A first-line treatment for relapsing forms of multiple sclerosis (MS) was approved in September 2010 by the US Food and Drug Administration: FTY720 (fingolimod, Gilenya), which acts as a sphingosine 1-phosphate (S1P) receptor modulator.
There is preclinical evidence that in addition to decreasing infiltration of lymphocytes into the central nervous system (CNS), FTY720 may provide additional neuroprotection through modulation of cerebral S1P receptors.
To further study the action of FTY720 in the CNS, Emmanuelle Briard, Yves Auberson, and colleagues at the Novartis Institutes for BioMedical Research in Basel (Switzerland) evaluated a series of iodinated FTY720 derivatives that could be used to study the drug's brain distribution in patients using nuclear imaging techniques, and their results are reported in ChemMedChem.
After extensive profiling, they identified 2-iodo-FTY720 (BZM055) as a close mimic of FTY720, having similar physicochemical properties and organ distribution, despite the addition of an iodine atom. They also showed that BZM055 is phosphorylated into its biologically active form at a similar rate to FTY720, retaining an affinity and selectivity for S1P receptors comparable to FTY720-phosphate, as well as similar brain penetration kinetics. [123I]BZM055 is currently being developed as a SPECT tracer for studying the pharmacokinetics and distribution of FTY720 in the human brain. In addition, and since FTY720 has been shown to accumulate in myelin sheaths, this tracer might also prove useful to image myelin in MS patients.
Author: Emmanuelle Briard, Novartis Institutes for BioMedical Research, Basel (Switzerland),
Title: BZM055, an Iodinated Radiotracer Candidate for PET and SPECT Imaging of Myelin and FTY720 Brain Distribution
ChemMedChem, Permalink to the article: http://dx.doi.org/10.1002/cmdc.201000477
Emmanuelle Briard | Wiley-VCH
'Lipid asymmetry' plays key role in activating immune cells
20.02.2018 | Biophysical Society
New printing technique uses cells and molecules to recreate biological structures
20.02.2018 | Queen Mary University of London
For the first time, a team of researchers at the Max-Planck Institute (MPI) for Polymer Research in Mainz, Germany, has succeeded in making an integrated circuit (IC) from just a monolayer of a semiconducting polymer via a bottom-up, self-assembly approach.
In the self-assembly process, the semiconducting polymer arranges itself into an ordered monolayer in a transistor. The transistors are binary switches used...
Breakthrough provides a new concept of the design of molecular motors, sensors and electricity generators at nanoscale
Researchers from the Institute of Organic Chemistry and Biochemistry of the CAS (IOCB Prague), Institute of Physics of the CAS (IP CAS) and Palacký University...
For photographers and scientists, lenses are lifesavers. They reflect and refract light, making possible the imaging systems that drive discovery through the microscope and preserve history through cameras.
But today's glass-based lenses are bulky and resist miniaturization. Next-generation technologies, such as ultrathin cameras or tiny microscopes, require...
Scientists from the University of Zurich have succeeded for the first time in tracking individual stem cells and their neuronal progeny over months within the intact adult brain. This study sheds light on how new neurons are produced throughout life.
The generation of new nerve cells was once thought to taper off at the end of embryonic development. However, recent research has shown that the adult brain...
Theoretical physicists propose to use negative interference to control heat flow in quantum devices. Study published in Physical Review Letters
Quantum computer parts are sensitive and need to be cooled to very low temperatures. Their tiny size makes them particularly susceptible to a temperature...
15.02.2018 | Event News
13.02.2018 | Event News
12.02.2018 | Event News
20.02.2018 | Life Sciences
20.02.2018 | Medical Engineering
20.02.2018 | Physics and Astronomy