Metabolite identification plays a key role in drug discovery, preclinical development and clinical development. Metabolite identification studies are designed to screen metabolites and better understand the biotransformation capabilities of molecules. BOC Sciences provides rapid and efficient metabolite analysis services, and our scientific team performs metabolite identification studies to identify and confirm metabolic sites and corresponding structures. This information provides our clients with a sound scientific basis and accelerates drug development projects.
A metabolite is any substance produced during metabolism (digestion or other body chemical processes) and can also refer to the a by-product produced when a drug is broken down or metabolized by the body. Understanding drug metabolism by determining the formation of metabolites in in vitro or in vivo studies is essential for the interpretation of pharmacological, pharmacokinetic and toxicological data. In addition, pharmacologically active metabolites can significantly contribute to the overall treatment and side effects of a drug, and it can also be developed as a drug. Therefore, metabolites are critical to fully understand the mechanism of action of drugs.
The biotransformation reactions leading to metabolite formation can be divided into two main categories, namely phase I and phase II. Phase I reactions are functionalization reactions in which polar chemical groups are introduced by insertion of new polar functional groups or by alteration of existing functional groups by oxidation, reduction and hydrolysis reactions. In phase II reaction, small endogenous polar molecules are conjugated to functional groups formed in the first stage reaction; or direct conjugation of endogenous molecules occurs.
Examples of drug metabolites generated through biotransformation:
|Reduction of carbonyl to hydroxyl group
BOC Sciences' metabolite studies identify the major metabolites of a test drug, the specific metabolic pathways and the specific enzymes responsible for their metabolism to assess the impact of metabolites on drug safety and efficacy. There are two basic approaches used in in vitro metabolism studies to model drug metabolism in the human liver.
The analytical techniques used in metabolite identification mainly include liquid chromatography-mass spectrometry (LCMS), gas chromatography-mass spectrometry (GCMS) and nuclear magnetic resonance (NMR).