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Radiopharmaceutical Research


Lifecycle:1 Jan 1995 →  Today
Organisation profile:

The Radiofarmaceutical Research team aims to develop and apply new radiopharmaceuticals for diagnosis (PET en SPECT) or for radionuclide therapy.  The development of radiopharamaceuticals can be subdivided in different steps in which the team has acquired expertise:

  • design: structure design of new radiotracers based the target that needs to be visualized and the requitrement for fast and efficient incorporation of the radionuclide in the tracer molecule
  • organic synthesis : chemical synthesis of the tracer precursor (the tracer derivative that is chemically coupled to the radionuclide in the radiochemistry step and the non-radioactive (stable) form of the tracer.  Analysis (purity assay, (TLC-HPLC) and characterisation (confirmation of the expected chemical structure) (NMR, LC-MS)
  • radiochemistry: chemical coupling of the radionuclide with the tracer precursor.  The radionuclide is generated using a cyclotron or a radionuclide generator. The resulting reaction mixture is purified (separation from tracer-precursor) and formulated for intravenous injection .  The raduiochemical steps can be performed in remote controlled or fully automated synthesis modules that are set up in lead shielded "hotcells". The radiotracer is subsequently analysed using radio-HPLC or radio-TLC.
  • in vitro evaluation: stability of the tracer (HPLC, TLC), binding studies with cells tissue homogenates of cryosections.  Quantification of the activity using a gamma-counter or autoradiography
  • in vivo/ex vivo evaluation: biodistribution in small animals(mouse, rat), study of the farmacokinetics.  microPET studies with/without pharmacological (pre)treatment.  Specific animal models for validation of radiotracers. Non-human primate studies in preparation for clinical studies
  • preclinical application: application of radiotracers to quantify targetmolecules in small animals
  • implementation of GMP conform production for clinical studies: upscaling of the production and identification of critical parameters, engineering runs, development of a suitable formulation for intravenous injection, development and evaluation of QC methods (radioHPLC), execution of validation runs, drafting of IMPD and FANC documentation that are necessary for application for a clinical study

Radiotracers can be labeled with carbon-11 (11C), fluorine-18 (18F), gallium-68 (68Ga), zirconium-89 (89Zr), iodine-124 (124I) for PET and technetium-99m (99mTc), iodine-123 (123I) for SPECT.

Keywords:radiopharmaceuticals, 11C, 18F, 3H, autoradiography, SPECT, PET, pharmacokinetics, biodistribution, single photon emission tomography, positron emission tomography, radiotracer
Disciplines:Medical imaging and therapy, Other chemical sciences, Chemical product design and formulation, Biomaterials engineering, Medicinal products