EC
Radiochemistry molecular probes for in vivo imaging
Description
The aim of the course is to provide students with the basic fundamental knowledge of radiochemistry / radiotracer design related to molecular nuclear imaging (Positron Emission Tomography (PET) / Single Photon Emission Tomography (SPET)). The course is based on a series of lectures (organized within three sessions: radioisotopes / radiochemistry ; radiopharmaceutical design and manufacturing ; PET / SPET preclinical and clinical applications) and includes two tutorials as well as a visit of the cyclotron / radiochemistry facilities of CYRCé (Institut Pluridisciplinaire Hubert Curien, Cronenbourg).
- Introduction to molecular imaging (Positron Emission Tomography (PET) / Single Photon Emission Tomography (SPET));
- Radioisotope production (cyclotron including target issues, generator);
- Basic radiochemistry (radioisotope incorporation, isotopic labeling versus foreign labeling), applications to the labelling of drug-like molecules (low molecular weight) as well as macromolecules;
- Biogenic radiotracer synthesis : incorporation of the short-lived radioisotopes 11C, 13N and 15O;
- Non-biogenic radiotracer synthesis : the radiohalogens (18F, 76Br, 123I, 124I) and radiometals (64Cu, 68Ga, 89Zr, 99mTc);
- Radiotracer design : pharmacological criteria (lipophilicity, non-specific binding, target density, target affinity and selectivity, metabolism issues, labeling position, pharmacokinetics);
- Manufacturing of radiopharmaceuticals : production (automation, synthesis process, reagents and kits), quality controls, radioprotection and waste management, radiopharmacy (reglementary issues, pharmacopoeias);
- Selected examples of imaging applications of PET / SPET probes (preclinical / clinical).
Compétences visées
Basic knowledge in molecular nuclear imaging; PET / SPET radioisotope properties and production aspects; design of a PET / SPET radiotracer (drug-like molecules (low molecular weight) as well as macromolecules), based on chemical - ease of introduction, choice of the radioisotope - but also pharmacological - notably metabolism issues - criteria; radiochemistry (radiosynthesis pathway and process, including purification, automation and radioprotection issues); quality controls (analytical methods, specifications) and introduction to radiopharmaceutical aspects.