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Medicilon's Metabolite Identification Services

2020-08-25
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Met-ID Service Platform

The MetID team of Medicilon is composed of experienced scientists. We provide fast and reliable in vivo and in vitro MetID and reactive metabolite capture services. We also support new drug screening and domestic and foreign IND filings. Since the establishment of MetID team, Medicilon has successfully completed a large number of different types of research projects for the clients, including the challenging peptide MetID research.

In the process of drug development, it is necessary to determine the metabolic characteristics of drugs, which can be determined by in vitro and in vivo test methods at different development stages. In vitro tests can use liver microsomes, liver slices or hepatocytes from different animals and humans, and in vitro tests should usually be performed before the start of clinical trials.

Metabolite Identification (MetID) plays an important role in the field of new drug development.

  •    -In the lead optimization stage, MetID can help to locate the metabolic soft spots, so that medicinal chemists can make targeted structural modifications to improve the pharmacokinetic characteristic.

  •    -According to the NMPA and FDA guidelines, the identification and comparison of in vitro metabolites is an important basis for the selection of experimental animal species at the IND-Enabling stage.

  •    -In addition, reactive metabolites can covalently bind to biological macromolecules in the body, leading to toxic reactions.

  • Therefore, early screening of reactive metabolites by GSH Trapping will help reduce the risk of later development.

    Significance of Metabolite Identification
    The significance of drug metabolism to the discovery and development of new drugs Drug metabolism research runs through the entire industry chain of innovative drug research and development. In the drug discovery stage, candidate compounds with poor metabolic properties will be found in time through drug metabolism screening, and in cooperation with medicinal chemists, through Structural modification reduces metabolic instability and avoids reactive metabolites through rational molecular design; in the preclinical development stage of the drug, it cooperates with pharmacodynamic research and safety evaluation to complete preclinical comprehensive evaluation, and is a clinical phase I drug in humans. A solid foundation for metabolic research. Metabolites may be pharmacologically active, toxic, or cause drug-drug interactions; therefore, metabolite identification is critical at many stages of drug discovery and development. 
    Want to expedite MetID research? Selecting a Rapid MetID Lead Optimization Solution
    Understanding the biotransformation of a compound during lead optimization can enhance the properties of a lead candidate, enabling you to make informed decisions early and avoid costly development schedule delays.
    1.   -Obtain early cross-species comparison information to support compliance with MIST, ICH M3 and EMA/FDA DDI guidelines, including proper selection of preclinical toxin species

    2.   -Targeted modifications to alter clearance properties

    3.   -Mitigate risks associated with potential drug-drug interactions

    4.   -Reduce reactive metabolites

    5.  -Early detection of potentially unique or disproportionate human metabolites

    Metabolite identification (MetID) plays an important role in drug discovery and development process. During the lead optimization stage, early MetID study can help identify the metabolic “soft spots”, so medicinal chemists can make appropriate structure modification to improve the pharmacokinetic properties of the compounds. During the IND-enabling stage, the information obtained from cross-species metabolite profiling can guide the selection of animal species for safety assessment, which is the approach advocated by the guidance documents from regulatory agencies. In addition, reactive metabolites may trigger organ toxicity, especially hepatic toxicity. Early screening for reactive metabolite formation by GSH trapping can help minimize this risk.

    Medicilon recently added Thermo Scientific Q Exactive HF-X BioPharma, one of the most advanced high resolution mass spectrometers (HRMS), into the powerful arsenal of its DMPK/BAS Division. QE HF-X is a Quadrupole-Ultra High-Field-Orbitrap mass spectrometer with a resolution up to 240,000 FWHM, high precision (< 1ppm), high sensitivity (with High Capacity Ion Transfer Tube and Electrodynamic Ion Funnel), high scan speed (up to 40 Hz), and high mass stability (without the need for frequent recalibration), outperforming the majority of commonly used HRMS. It is also complemented by Thermo Vanquish Flex UHPLC, Diode Array Detector (DAD), Variable Wavelength Detector (VWD), Compound Discoverer software, and BioPharma Finder software.

    Medicilon 's Metabolite Identification Services

    Medicilon 's Metabolite Identification Services

    Our MetID team is consist of experienced scientists who are capable of conducting fast and reliable in vivo and in vitro metabolite identification and reactive metabolite capture services, and supporting new drug screening and IND application in different countries. Since its establishment, we have successfully assisted in many different types of research projects for customers, including peptide MetID.

    Our seasoned MetID scientists utilize this high-end UHPLC-HRMS system to provide fast and reliable in vivo and in vitro metabolite identification and GSH trapping services, and have successfully completed many different types of studies from clients around world, including some challenging peptide MetID works.

    List of Services (Available for Early Discovery and IND-Enabling)

    In VitroMetabolite Identification in Following Matrices

    • Liver Microsomes

    • Hepatocytes

    • S9 Fraction

    • Cytosol

    • Plasma

    Screening for Reactive Metabolites

    • GSH Trapping

    In Vivo Metabolite Identification in Following Matrices

    • Plasma

    • Urine

    • Bile

    • Feces

    • Tissues and organs

    The MetID Service includes

    Identification of metabolites in vitro

    • Liver microsomes

    • Hepatocytes

    • S9

    • Hepatocyte fluid

    • Plasma

    Identification of reactive metabolites

    • GSH Trapping

    Identification of metabolites in vivo

    • Plasma

    • Urine

    • Bile

    • Feces

    • Tissues and organs

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