In Vitro Metabolism
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In Vitro Metabolism

The drug metabolic pathways and individual differences can significantly affect the drug metabolism rate, and lead to large differences in the concentrations of effective drug molecules and metabolites in the blood and tissues of the same organism. In order to balance drug safety and efficacy, drug metabolism and drug interaction testing for different individuals is required in the early stage of drug discovery to better predict drug toxicity, efficacy and side effects. BOC Sciences specializes in early in vitro metabolic assays for drug discovery, and can perform metabolic characterization services for drug candidates targeting both cytochrome P450 and non-P450 metabolic pathways. We have built robust test systems to define the absorption, distribution, metabolism and elimination (ADME) characteristics of drug candidates.

In Vitro Metabolism

Drug metabolism refers to the process by which drug molecules undergo complex biochemical processes in the body resulting in drug transformation or inactivation, which helps eliminate foreign substances from the body. In vitro drug metabolism is mainly used to determine the pathways and enzymes that affect the elimination of the tested drug and its metabolites, and can also be used to evaluate the impact of the tested drug on the metabolism of other drugs. Metabolism of most drugs occurs primarily in the liver. Other organs may also be involved in metabolism, such as the spleen, intestines, lungs, kidneys, and skin. In the liver, drug metabolism is primarily measured by phase I and phase II enzymatic activity. Some drugs are metabolized by Phase I or Phase II enzymes only, while others are metabolized by both Phase I and Phase II enzymes.

The purpose of metabolite analysis and identification is to identify the metabolic pathways of drug candidates. BOC Sciences provides rich enzymatic substrates for clients at all stages of drug discovery and development, including in vitro metabolism in hepatocytes, liver microsomes, S9, recombinant enzymes, or extrahepatic tissue. Our in vitro ADME models provide customers with decision-making data for lead optimization and selection and help them design preclinical and safety studies.

BOC Sciences' metabolic analysis system can measure the in vitro clearance and metabolism of drugs in hepatocytes, liver microsomes, S9, recombinant enzymes, or extrahepatic tissues. Our metabolic stability assays cover a broad range of compounds, including low-, intermediate-, and high-clearance compounds. Our research data can be used to measure compound half-lives, calculate intrinsic clearance and predict human pharmacokinetic profiles.

With extensive experience in drug discovery, BOC Sciences also provides detection and analysis of extrahepatic metabolism, including intestine, brain, kidney, skin, and plasma. Our services includes in vitro metabolite profiling and identification of extrahepatic tissues, metabolic clearance of extrahepatic tissues, drug interactions in extrahepatic tissues, and drug metabolism by immune cells.

Reactive metabolites refer to biologically active metabolites that may produce adverse reactions or pharmacological effects. BOC Sciences provides characterization and screening services for reactive metabolites with short turnaround and cost-effectiveness. We performed multivariate data analysis using liquid chromatography and high-resolution mass spectrometry after stabilization of highly reactive and short-lived metabolites by trapping agents, such as glutathione tri-peptide (GSH), potassium cyanide (KCN) or semicarbazide.

Testing the interaction of candidate drug molecules with other drugs or substances in the body is a key component of drug discovery. Common metabolic drug-drug interactions are inhibition and induction of drug metabolic enzymes. BOC Sciences has established a complete ADME detection system to characterize drug-drug interactions, including cytochrome P450 induction and inhibition, UGT inhibition and time-dependent inhibition.

Reaction phenotyping researches are primarily used to identify the enzymes responsible for the biotransformation of compounds. BOC Sciences has the ability to provide in vitro reaction phenotyping researches that meet regulatory expectations, including CYP enzymes, non-CYP enzymes, and conjugated enzymes. Our reaction phenotyping characterization provides metabolic data information for the sample to be tested, which can be used to assess victim DDI potential and provide useful information for clinical study design.

BOC Sciences also provides screening, optimization, synthesis, and production services for candidate drug metabolites after metabolites have been identified through metabolic studies. We employ recombinases, liver microsomes or biomimetic catalysts for scale-up metabolite production, which are then characterized and isolated using NMR and chromatography.

BOC Sciences provides high-quality in vitro metabolic services to evaluate the metabolic pathways of your lead compounds in the liver and extrahepatic tissues (spleen, intestine, lung, kidney, and skin). We also analyze samples using state-of-the-art UPLC/HR-MS equipment. Please contact us to learn more about our services.