MetID_Metabolite Identification_In Vivo Metabolite Identification_In vitro Metabolite Identification services

Metabolite Identification (MetID)

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 oversees IND filings. Since the establishment of MetID team, Medicilon has successfully completed multiple different types of research projects for clients, including challenging peptide MetID research.

Download

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 stage development.
More "Drug R&D Platforms":
Medicinal Chemistry
In Vitro Pharmacokinetic Assays
In Vivo Pharmacokinetic Assays
IND Filings Services

Medicilon Metabolite Identification (MetlD) Service Platform

High Resolution Mass Spectrometer （HRMS） High Resolution Mass Spectrometer (HRMS) is an essential tool for metabolite identification research. The Bioanalysis Department of Medicilon utilises Thermo Scientific Q Exactive HF-X Quadrupole-Ultra High-Field-Orbitrap Mass Spectrometer, which is one of the most advanced HRMS. Its resolution is up to 240,000 FWHM, and has high-quality accuracy ( < 1ppm, which can accurately fit the molecular formula), high sensitivity (equipped with a new high-capacity ion transfer tube and electric ion funnel, which can detect nanogram samples), high scanning speed (Up to 40 Hz), high stability (no need to frequently calibrate the mass axis), which is better than the IT-TOF, TripleTOF, QTof, LTQ-Orbitrap, QE Focus and QE Plus, the most common equipment in the industry. For liquid chromatography, Medicilon uses Thermo Fisher’s Vanquish Flex UHPLC and DAD detector and Thermo Fisher’s Compound Discoverer software for data analysis. UHPLC-UV-QE HF-X

MetID Research Support New Drug Discovery and Filing

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

FAQs

What is the Explanation for the Clearance (CL) > Hepatic Blood Flow (Qh) in the In Vivo PK Test in Animals?

(1) The liver is the main organ of drug metabolism, but not the only way of drug elimination. There is also renal elimination, etc.
(2) The drug is unstable in the blood, and the clearance of the drug does not have a hepatic effect.
(3) In some cases, when the drug concentration in red blood cells is much higher than that in plasma, the calculation of proper clearance cannot be approximated by the drug concentration in plasma.
(4) In individual cases, metabolism or uptake by the lungs occupies a significant role.
What Should Explain Bioavailability F > 100% in Animals' In Vivo PK Test?

(1) Dose deviation due to administration error.
(2) Nonlinear pharmacokinetics (Nonlinear PK).
(3) High bioavailability and individual variability in the DMPK properties of the drug, with IV and PO, given to different groups of animals.
(4) Overestimation of PO AUC or underestimation of IV AUC due to unreasonable sampling points.
(5) IV samples were left for extended periods, and compounds were unstable in plasma.
(6) When administered as a racemate, the faster-clearing enantiomer is converted to the slower-clearing enantiomer in the GI tract.
What Should be Done for Significant AUC Differences In Vivo PK Tests in Animals?

(1) The reasons for large differences can be summarized as poor solubility of the compound or solubility being subject to significant fluctuations in digestive tract pH.
(2) Improve the formulation and adjust the digestive tract PH value.

Relevant laboratories

Return