ADME is the abbreviation of “Absorption, Distribution, Metabolism, and Excretion” of a drug, which represents the process of the body’s disposal of the drug after it enters the body. These four attributes of a drug determine the concentration, tissue distribution, and metabolic pathway of a drug in the body, which are useful for predicting the bioavailability and biological activity of a drug (that is, whether a drug can reach its target and produce corresponding therapeutic effects) It has very important reference value. Therefore, understanding the ADME properties of compounds is of great significance for the drug development process.
Drug development is a high-risk, high-investment, but also a high-return process. The earlier the ADME characteristics of the drug are evaluated and optimized in this process, the more compounds with poor ADME characteristics can be eliminated in time, which greatly reduces unnecessary investment and waste of resources in the later stage. AxisPharm can provide you with comprehensive ADME testing services, including high-throughput ADME screening, in vitro drug metabolism testing, drug permeability and transport experiments, etc.
AxisPharm Bioanalytical Labs is well equipped with all the necessary tools and instruments to perform in vitro ADME tests, can provide customers with reliable drug ADME characteristics testing services, and can design the most reasonable experimental plan according to the specific needs of customers, fully assisting your drug development process.
High-throughput ADME screening
As a powerful tool for early drug screening, high-throughput technology has been widely used in the discovery and optimization of lead compounds, and has made it possible to quickly and efficiently screen large quantities of compounds. Our high-throughput ADME screening service can be customized according to the specific requirements of customers to meet the special service needs of different customers. Equipped with advanced instruments and equipment, we can complete the screening of about 300 compounds within a week.
The ADME screening process mainly includes the following five steps:
-Plot the drug to be screened on the well plate
-MS/MS method optimization
-ADME detection and sample removal
–LC-MS/MS raw data collection and processing
– Archiving of analyzed data
Our high-throughput ADME services can include the following assays:
-Water Solubility (Thermodynamics & Kinetics)
– Metabolic stability (microsomal stability, plasma stability, hepatocyte stability, etc.)
– Permeability (PAMPA)
– protein binding (plasma, microsomes, brain tissue)
-CYP inhibition
-CYP analysis
– In vitro drug metabolism assay
-Clarify the main metabolic pathways of drugs and their metabolic enzymes
-Assess the effect of the tested drug on other drug metabolism processes and vice versa
We provide a variety of in vitro metabolic testing services, including but not limited to:
Hepatocyte Stability Assay
S9 stability test
Microsomal Stability Assay
Plasma stability testing
Metabolite Identification
CYP/UGT reaction test
CYP induction test
CYP inhibition test (single-point inhibition, time-dependent inhibition)
UGT inhibition assay (and other non-CYP metabolizing enzymes)
Drug Permeability and Transport Assays
Caco-2 osmotic transport assay (unidirectional or bidirectional)
MDCK/MDR1-MDCK Permeability Assay
Artificial Membrane Permeability Assay (PAMPA)
Transport experiment (P-gp, BCRP, BSEP, OAT1, OAT3, OATP1B1, OATP1B3, OCT1, OCT2, etc. optional)
Drug safety and efficacy are two of the most important aspects in the drug development process, and both are largely affected by drug metabolism pathways and drug-drug interactions. Since the drug is usually metabolized into one or more metabolites with enhanced or weakened activity after entering the body, the metabolic rate of the drug, the biological activity of the metabolite and the clearance process will directly affect the residence time of the drug in the body in active form. , which in turn affects the blood concentration and may cause toxic reactions. In addition, the interaction between drugs and drug-metabolizing enzymes will also affect the metabolic rate and retention time of other drugs in the body. Therefore, understanding the metabolic pathway of drugs is of great significance for better predicting drug toxicity or side effects and drug-drug interactions. At the same time, this information can also provide certain guidance for the formulation of drug regimens (including combined drugs).
The main purposes of drug metabolism assays include: Metabolic pathway identification
The ability of drugs to pass through biomembranes is an important factor affecting the absorption of drugs into the blood through the mucous membrane of the digestive tract and into various tissues and organs through the blood. Poor drug permeability can lead to poor absorption of the drug or affect its distribution in the body. The ability of drugs to penetrate membranes is mainly affected by two aspects: passive diffusion and active transport.