Radiochemistry molecular probes for in vivo imaging
Master ChimieParcours Chimie, biologie et drug design
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.