Radiopharmaceutical Chemistry

Division of Radiopharmaceutical Chemistry

Prof. Dr. rer. nat. Klaus Kopka

Baranski, Ann-Christin et al. awarded with the Henry N. Wagner, Jr., MD, Image of the Year Award 2017 of the Society of Nuclear Medicine and Molecular Imaging (SNMMI), Denver, Colorado (USA).
© dkfz.de

The Division of Radiopharmaceutical Chemistry has a long-standing expertise in Radiopharmaceutical Drug Development. The research interests are focussing on all facets of Radiopharmaceutical Sciences in Cancer Research. The provision of tailor-made targeted theranostic radiotracers both for non-invasive imaging by means of i.a. PET/CT and PET/MRI as well as for radioligand-assisted cancer therapy (i.e. endoradiotherapy) is the mission of the Division of Radiopharmaceutical Chemistry.

Theranostic PSMA Radioligands/Radiotracers:
We have developed a new series of prostate-specific membrane antigen (PSMA)-targeted radioligands for non-invasive PET imaging as well as endoradiotherapy of prostate cancer. In 2011 the PET tracer [68Ga]Ga-PSMA-11 was already clinically introduced for PCa imaging at Heidelberg University Hospital (Dept. of Nuclear Medicine). This tracer will be examined in the DKTK-funded multicenter clinical trial (phases-I and -II) in high-risk prostate cancer patients (Sponsor DKFZ Heidelberg) with 11 participating centers within the D-A-CH region. This endeavor is one of the defined DKTK highlight projects. The inclusion of the first patient is already expected in 2017.
Since 2013 PSMA-11 was transformed into the theranostic version PSMA-617 which can be radiolabelled with the radiometals lutetium-177 for beta therapy and actinium-225 for alpha therapy. [177Lu]Lu-PSMA-617 has recently entered the agenda of the German Society of Nuclear Medicine (DGN e.V.): a consortial project was founded to initiate a prospective multicenter clinical trial (phases-II/-III) for radioligand therapy of advanced PCa patients.
There is also a strong need for 18F-labelled PSMA PET tracers (T1/2: 110 min), in addition to the 68Ga-labelled PSMA tracers (T1/2: 68 min), to cover all daily patient examinations. Therefore, [18F]PSMA-1007 was recently developed by our group, an ideal prostate PET imaging agent for primary diagnosis of PCa and imaging of local relapse. As PSMA-1007 is derived from PSMA-617, both tracers ([18F]PSMA-1007 and [177Lu]Lu-PSMA-617) can be used as a theranostic tandem for PSMA-targeted imaging and therapy.

Future Outlook:
In a next step we will clinically develop bimodal dual-labelled PET/OI tracers (supported by BMBF VIP+) combining preoperative staging by means of PET/CT, followed by targeted fluorescence-guided surgery of lymph node metastases. For this ongoing research, the Div. of Radiopharmaceutical Chemistry (Ann-Christin Baranski et al.) together with the Dept. of Nuclear Medicine have been awarded (after only 2 years again) with the highly renowned Image of the Year Award 2017 of the Society of Nuclear Medicine and Molecular Imaging (SNMMI), Denver, Colorado (USA).

Contact

Prof. Dr. rer. nat. Klaus Kopka
Radiopharmaceutical Chemistry (E030)
Deutsches Krebsforschungszentrum
Im Neuenheimer Feld 280
69120 Heidelberg
Tel: +49 6221 42 2432

Selected Publications

  • Kopka K, Benešová M, Ba?inka C, Haberkorn U, Babich J. Glu-Ureido-Based Inhibitors of Prostate-Specific Membrane Antigen: Lessons Learned During the Development of a Novel Class of Low-Molecular-Weight Theranostic Radiotracers. J Nucl Med 2017 Sep;58(Suppl 2):17S-26S.
  • Baranski AC, Schäfer M, Bauder-Wüst U, Wacker A, Schmidt J, Liolios C, Mier W, Haberkorn U, Eisenhut M, Kopka K, Eder M. Improving the imaging contrast of 68Ga-PSMA-11 by targeted linker design: charged spacer moieties enhance the pharmacokinetic properties. Bioconjugate Chem 2017;28(9):2485-2492.
  • Giesel FL, Hadaschik B, Cardinale J, Radtke J, Vinsensia M, Lehnert W, Kesch C, Tolstov Y, Singer S, Grabe N, Duensing S, Schäfer M, Neels OC, Mier W, Haberkorn U, Kopka K*, Kratochwil C*. F-18 labelled PSMA-1007: biodistribution, radiation dosimetry and histopathological validation of tumor lesions in prostate cancer patients. Eur J Nucl Med Mol Imaging 2017;44(4):678-688. *contributed equally
  • Cardinale J, Schäfer M, Benešová M, Bauder-Wüst U, Leotta K, Eder M, Neels OC, Haberkorn U, Giesel FL, Kopka K. Preclinical Evaluation of 18F-PSMA-1007: A New PSMA-Ligand for Prostate Cancer Imaging. J Nucl Med 2017;58(3):425-431.
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