Metabolic stability & identification
- Overview
- Services
- Features
- Explore Other Options
Drug metabolism and stability are key factors that influence a compound's pharmacokinetic properties, therapeutic activity, and safety profile.
Drug metabolism primarily occurs in the liver, but also involves extrahepatic tissues such as the intestine, kidney, and plasma. It is mediated by a variety of enzymes, mainly phase I (functionalization) and phase II (conjugation) enzymes, such as cytochrome P450s (CYPs), flavin-containing monooxygenases (FMOs), esterases, UDP-glucuronosyltransferases (UGTs), sulfotransferases (SULTs), and glutathione-S-transferases (GSTs). The rate and pathways of drug metabolism and the formation of active or toxic metabolites are determined by these enzymes.
Drug stability refers to the resistance of a compound to enzymatic and chemical degradation in vivo. It is an important consideration in drug design, as low stability can lead to rapid clearance, low systemic exposure, and poor therapeutic index, while high stability can result in accumulation, prolonged half-life, and potential toxicity. Therefore, achieving an optimal balance between stability and reactivity is a key challenge in lead optimization and candidate selection.
The Metabolic Challenge in Drug Development
Bioavailability
First-pass metabolism can drastically reduce systemic exposure.
Half-life
Rapid metabolic clearance may necessitate frequent dosing.
Safety
Reactive or pharmacologically active metabolites can cause toxicity or off-target effects.
Drug-Drug Interactions
Competition for metabolizing enzymes (e.g., CYP450s) may alter the efficacy of co-administered drugs.
Key Services
Our Metabolic Stability & Identification platform integrates cutting-edge in vitro assays, high-resolution mass spectrometry, and expert data interpretation to deliver actionable insights at every stage of drug development. We support:
Early Screening
Rapid assessment of metabolic lability to prioritize lead compounds.
Mechanistic Studies
Elucidation of metabolic pathways and enzyme contributions.
Regulatory Compliance
GLP-ready assays for IND/NDA-enabling packages.
Evaluates drug metabolism using primary hepatocytes (human & preclinical species) to assess Phase I/II enzyme activity with high physiological relevance for in vivo predictions.
Analyzes combined Phase I/II metabolism using liver S9 fractions (microsomes + cytosol), ideal for high-throughput screening of compounds requiring conjugation metabolism.
Measures CYP450-mediated Phase I metabolic stability in liver microsomes to determine intrinsic clearance rates and half-life.
Tests chemical/enzymatic degradation in plasma (e.g., esterase hydrolysis), critical for peptide drugs and prodrug development.
Pinpoints metabolic enzymes (CYPs/UGTs) involved in drug clearance through recombinant enzyme phenotyping for DDI assessment.
Why Choose Us?
Diverse in vitro systems
Human and multiple preclinical species hepatocytes, microsomes, S9 fractions, and plasma.
Cutting-Edge Technology
High-resolution LC-MS/MS (Q-TOF, Orbitrap) and automated platforms for precise metabolite identification & quantification.
Integrated service offerings
From early metabolic stability screening to comprehensive metabolite profiling to regulatory submission support.
Transparent reporting
Visual representation of CLint, t1/2, metabolite structures with practical recommendations.
Experienced scientific support
Expert knowledge of enzymology, pathway elucidation for early risk prediction.
Flexible study design
High-throughput screening or tailored studies to meet your needs.
Explore Other Options
