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Understanding the metabolic pathway and the structure of the metabolites is important for the design and optimization of lead compounds, safety assessment in drug development, and support of IND and/or NDA filings. MetID studies help understand the clearance pathways, find active/reactive metabolites, and discover human disproportionate/unique metabolites to support the evaluation of drug efficacy and safety.

MetID

We provide comprehensive MetID services, including preclinical in vitro and in vivo MetID, clinical human MetID (FIH, SAD, and MAD) and metabolites in safety testing (MIST) study, metabolite biosynthesis, and structural characterization. The services cover from the lead compound optimization in drug discovery stage to the clinical trial stage, also including the radiolabeled ADME (absorption, distribution, metabolism, and excretion) study in animals and AME in humans.

Our scientific team offers customized services to solve complex problems in metabolism studies and ensure the timely delivery of high-quality reports to meet the requirements of the regulatory authorities (NMPA, FDA, EMA, etc.).

Overview
Metabolite Biosynthesis and Structural Characterization
  • In vitro incubation biosynthesis of the target metabolites and their structural characterization
  • Animal in vivo biosynthesis of the target metabolites and their structural characterization


Services
Metabolites in Safety Testing (MIST)
  • MetID in toxicology animal plasma from multiple ascending doses in a steady state
  • MetID in human MAD (multiple ascending doses) plasma in steady state
  • Compare the exposure of the major metabolites (with relative abundance ≥10% from human) between human and animal

In Vitro Metabolite Identification
  • Metabolic soft spot analysis and identification
  • Reactive metabolite trapping (glutathione, cysteine, methoxamine, etc.)
  • MetID in liver microsomes
  • MetID in hepatocytes
  • MetID in S9
  • MetID in tissue homogenates
  • MetID in in vitro  plasma or blood

In Vivo Metabolite Identification
  • MetID in animal samples (plasma/blood, urine, feces, bile, tissue, etc.)
  • MetID in human samples (plasma, urine, feces, etc.)
    • MIST (metabolite in safety testing)
How does metabolite profiling and identification assist in preclinical studies of drugs?    

The metabolite profiling and identification helps in understanding how the drugs are metabolized and eliminated from the body. It provides information on the metabolic pathways involved, the metabolites formed, and their relative abundance over time. This information is essential for optimizing drug dosing, predicting drug-drug interactions, and assessing the potential toxicity.

Understanding characteristics and structural assignments of the metabolites in different preclinical species (cross-species comparison) can help identify human-specific metabolites or those found at disproportionately high levels in humans in comparison to toxicity models. Comparing the in vitro and in vivo metabolism data of animals can determine if there is a good in vitro-in vivo correlation of metabolism, which can further ensure the reliability of using in vitro metabolism to predict in vivo metabolism in humans.

 What is the metabolite profiling and identification?                                               
The metabolite profiling and identification is the process of analyzing and characterizing the metabolites present in a biological sample, also known as the qualitative and semi-quantitative study of the biotransformation of a compound in in vitro and in vivo (animals and human). The parent drug is transformed into the metabolites by the action of biological enzymes (metabolic enzymes). Understanding the transformation can be helpful in anticipating of safety concerns arising from disproportionate toxic metabolites, predicting drug-drug interactions, and understanding routes of elimination.
 How soon can I expect to receive my metabolite identification results?
The timeline for receiving metabolite identification results depends on the complexity of the test compounds and the type of the assays. For regular small molecule compounds, the study can be completed in several days to two weeks during the early screening stage and generally takes four weeks for IND (Investigational New Drug) filing. For new modalities or special compounds, the process extends to approximately four to six weeks. It would be great to contact your study director if you have any questions about the availability of the study results.

FAQs
How to do the metabolite profiling and identification (MetID)?                                               
MetID of both in vitro and in vivo metabolic samples was performed by using ultra-high performance liquid chromatography (UPLC) -ultraviolet detector (PDA) -high-resolution mass spectrometry (Q-TOF/Orbitrap) tandem technology. Combined with the nuclear magnetic resonance spectroscopy (NMR) technique, the accurate structure of the metabolite was identified. If working with the radiolabeled compound, the LC-UV-HRMS with radioactivity detector can be used to detect and identify the metabolites.