Absorption, distribution, metabolism, and excretion (ADME) analysis is an important step in the drug discovery and development process to evaluate the pharmacokinetic properties and to evaluate the potential efficacy. In vitro, cellular structures, subcellular structures, enzymes, and 3D cell models are usually used to evaluate the ADME properties of drug candidates.
Solubility and permeability are key parameters governing drug absorption. Solubility and dissolution studies under pH changes are important in vitro experiments to simulate behavior under physiological conditions. Parallel artificial membrane permeability assay (PAMPA) is a widely used method to measure permeability based on lipid artificial membranes that mimic different membrane types, such as blood-brain barrier, mitochondrial membrane, etc. Since protein binding plays an important role in the pharmacokinetics and pharmacodynamics of drugs, in vitro plasma protein binding assays are used to assess the binding degree of a drug to proteins in plasma, which can provide a guide to the pharmacokinetic distribution. In vitro metabolism assays mainly include metabolic enzyme kinetic assays using hepatic enzymes, such as CYP450, and metabolic stabilization and metabolite characterization assays using hepatic microsomes or hepatocytes. Studies of drug excretion in vitro include determining the metabolic pathway of the drug and measuring the excretion rate. Renal tubular cell models are used to assess the renal excretion and hepatobiliary tract tissues are commonly used to study biliary excretion. These in vitro assays can provide preliminary ADME information for early drug screening, designing, optimization, and safety assessment. Compared to in vivo experiments, in vitro experiments can be used to rapidly screen a large number of candidate compounds and provide detailed information on metabolism and transport mechanisms. In addition, the use of in vitro assays can reduce the use of animal models and are more cost-effective.
Amerigo Scientific offers a wide range of in vitro ADME products including metabolic stability kits, metabolic phenotype kits, cytochrome P450 enzyme inhibition (IC50) kits, liver and intestine microsomes, S9 and cytoplasm of different species, etc.
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