Drug metabolism is the enzymatic biotransformation of xenobiotics into more polar, readily excretable metabolites. Cytochrome P450 enzymes account for the majority of Phase I oxidative reactions, while Phase II conjugation pathways — glucuronidation, sulfation, acetylation, and glutathione conjugation — further modify both parent compounds and Phase I metabolites to facilitate elimination.
Our Metabolism portfolio encompasses hepatic and extrahepatic microsomal fractions, recombinant metabolic enzymes, transporter-expressing cell lines, reaction phenotyping kits, inhibition assay systems, and metabolite identification reagents — supporting the complete drug metabolism characterisation workflow from early screening to regulatory-grade studies.
Drug metabolism serves two principal functions: inactivation of pharmacologically active compounds to terminate their effect, and bioactivation of prodrugs or stable compounds into reactive intermediates that may be associated with toxicity. The liver is the primary site of drug metabolism, with the highest concentrations of cytochrome P450 (CYP) enzymes — particularly CYP3A4, CYP2D6, CYP2C9, CYP2C19, and CYP1A2 — accounting for the biotransformation of the majority of marketed drugs. Extrahepatic metabolism in the intestine, lung, kidney, and brain contributes to the overall clearance and metabolic profile.
Accurate in vitro characterisation of metabolic pathways is essential for predicting in vivo clearance (CLint), identifying reactive metabolite risks, evaluating drug–drug interaction (DDI) potential through CYP inhibition and induction, and assigning the enzymes responsible for a compound's primary metabolic routes (reaction phenotyping). Our portfolio spans all key in vitro metabolism assay formats — from high-throughput microsomal stability screening through to definitive recombinant enzyme kinetics and soft-spot identification by mass spectrometry.
Liver microsomes, S9 fractions, cytosol, and hepatocytes are the foundation of in vitro metabolic stability and clearance prediction. Multi-species pools and gender-specific lots enable cross-species scaling and metabolic phenotype characterisation.
Recombinant enzymes expressed in baculovirus-insect cell or E. coli systems provide defined, single-enzyme activity for precise reaction phenotyping, kinetic parameter determination (Km, Vmax, CLint), and isothermal stability experiments without interference from co-expressed isoforms.
CYP inhibition — both reversible and mechanism-based (time-dependent) — is a primary driver of clinical drug–drug interactions. In vitro IC50 and Ki determination using probe substrates in human liver microsomes or recombinant enzymes provides the data required for prospective DDI risk assessment and regulatory submissions.
Phase II conjugation reactions enhance the polarity of drug molecules and their Phase I metabolites, facilitating renal and biliary excretion. UDP-glucuronosyltransferases (UGTs) and sulfotransferases (SULTs) are the dominant Phase II enzymes in drug metabolism, while reactive metabolite trapping assays identify electrophilic intermediates that may pose bioactivation risk.
The product catalogue below is ready to receive SKU data. Use the filter chips to browse by dimension. Each product entry carries a catalogue number, product name, category classification, species applicability, format, and a datasheet link.
[Cat#: ITS-0426-YL2]
[Cat#: ITS-0426-YL3]
[Cat#: ITS-0426-YL4]
[Cat#: ITS-0426-YL5]
[Cat#: ITS-0426-YL6]
[Cat#: ITS-0426-YL7]
[Cat#: ITS-0426-YL8]
[Cat#: ITS-0426-YL10]
[Cat#: ITS-0426-YL11]
[Cat#: ITS-0426-YL12]
[Cat#: ITS-0426-YL13]
[Cat#: ITS-0426-YL14]
[Cat#: ITS-0426-YL15]
[Cat#: ITS-0426-YL16]
[Cat#: ITS-0426-YL17]
[Cat#: ITS-0426-YL18]
[Cat#: ITS-0426-YL19]
[Cat#: ITS-0426-YL20]
[Cat#: ITS-0426-YL21]
[Cat#: ITS-0426-YL22]
[Cat#: ITS-0426-YL23]
[Cat#: ITS-0426-YL24]
[Cat#: ITS-0426-YL25]
[Cat#: ITS-0426-YL26]
[Cat#: ITS-0426-YL27]
[Cat#: ITS-0426-YL29]
[Cat#: ITS-0426-YL30]
[Cat#: ITS-0426-YL31]
[Cat#: ITS-0426-YL32]
[Cat#: ITS-0426-YL33]
[Cat#: ITS-0426-YL34]
[Cat#: ITS-0426-YL35]
[Cat#: ITS-0426-YL36]
[Cat#: ITS-0426-YL37]
[Cat#: ITS-0426-YL38]
[Cat#: ITS-0426-YL39]
[Cat#: ITS-0426-YL40]
[Cat#: ITS-0426-YL41]
[Cat#: ITS-0426-YL42]
[Cat#: ITS-0426-YL43]
[Cat#: ITS-0426-YL44]
[Cat#: ITS-0426-YL45]
[Cat#: ITS-0426-YL46]
[Cat#: ITS-0426-YL47]
[Cat#: ITS-0426-YL48]
[Cat#: ITS-0426-YL49]
[Cat#: ITS-0426-YL50]
[Cat#: ITS-0426-YL51]
[Cat#: ITS-0426-YL52]
[Cat#: ITS-0426-YL53]