Novel Chelate Complexes for Radiopharmaceuticals - TLB

Nuclear medicine | Diagnosis & Therapy | Technology Offer - page 1
Novel Chelate Complexes for Radiopharmaceuticals
Market
Radiopharmaceuticals are widely used in modern oncology
and neurology and the market for radiopharmaceuticals is
permanently growing worldwide. According to the business
consulting firm Frost & Sullivan, a European-wide increase
in the demand for radiopharmaceuticals and an increase in
turnover for contrasting agents from US$ 779.5 million in
2003 to US$ 1,238.3 million in 2010 (increase of 37%) is
expected.
To meet the growing demand for innovative radiopharmaceuticals
and to provide existing and new fields of
application in nuclear medicine, novel chelate complexes
have been developed at the University of Heidelberg and at
the Research Center Dresden-Rossendorf that are
outstanding due to the following characteristics:
Innovation
A) Tetrathiol Derivates:
Technetium-99m is probably the most important metallic
radionuclide in imaging diagnostics because it is readily
accessible through commercial Tc-generators, it has
excellent half-life properties, it is widely distributed, and a
lot of experienced data is available. Moreover, the
tetrathiols have been specifically designed for the Rhenium
nuclides 188/186 Re. In particular due to its dual function as
�- and � - -emitter 188 Re has the potential to allow for the
development of unique radiopharmaceutical products that
could be therapeutic and diagnostic agents at the same
time. A single compound could be used simultaneously for
pre-therapeutic dosimetry and as therapeutic agent.
B) Bispidine Derivates:
This ligand system is primarily specialized in complexing
Copper nuclides, in particular the diagnostically important
positron emitter 64 Cu and the therapeutic nuclide 67 Cu, but
is also applicable to other common radio nuclides (e.g.
99m Tc, 188/186 Re, 111 In, 90 Y or 68 Ga). 64 Cu is outstanding due
to its excellent PET imaging quality and its very good halflife
properties. The diagnostic potential of a 64 Cubispidine-bombesin
conjugate has already been
impressively demonstrated in preclinical "proof of concept"
animal models bearing the human prostate cancer AC-3
(S. Juran et al. 2009).
C) Bispidone Derivates:
In principal this ligand system exhibits the same
performance as the aforementioned bispidine system but is
superior to conventional chelating agents in that its ligands
are not specific for only one radionuclide, but can be
customized to a variety of metallic radionuclides like 99m Tc,
186 Re, 188 Re, 67 Cu, 64 Cu, 177 Lu, 89 Sr, 225 Ac, 68 Ga, 82 Rb or
90 Y.
Additional Advantages
hydrolytically and chemically stable ligands with
outstanding complexing characteristics
basic structure of the ligands offers manifold options
for connection of functional residues including
biomolecules
cost-effective and easy process for the synthesis of
radionuclide complexes
ligands are optimally designed for complexing the most
important radionuclides ( 99m Tc, 188/186 Re, 67/64 Cu, 68 Ga,
111 In, 90 Y, 177 Lu, 89 Sr, 225 Ac, 82 Rb, ...) which opens a
broad medical field of application
attractive patent portfolio (PCT)
Fields of Application
These novel complexing agents are suitable for the
production of innovative radiopharmaceuticals that are
based on metallic radionuclides. Radiopharmaceuticals are
widely used in nuclear medicine:
Radio diagnostics:
- contrasting agents, imaging diagnostics
- scintigraphy, e.g. myocardium, kidneys, bones,
thyroid gland…
- receptor imaging (neuroendocrine tumors)
- oncology, neurology
- PET and SPECT
Radio therapeutics:
- radio immunology
- tumor therapy (radiation therapy)
- pain therapy (rheumatoid arthritis)
Technology Transfer
Copyright © 2009 Technologie-Lizenz-Büro (TLB) der Baden-Württembergischen Hochschulen GmbH
The Technologie-Lizenz-Buero GmbH has been charged
with the commercialization and offers companies the
opportunity to obtain a license to exploit this new and
promising technology.
Further information about "radiopharmaceuticals":
Dr. Daniel Veith
dveith@tlb.de
Technologie-Lizenz-Buero (TLB)
der Baden-Wuerttembergischen Hochschulen GmbH
Ettlinger Straße 25 | 76137 Karlsruhe | Germany
Tel.: +49-(0)721-79004-0 | Fax: +49-(0)721-79004-79
www.tlb.de

Nuclear medicine | Diagnosis & Therapy | Technology Offer – page 2
Patents:
DE 1 / US 2 / EP 2
1
granted
2
pending
Tetrathiols Bispidines Bispidones
DE 1 / US 2 / EP 2
Copyright © 2009 Technologie-Lizenz-Büro (TLB) der Baden-Württembergischen Hochschulen GmbH
DE 2 / PCT 2
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Biomolekül
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Mn +
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