Isotope analysis has been broadly used in the scientific community for several decades. The advancement of mass spectroscopy techniques has allowed users to determine isotopic fingerprints for natural and synthetic materials. This methodology has been extended to pharmaceutical developers and manufacturers to determine the metabolic degradation of the API, but also to authenticate end-manufactured drug APIs and ingredients.
IsoSciences specializes in the synthesis of organic molecules and molecules of biological interest. Starting with typical organic and labeled raw materials, the synthetic chemists at IsoSciences are able to create successful paths to labeled precursors, labeled intermediates, labeled APIs and finally, labeled drugs and metabolites, while incorporating the stable isotope label in strategic locations. The location of labels is critical to creating a molecule that ultimately gives the information necessary during the metabolic processes.
Additionally, it has been found in recent work that strategic incorporation of stable isotope labeled APIs can ultimately allow an improved technical performance. For instance, careful replacement of hydrogen with deuterium could potentially lead to increased bioavailability in addition to the inhibition of biological processes that could lead to toxicity and other related side effects. The synthesis of labeled APIs has many potential benefits from monitoring the authenticity of the drugs, determining the metabolic decomposition of the labeled active ingredient, and potentially the development of new APIs by improving technical performance of non-labeled APIs.
Strategic development of a labeled API is very important and so is selecting a veteran team that can help develope suitable APIs for a metabolic study. For example, if an API study of Rifampicin (see structure) was necessary the IsoSciences team would consider all reasonable metabolic break points (e.g., hydrolysis of ester or imine functionalities, or oxidation of the para-dihydroxynaphthyl structure) and then determine where best to place stable isotope labels in order to synthesize a suitable labeled candidate.