The Use of Isotopically Labeled Compounds in Drug Discovery

摘要

Isotopically labeled compounds are critical to the drug development process for use as radioligands in lead discovery [1], as metabolic tracers in development [2], and in phase IV clinical studies [3]. Large pharmaceutical companies typically have a radiochemistry group to synthesize isotopically labeled compounds and coordinate the use of contract laboratories for custom synthesis when required. In contrast, smaller companies generally outsource this work to contract laboratories. This review familiarizes the reader with the uses of long-lived radiolabeled compounds (those compounds with half-lives greater than 1 month) and stable isotope-labeled (SIL) compounds and enables them to effectively plan radiochemical syntheses. The synthesis and use of short-lived positron-emitting radiolabeled compounds (those labeled with ~(11)C, ~(13)N,~ (15)O, ~(18)F) used in nuclear medicine imaging studies is discussed in a separate review in this journal.