ADME/Tox Research
Services
The most rapid path to sound decision making.
For years, drug developers require faster and more predictive compound screens to reduce time-to-market and potential drug-drug interactions. BD Biosciences ADME contract research services organization works as an extension of a client’s team to provide reliable data and faster results. Utilizing state-of-the art techniques, products, and equipment,
BD Biosciences is able to assist clients in screening for viable drug candidates during drug discovery or by preparing regulatory agency submission-quality reports for your drug development compounds.
Learn more about our Discovery Services
CYP Inhibition Service with RapidFire®
High throughput CYP Inhibition service with FDA-recommended probe substrates
High Throughput Reaction Phenotyping
Enzyme identification by substrate loss analysis using BD Supersomes™ enzymes
Metabolic Stability in Microsomes
Assays performed in human and animal microsomes to predict the intrinsic clearance or metabolic half life of a test article
Metabolic Stability in Hepatocytes
Metabolic stability in cryopreserved hepatocytes from human or preclinical species
Permeability and Transport Testing
Permeability testing and P-gp transport and inhibition screening across Caco-2 and MDR1-LLC-PK1 monolayers
Plasma Protein Binding
High throughput, cost-effective equilibrium dialysis method
Sample Data
We’ve highlighted some sample data from our discovery services.
Correlation data between conventional LC/MS at BD Biosciences and Rapidfire® at Biocius life sciences
Data from 8 different enzyme/substrate pairs and 1 to 3 inhibitors for each pair was generated using traditional LC/MS/MS at BD Biosciences and RapidFire® technology at BIOCIUS Life Sciences. Inhibitors include ketoconazole, α-naphthoflavone, montelukast, S-benzylnirvanol, sulfaphenazole, azamulin, paroxetine, ticlopidine, S-fluoxetine, tienilic acid, verapamil, and diltiazem.
Historical assay performance for high throughput reaction phenotyping using BD Supersomes enzymes
In vitro half-life results obtained for positive controls under the conditions listed in the table. Boxes represent the 25th-75th percentile, the line indicates the median, error bars indicate the 90th and 10th percentiles, and circles represent outliers outside the 5th/95th percentiles. Data was obtained using multiple lots of BD Supersomes enzymes.
Historical assay performance for metabolic stability in human, rat, and mouse liver microsomes
In vitro intrinsic clearance results obtained for positive control compounds in human (HLM), rat (RLM), and mouse (MsLM) liver microsomes. Boxes represent the 25th-75th percentile, the line marks the median, error bars indicate the 90th and 10th percentiles. Data was obtained using multiple lots of microsomes.
Time course of ethoxycoumarin metabolism in human cryopreserved hepatocytes
Time course of ethoxycoumarin metabolism in a 10-donor pool of cryopreserved hepatocytes showing the expected linearity in formation of metabolites.
Efflux transporter activity in Caco-2 and LLC-PK1 cell monolayers
P-gp, BCRP, and MRP2 transporter activity assessment in Caco-2 and LLC-PK1 cell monolayers. Data represents efflux ratios of each probe substrate and the effects of prototypical inhibitors on the activity of each transporter. Efflux ratios were generated from mean A-B and B-A Papp values of duplicate monolayers. Efflux of the P-gp probe substrate digoxin was observed in both Caco-2 and MDR1-LLC-PK1 cells, and can be inhibited by the known P-gp inhibitors ketoconazole, quinidine, and verapamil. Efflux of the BCRP probe substrate estrone-3-sulfate (E3S) was observed in Caco-2 cells only, with an efflux ratio similar to that of digoxin. E3S efflux is significantly inhibited by the BCRP inhibitors novobiocin and fumitremorgin C (FTC). No efflux was observed for the MRP2 substrate LTC4 in either Caco-2 or MDR1-LLC-PK1 cells. LLC-PK1 control cells showed no efflux activity for any of the probe substrates.
Protein binding in human plasma compared with literature values
Comparison of % bound values obtained at BD Biosciences using rapid equilibrium dialysis in human plasma with literature data. Experimental values are means of replicates (N ≥ 4) with standard deviations in parentheses. Majority of literature values were collected from www.rxlist.com.To inquire about BD GentestSM Contract Research Services, locate your nearest BD Biosciences office.
