Although the liver plays the major role in drug metabolism, other organisms are also present drug metabolizing. Creative Biolabs has worked extensively on a wide variety of metabolism studies. As part of our in vitro metabolism service, we provide extrahepatic metabolism service to measure the metabolism of particular drugs in extrahepatic sites.

Extrahepatic Metabolism

Metabolic reactions in both hepatic and extrahepatic tissues can be classified as phase I (functionalization phase) and phase II (conjugation phase) reactions depending upon the end product formed. Phase I reactions are mainly oxidative, reductive or hydrolytic, among which oxidative pathways play the major role and CYP enzyme family is the major oxidative enzyme. In phase II reactions, the parent drug or its phase I metabolite is conjugated with an endogenous substrate by specific enzyme systems (such as glutathione-S-transferases and UGT).

Metabolic enzymes are distributed in the microsomal and cytosolic fractions of different tissues. Microsomal enzymes control liver metabolism, whereas extrahepatic metabolism is manipulated by cytosolic enzymes. Creative Biolabs assesses the cytosolic enzyme activity by incubation of extrahepatic samples (gastrointestinal tract, kidneys, lungs, skin and brain) with the drugs of interest.

Extrahepatic Metabolite Profiling and Identification

The procedure of extrahepatic metabolite profiling is the same as that in liver samples. All the samples are available from multiple species for cross-species metabolite profiling. We measure compound degradation, isolate of metabolites and elucidate the chemical structure by a variety of methods, of which the high-resolution mass spectrometry (HR-MS) is the major tool for metabolite identification both qualitatively and quantitatively. We are also able to detect radiolabeled chemicals for analysis of different types of chemistry.

Metabolic Clearance in Extra-Hepatic Material

Creative Biolabs provides metabolic stability studies to measure the half-life, in vitro clearance, and AUC of a chemical. This assay can be used to evaluate clearance rate in skin and intestine microsomes, blood and plasma. All the samples are available from multiple species for Interspecies comparisons. For more detail information, please visit our metabolic stability studies website.

Drug-Drug Interaction in Extra-Hepatic Material

Creative Biolabs has established a full portfolio of assay systems to provide our customers overall information concerning the DDI potential of investigated compounds. We provide CYP inhibition test, UGT inhibition test, CYP induction test, UGT induction test, CYP-reaction phenotyping assay, UGT-reaction phenotyping assay and some transporter-mediated DDI assay to investigate drug-drug interaction in extra-hepatic material. The result is analyzed by UPLC-MS/MS technology.

Drug Metabolism by Immune Cells

Drug metabolism may evoke immune cell reactions. The reactive metabolites of a drug can be directly or indirectly toxic to cells, which might stimulate innate immunity, or might bind to protein to generate neoantigens for cellular and humoral responses. Creative Biolabs provides reactive metabolite analysis to determine the effect of drug metabolism on immune cells.

For more detailed information, please feel free to contact us or directly sent us an inquiry.

Reference

  1. Krishna D R and Klotz U (1994). “Extrahepatic metabolism of drugs in humans.” Clin Pharmacokinet 26(2):144-160.

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