation method for [⁶⁸Ga]-EDTMP and to evaluate the applicability of [⁶⁸Ga]-EDTMP as a potential positron emission tomography (PET) bone imaging agent using pre vivo, ex vivo and in vivo models.

Methods

[⁶⁸Ga]-EDTMP was prepared using [⁶⁸Ga]-gallium chloride eluted from the ⁶⁸Ge/⁶⁸Ga generator and commercially available Multibone kits. Binding affinity to bone compartments was evaluated using a recently established pre vivo model. In vivo (microPET) and ex vivo experiments were performed in mice, and the results of which were compared with those obtained with [¹⁸F]-fluoride.

Results

[⁶⁸Ga]-EDTMP was accessible via simple kit preparation and predominantly accumulated in bone tissue in vivo, ex vivo and pre vivo. Binding to mineral bone was irreversible, and low binding was observed in organic bone. In vivo microPET evaluation revealed predominant uptake in bone with renal excretion. Compared with [¹⁸F]-fluoride, the uptake was lower and the PET image quality was reduced.

Conclusions

From the present evaluation, apart from the autonomy for PET centers without an onsite cyclotron, the advantage of [⁶⁸Ga]-EDTMP over [¹⁸F]-fluoride is not apparent and the future clinical prospect of [⁶⁸Ga]-EDTMP remains speculative.

Keywords: Bone, PET, Gallium-68, Fluorine-18, Bone scan