Metabolite Identification Services
Creative Animodel is devoted to offering a set of state-of-the-art metabolite identification services including structural elucidation, quantification and reactive metabolite characterization, etc. The high-level platforms and experienced researcher team endow us with the capabilities to meet your pharmaceutical demands.
Most drugs are converted into metabolites within the body. Pharmaceutical industries are mandated by regulatory agencies to identify metabolites of NCE. The generated metabolites modulating the efficacy of drugs may be pharmacological active or toxic (Figure 1). Reactive metabolites account for the big part of the unexpected deleterious effects of drugs. And a number of drugs have been withdrawn from the market or severely restricted in use due to toxicities. Therefore, metabolite identification is a crucial step to study the efficacy and toxicity of drug candidates at an early stage by investigating metabolite structure, metabolite quantification and reactive metabolites. The evaluation and design of drugs can be hence achieved after characterized these metabolites.
Figure 1. The general metabolism pathway of drug within the body.
Metabolite Structural Elucidation
Figuring out the structure of metabolites helps shed a light on compounds’ therapeutic potentials and safety. Creative Animodel performs computational prediction and experimental processing using multiple techniques, like LC/MS and NMR, to confirm metabolite structures. LC/MS is well suited for metabolite structure illustration due to its speed, resolution, selectivity, and sensitivity.
Metabolite quantification recommended by the European Bioanalysis Forum should be conducted from drug discovery phases, pre-clinical I phase to early clinical phase for a better understanding of their activity or toxicity of the dosed drug. LC/MS allows quantification of metabolite on a large scale by using internal standards, such as U-13C-labelled E.coli extracts.
Reactive metabolite has been suggested to be responsible for the negative effects of drugs, due to a process called as metabolic activation or bioactivation. Toxicity may be generated after reactive metabolite binding to cellular molecules, like enzymes, receptors, DNA and membranes. Analysis of GSH conjugates by LC/MS shed a light on reactive metabolite analysis.
1. Attia, S.M. Deleterious effects of reactive metabolites. Oxidative medicine and cellular longevity. 2010, 3(4): 238-253.
2. Dunn, W.B.;et al. Mass appeal: metabolite identification in mass spectrometry-focused untargeted metabolomics. Metabolomics. 2013, 9(1): 44-66.