Résumé
Carbon isotope labeling is an important tool for studying how drugs behave in the body, including how they are broken down and processed over time. By replacing one or more carbon atoms in a drug molecule with naturally occurring carbon isotopes (13C or 14C), researchers can track the drug and its metabolites throughout preclinical and clinical development using a unique “isotopic fingerprint.” Despite its usefulness, carbon isotope labeling presents a major challenge. Producing isotopically labeled drug candidates is often difficult and expensive, largely because only a limited number of labeled starting materials are commercially available. As a result, researchers frequently rely on labor-intensive synthetic approaches, which—especially in the case of long-lived carbon-14—raise concerns about radioactive exposure and the disposal of hazardous waste. In this lecture, I provide an introduction to the topic and then elaborate on our own research dealing with direct methods for introducing the isotope label in some cases through a molecular surgery approach.
