Creative Biolabs has worked extensively on a wide variety of metabolism studies. As part of our in vitro metabolism service, we provide high-quality metabolite profiling and identification service to characterize a drug's metabolites.
The process of metabolites profiling and identification of therapeutic compounds in the early stage of drug discovery has great value in interpreting a drug's pharmacology, pharmacokinetic and toxicology characteristics and may have directive function in the following clinical tests. As we know, after a drug entering the body for a certain time, it will be eliminated either by excretion or by metabolizing to one or more metabolites. Those drugs undergoing metabolism may produce unexpected effects or potential toxicities. Therefore, it is important to identify the metabolites of a drug. Also, the knowledge of metabolic liability is useful for guiding lead optimization to overcome issues such as stability.
The FDA Guidance for Industry on Safety Testing of Drug Metabolites (2008) highlights in vitro metabolite assessment for humans and animals. Those metabolites which are unique to humans or have disproportionate levels in humans may require additional toxicological studies.
Creative Biolabs provides a variety of matrices for metabolite profiling and identification, including liver microsomal incubations, hepatocyte incubations, S9 incubations, recombinant enzymes as well as other in vivo approaches. All matrices are available from multiple species for cross-species metabolite profiling. We measure compound degradation, isolate of metabolites and elucidate the chemical structure by a variety of methods, of which the high-resolution mass spectrometry (HR-MS) is the major tool for metabolite identification both qualitatively and quantitatively. We are also able to detect radiolabeled chemicals for analysis of different types of chemistry.
Figure 1. General scheme of HR-MS-based approaches to drug metabolite detection and identification (Zhu et al. 2011).
A Typical Protocol
The Advantage of Our High-Resolution Mass Spectrometry (HR-MS) Platform
Mass spectrometry plays a key role in drug metabolite identification and profiling. Modern high-resolution mass spectrometry (HR-MS) instruments are the development of conventional MS instruments with improved accuracy and stability, along with new data processing techniques. Creative Biolabs equipped with the most advance HR-MS equipment which has improved the quality and productivity of metabolite identification processes. The resolution is > 10,000 at full-width at half-maximum and the mass is > 5 ppm deviation.
Our advantages:
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References
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