Metabolism is one of the most important elimination pathways and represents the major route of elimination for the majority of drugs. The drug-metabolizing enzymes that contribute significantly to the elimination pathway of compounds are cytochrome P450, UDP-glucuronosyltransferase, aldehyde oxidase, and sulfotransferase. Understanding the mechanism of compound clearance is the first step in successfully predicting human clearance. Accurate prediction of the clearance of these enzymes in humans using in vitro and in vivo tools is critical for the success of drug candidates in human translation.
Creative BioMart Consulting specializes in providing enzyme-based drug metabolism consulting services to biotechnology companies and the pharmaceutical industry. We can help you achieve your research and biomarker validation goals using precise and well-validated methods. We have extensive research experience in the field of drug-metabolizing enzymes, including their major isoforms, tissue distribution, generic polymorphisms, substrate specificity, species differences, catalytic mechanisms, in vitro-ex vivo extrapolation and the use of optimal assay significance conditions and relevant animal models. We are committed to providing useful information for your entire drug discovery and development cycle.
Creative BioMart Consulting can provide enzyme-based drug metabolism consulting, including biochemical activation of drug-metabolizing enzymes, their functions, mechanisms of action, and the effects of different contaminants on drug-metabolizing enzyme action and function. We can also help you study the role of drug-metabolizing enzymes in a wide range of diseases, including metabolic, cardiovascular, neurological, physiological, and inflammatory diseases. We offer drug metabolism enzyme consulting including but not limited to
Enzyme Classes | Types of drugs metabolized |
---|---|
Cytochrome P450 enzymes | Practically 90% of all drug substances |
Flavin-monooxygenases | Compounds with secondary and tertiary amines or sulphydryl groups (chlorpromazine, desipramine, methimazole) |
Prostaglandin H synthase (COX) | PAH-diols, aflatoxin B1, aromatic amines |
Alcohol/aldehyde dehydrogenases and oxidases | Various compounds with alcohol and aldehyde functions (ethanol) also some heteroaromatic systems |
Monoamine oxidase (MAO) | Selegiline, moclobemide |
Esterases/hydrolases/peptidases | Compounds with cleavable ester/amide bond (procaine, succinylcholine, lidocaine) |
UDP-glucuronosyl transferases | Most drugs with suitable O-, S- and N-functional groups or produced via oxidative metabolism (morphine, diazepam paracetamol) |
Sulphotransferases (SULT) | Phenols, alcohols, aromatic amines |
GSH transferases (GST) | Epoxides, arene oxides, nitro groups, hydroxylamines (ethacrynic acid) |
N-acetyltransferases (NAT) | Amines (sulphonamides, isoniazid, clonazepam, dapsone) |
Methyl transferases | Catecholamines, phenols, amines (L-dopa thiouracil) |
Note: If our list of enzymes does not meet your needs, our team of experienced scientists can create a custom solution specifically for your area of interest.
Creative BioMart Consulting has many years of experience in drug metabolism research. We aim to help you develop more accurate predictive methods and models to address these challenges in drug development. If you are interested in our services, please feel free to contact us.