radioactive yields also exhibit
sufficient to facilitate
robust PET scanning. Simultaneously, they must
fast an alternative radiochemistry,
which decays during a brief time span, without posing a hazard to the subject.” By using
radionuclide,
fluorine-18, the team has been able to synthesise a novel tracer which
exhibits these
attributes. Its properties will be augmented further by the researchers, who design
seek
measure reduce
increase P-gp to
new tracers to an
or activity,
thereby accentuating their profiles once
scanned.
“Measuring the transporters is
paramount, understanding also
P-gp have
if their
functionality can be controlled by modulating or inducing may
responses important
but
significant European market – with the current radiopharmaceutical sector in the Netherlands alone worth around €12.5m per year. “We’ve been successful
lead compounds, which are not only highly specific, but also very stable in vivo. A lot of in vitro data exists which
transporters “We strongly
suspect that the functionality of the BBB is
related to brain disorders”
medicinal applications.” Another, wider scientific benefit of the group’s pioneering tracers is
that they
can be utilised in PET facilities without a cyclotron. refined,
hope to use spin-off companies to sell them to other molecular imaging centres,” says
Luurtsema. “Their dissemination
will also create more opportunities for advanced research throughout
the field,
since they require less costly equipment to conduct scans”. Commercially, this is a
“Once our compounds are industrialised and patented, we
concerns within
the brain, but this is inapplicable in vivo. This
innovative
is quite a new science,
and the most unique aspect of our work,” says Luurtsema. The
based have first
experiments,
initiated their radiochemistry and
evaluated a first test on genetically
modified mice. “Our immediate goals are to undertake pre-clinical assessments, but the next step will be for us to internally produce these compounds in our facilities at
Groningen. Subsequently, we’ll
scrutinise the tracers in healthy, volunteer subjects, in conjunction with specialists in neurology and psychiatry,”
Luurtsema. “Of course, this is dependent on the success of pre-clinical
says trials, and
obtaining proof of concept in the tests we’re conducting on mice, rats and through full tracer kinetic modelling.”
Dr. Gert Luurtsema Dr. Gert Luurtsema is a trained radiopharmaceutical chemist and finished his PhD study at the VU University Medical Center in Amsterdam. His current research at the UMCG is to develop new PET radiopharmaceuticals to measure ABC transporters at the blood-brain barrier with positron emission tomography (PET).
Contact: Tel: +31503612686 Email:
g.luurtsema@
umcg.nl Web:
www.ngmb.umcg.nl
Schematic overview of the principle of PET; Injection of the fluorine-18 labelled tracer (a), decay of the radionu- clide 18F (b) and the detection of 511 keV gamma ray (c)
www.projectsmagazine.eu.com 25
AT A GLANCE Project Information in locating new
Project Title: New fluorine-18 labelled PET probes for P-gp measurements at the BBB in brain disorders
Netherlands- researchers
Project Objective: The goal of this project is to develop the synthesis, GMP production and preclinical evaluation of fluorine-18 labelled P-gp tracers suitable for PET imaging. In addition, the project will lead to a multi-centre trial in collaboration with the departments of neurology and psychiatry, in which these tracers will be validated in humans.
Project Duration and Timing: 4 years, 2012 to 2016
Project Funding: STW
Project Partners: Dr. A.D. Windhorst, prof. dr. N.A. Colabufo, prof. dr. P.H. Elsinga, prof. dr. A.A. lammertsma, prof. dr. R.A.J.O. Dierckx, dr. M. Cantore, MSc. H. Savolainen and MSc. R. Raaphorst
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