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.
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 Vitro Metabolite 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
