In Vitro ADME

Assessing the absorption, distribution, metabolism, and excretion (ADME) of lead compounds during drug discovery and development is an essential component of drug preclinical development. The In vitro ADME studies provide key physicochemical and pharmacological properties that drive the safety and efficacy of drug molecules. In general, the first step after determining that a drug candidate has a pharmacological effect on a target of interest is ADME in vitro characterization.

  • Physicochemical Characterization

The physicochemical properties of potential drugs, including water solubility, lipophilicity, stability, distribution coefficient LogD, and particle size, significantly affect the rate and extent of drug entry into the systemic circulation. It is critical to understand the physicochemical properties of a compound before actual administration, which is the cornerstone of the development of pharmaceutical formulations. BOC Sciences provides customers with cost-effective, standardized and customized ADME physicochemical analysis:

  • Aqueous Solubility Assays
  • Lipophilicity Assays
  • Stability Assays
  • Distribution Coefficient LogD Assays
  • Particle Size Assays
  • Permeability and Absorption

Drug permeability is a key factor affecting drug absorption and distribution. The sensitivity and permeability of drugs to transporters determine the transmembrane permeability of drug molecules. Assessment of compound permeability by cell monolayers is a good indicator of intestinal permeability and oral bioavailability. For example, parallel artificial membrane permeability assay (PAMPA) provides a high-throughput, acellular method for predicting passive transcellular intestinal absorption, the process by which most small-molecule drugs enter the circulation. In addition, drug formulation, physicochemical properties, and route of administration also affect drug absorption. BOC Sciences has a comprehensive selection of products and services for drug discovery, and our permeability and absorption analysis methods include:

  • Dermal Absorption
  • Parallel Artificial Membrane Permeability Assay (PAMPA)
  • Caco-2 Permeability
  • MDR1-MDCK Permeability
  • Transporter Substrate Identification
  • Drug Distribution

Drug distribution refers to the reversible movement of drug molecules from the blood to various tissues. The physicochemical properties of drugs, permeability, tissue and plasma protein binding and other factors will affect the distribution of drugs in the body. For example, when drugs bind to proteins circulating in the blood, it is difficult to penetrate effectively from blood vessels into tissues. However, when the drug is tightly bound to proteins in specific tissues, it also prolongs the action time and accumulation time of the drug. BOC Sciences offers several in vitro binding assays, including plasma protein binding, brain tissue binding, microsome binding, and plasma partitioning. We provide flexible custom contract development services according to the specific requirements of our clients.

  • Plasma Protein Binding
  • Blood Plasma Partitioning
  • Brain Tissue Binding
  • Microsomal Binding
  • In Vitro Metabolism and Excretion

The detection of metabolic pathways in vivo and the identification of metabolites will not only affect the safety and efficacy of drugs, but also affect the strategy and design of biological analysis. Drug metabolism and excretion normally occur in the cytochrome P450 (CYP) enzyme family in the hepatic endoplasmic reticulum. In addition to the liver, cellular metabolism can also occur in the gastrointestinal tract, lung, skin, and nasal mucosa. BOC Sciences offers a wide range of liver microsomal stability assays, including CYP450, flavin monooxygenase, carboxylesterase and epoxide hydrolase. Our metabolic stability assays provide intrinsic clearance of compounds using advanced mass spectrometry instruments.

  • Plasma Stability
  • Blood Stability
  • Hepatocyte Stability
  • Microsomal Stability
  • Extrahepatic Metabolism
  • Metabolic Stability Assay
  • Intestinal/Lung Metabolic Stability
  • Reactive Metabolite Analysis
  • Drug-Drug Interactions
  • Reaction Phenotyping
  • Metabolite Production
  • Metabolite Profiling and Identification

With leading experts in formulations, BOC Sciences is committed to providing customers with reliable screening results in the early stages of drug discovery at a cost-effective rate. We have the ability to provide standardized and customized ADME parametric analysis. Please contact us to learn more about our services.

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