Abstract
Drug metabolism and pharmacokinetics (DMPK) represents a critical component in support of drug discovery and development. This is because the therapeutic efficacy of a drug is dependent on its exposure which in turn is dictated in part by metabolic stability of the molecule. In addition, drug metabolism may lead to the formation of metabolites that can either be pharmacologically active or elicit adverse effect. On this basis, metabolite identification and profiling have become a routine exercise during lead optimization and subsequent development processes. The current communication provides an overview on the account of metabolite identification and profiling in support of drug design with an additional emphasis on the commonly used analytical techniques. The discussion is supported by case studies. Future directions are discussed in the context of newer platforms of technology and bioanalytical approaches enabling better operation efficiency in pharmaceutical research.
Keywords: Bioactivation, drug discovery, drug metabolism, high resolution mass spectrometry, metabolite identification, profiling
Current Pharmaceutical Design
Title: Metabolite Identification and Profiling in Drug Design: Current Practice and Future Directions
Volume: 15 Issue: 19
Author(s): Zhoupeng Zhang, Mingshe Zhu and Wei Tang
Affiliation:
Keywords: Bioactivation, drug discovery, drug metabolism, high resolution mass spectrometry, metabolite identification, profiling
Abstract: Drug metabolism and pharmacokinetics (DMPK) represents a critical component in support of drug discovery and development. This is because the therapeutic efficacy of a drug is dependent on its exposure which in turn is dictated in part by metabolic stability of the molecule. In addition, drug metabolism may lead to the formation of metabolites that can either be pharmacologically active or elicit adverse effect. On this basis, metabolite identification and profiling have become a routine exercise during lead optimization and subsequent development processes. The current communication provides an overview on the account of metabolite identification and profiling in support of drug design with an additional emphasis on the commonly used analytical techniques. The discussion is supported by case studies. Future directions are discussed in the context of newer platforms of technology and bioanalytical approaches enabling better operation efficiency in pharmaceutical research.
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Cite this article as:
Zhang Zhoupeng, Zhu Mingshe and Tang Wei, Metabolite Identification and Profiling in Drug Design: Current Practice and Future Directions, Current Pharmaceutical Design 2009; 15 (19) . https://dx.doi.org/10.2174/138161209788682460
DOI https://dx.doi.org/10.2174/138161209788682460 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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