Tritium: a coming of age for drug discovery and development ADME studies

Owing to recent developments in tritium chemistry and analysis, high-quality tritium-labelled drugs can now be prepared simply, cheaply and in timescales commensurate with those needed for rapid drug discovery in adsorption, distribution, metabolism and excretion (ADME) projects. Such 3H-labelled drugs are enabling high-quality decision-making at key points in the drug discovery process, thus ensuring more effective research projects, a key issue in commercial success. In addition, tritium-labelled compounds continue to play a significant role in ADME studies later in the pharmaceutical development process. This is especially so for highly potent and hence low-dose agents, for drugs with complex structures and for those compounds that undergo molecular fragmentation as a result of metabolism.