Abstract
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.
Recent developments in tritium chemistry and analysis mean that high‐quality tritium‐labelled drugs can now be prepared simply, cheaply and in timescales commensurate with those needed for rapid drug discovery projects. This rapid‐labelling approach is ensuring more effective pharmaceutical research projects, a key issue in commercial success. At later stages in the pharmaceutical development process, the same tritium labelling and analysis methodologies can also be utilised to support high quality adsorption, distribution, metabolism and excretion studies.