What items are included in the in vitro ADME experiment?



In vitro research refers to research projects such as metabolic stability, P450 induction and inhibition, metabolic pathway research, metabolite identification, etc. The animals involved include rats, mice, rabbits, dogs, monkeys, etc.

AxisPharm is a San Diego based bioanalytical LC/MS/MS service provider with more than 25 years experience in the field. Our bioanalytical chemistry department specializes in developing and validating robust bioanalytical methods for PK/TK sample analysis of small molecules, proteins, and metabolites using LCMS/MS (HPLC, UPLC, on-line SPE), HPLC/UV, and HPLC/FL. We have experience analyzing API and metabolites in various biological matrices and can provide bioanalytical support throughout all the stages of drug development.

AxisPharm Labs is well equipped with all the necessary tools and instruments to perform in vitro ADME tests.

In the area of ​​in Vivo DMPK, AxisPharm offers services in species such as mouse, rat, dog, monkey, cat, rabbit, guinea pig, and etc.

Physicochemical Properties of Drugs
– Solubility
– Oil-water partition coefficient: LogD
– protein binding
Blood to Plasma Ratio
– chemical stability

Drug absorption and transporter experiments
– Intestinal absorption/Pgp binding assays: Caco-2/PAMPA, bidirectional transport assays, intestinal permeability, Pgp substrate/inhibitor confirmation
– Transdermal absorption: animal skin, skin permeability
– Permeability evaluation: PAMPA, Caco-2, MDCK
– Transporters: P-gp, BCRP, BSEP, MRP2, OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, MATE1, MATE2

Distribution test: determination of plasma protein binding rate, plasma stability test
– Plasma protein binding: different species of plasma, equilibrium dialysis/ultrafiltration, molecular exclusion (SHLC, macromolecules), plasma drug stability, comparative studies of different species
– Whole blood distribution: drug concentration analysis of different blood components (whole blood/plasma concentration ratio), blood drug stability

Drug metabolism research: metabolite speculation, metabolite confirmation, metabolic pathway speculation, metabolic pathway confirmation, metabolic phenotype research, liver microsome metabolism test, CYP450 inhibition test, CYP450 induction test
– Cytochrome P450 inhibition assay: human liver microsomes and cDNA expression enzymes, CYP subtypes: 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 & 3A4, standard substrates, IC50, Ki, time-dependent inhibition (TDI)
– Cytochrome P450 induction experiment: fresh liver and human hepatocytes, CYP isozymes: 1A2, 2C9, 2C19, 3A4, etc.

Drug metabolites: hepatocytes of different species, liver metabolic stability study, metabolite identification and structure confirmation by LC-MS/MS, inter-species comparative study, drug-drug interaction, transmembrane transport test
In vitro toxicology

Hepatotoxicity: Evaluation of General Toxicity and Toxic Mechanisms
– Cardiotoxicity
– Genotoxicity