Your cart is empty.
Tecan uses cookies to improve our website. By continuing to browse our website, you accept our cookie policy.
Tecan uses cookies to improve our website. By continuing to browse our website, you accept our cookie policy.
Tecan has created a range of automated screening systems to support ADME (Absorption, Distribution, Metabolism and Excretion) screening in the early stages of drug discovery. These platforms are based on our flexible and scalable liquid handling platforms, for automated cell permeability, drug solubility, in vitro drug metabolism, protein binding studies and compound characterization procedures. Integration of Tecan multimode readers allows walkaway processing with full sample tracking.
***************************************************************************************
***************************************************************************************
Tab 01 / Permeability
***************************************************************************************
***************************************************************************************
The Freedom EVO® Cell Permeability platform has been designed to include all of the components necessary to perform compound permeability assays across either cell or artificial membrane barriers.
Solubility and permeability are two of the most critical physicochemical factors related to the oral bioavailability of a compound. The cell-free Parallel Artificial Membrane Permeability Assay (PAMPA) is an alternative to cell-based assays, offering a fast, cost-effective technology to screen for passive diffusion, a major absorption pathway.
Show moreIt’s time to make ADME screening efficient. Automate pION’s world-leading PAMPA technology on Tecan’s liquid handling platforms for a comprehensive high throughput solution. This high throughput walkaway system includes
PAMPA Evolution data analysis is an integral part of the pION-Tecan solution, providing clear visual data reporting for fast interpretation of results.
Comparison of a set of Double-Sink® PAMPA measurements on the new pION PAMPA Evolution PLUS System against values from pION‘s database. Assay conditions: pH 6.2 in donor, 30 minutes incubation and Gut-Box stirring at 40 μm setting.
Data courtesy of pION INC, Woburn, MA, USA
The CFO at pION said:
"The PAMPA software has been adapted to be able to take the raw data from the Infinite M200 and process it to generate the assay results."
Read more in "Cost-effective PAMPA with Infinite® M200"
Tecan’s liquid handling platforms have been configured for Caco-2 and Madin-Darby canine kidney (MDCK) cell-based assays to predict the in vivo intestinal permeability potential of a compound, including not only passive diffusion but also active transport, active efflux and paracellular permeablity.
Show moreRadiometric determination of permeability rates for Caco-2 and MDCK cell lines shows highly comparable results for manual handling and fully automated assay processing on Tecan’s liquid handling platform. Replicates of six wells per cell line were run for each drug.
Kellard L, Engelstein M. 2007. Journal of the Association for Laboratory Automation (JALA), 12:104–109.
***************************************************************************************
***************************************************************************************
Tab 02 / Solubility
***************************************************************************************
***************************************************************************************
Poor solubility can limit the absorption of a compound from the gastrointestinal (GI) tract resulting in reduced bioavailability. Running assays in a high throughput format allows for early, informed decision making and prevents development delays.
pION’s patented µSOL assays allow measurement of the onset of compound precipitation by monitoring absorbance changes. The assays mimic the compound solubility changes observed in the GI tract at different pH values. Automation on Tecan’s liquid handling platforms offers increased throughput while maintaining full assay flexibility.
Show moreµSOL Evolution™ data analysis software is an integral part of the pION-Tecan solution, rapidly determining whether a compound is relatively soluble (green) or insoluble (blue).
The µSOL Evolution software offers the ability to manipulate pH using a powerful pH mapping procedure. 96 different buffers can be prepared, from pH 1.5 to pH 10.0. This allows multiple measurements to be easily made and consistently reproduced.
***************************************************************************************
***************************************************************************************
Tab 03 / Metabolism
***************************************************************************************
***************************************************************************************
Tecan’s liquid handling Drug Metabolism platforms can routinely perform a variety of in vitro assays, including metabolic stability, cytochrome P450 (CYP450) inhibition, isoform identification, metabolite identification and CYP450 induction assays.
The Basel research center of Roche said:
"Roche has taken a different approach for drug metabolism work, creating a centralized automation facility that is agile enough to respond to the changing demands of R&D."
Read more in "A flexible lab for the future"
The pharmacological effects of a drug depend greatly on the duration and intensity of its action, which is strongly influenced by its rate of metabolism. One of the most important enzyme systems is CYP450, which catalyzes the oxidation of a multitude of drugs.
Show moreKeep microsomes or hepatocytes in suspension and at a required temperature for your metabolic stability assay. Tecan offers temperature-controlled shakers, racks and reagent carriers to handle pre- or post-incubation processing steps.
The Vanderbilt Center for Neuroscience drug discovery (VCNDD) said:
"Overall, our system is very flexible, very efficient and has tightened up our reproducibility and error rate, saving considerably on compounds, microsomes and FTE time, simply because we no longer need to repeat failed Tier 1 assays."
Read more in "The right tools to drive drug discovery"
***************************************************************************************
***************************************************************************************
Tab 04 / Protein binding
***************************************************************************************
***************************************************************************************
Add plasma protein binding data to your compound’s ADME profile to speed up time-to-clinic.
The Department Head for ADMETox at Johnson&Johnson said:
"From data produced in our laboratory over a six month period we estimate that, compared to a manual equilibrium dialysis assay, this semi-automated method can generate four times as much data with approximately half the resource costs."
Read more in "Automated equilibrium dialysis for plasma protein binding analysis"
A compound’s ability to bind to plasma proteins has a major effect on its pharmacodynamics properties, such as bioavailability or tissue distribution. Equilibrium dialysis is one of the most frequently used methods of determining drug binding. Discover automated Rapid Equilibrium Dialysis (RED, Thermo Fisher Scientific) and reduce assay preparation and equilibration times.
Show moreEliminate the plasma protein binding study bottleneck by automation of the 96-well, high throughput format RED system on a liquid handling platform, running from one to 48 assays without wasting an entire plate. RED plates are supplied in an easy-to-use disposable format, which is especially convenient when working with radioactive materials.
***************************************************************************************
***************************************************************************************
Tab 05 / Lead characterization
***************************************************************************************
***************************************************************************************
Tecan’s Compound Characterization platforms are designed to help researchers better understand the biophysical nature of their compounds. These systems include an integrated multimode microplate reader that can quickly scan a compound in solution and rapidly determine the amount present and relative purity.
Read more
The head of quality control at Tessa Therapeutics in Singapore said:
"Spark offers the best of both worlds, combining the sensitivity of filters with the flexibility of monochromators in one reader."
Read more in "Targeting the treatment of solid tumors"
Real-time, fully automated monitoring of biomolecular interactions in a high throughput. Tecan and Pall FortéBio have come together to automate Dip and Read™ biosensor assays based on the Octet® platform, integrating the system on the Freedom EVO platform.
Read more
***************************************************************************************
***************************************************************************************
Tab 06 / Literature
***************************************************************************************
***************************************************************************************
The permeability and solubility of a drug candidate are very important parameters that can affect the cost and success rate of development. Tecan has teamed up with pION Inc. to provide an automated solution for high throughput drug permeability screening assays.
The current trend in the industry is to incorporate ADME screening into the early stages of drug discovery to reduce high-cost, late-stage compound failures. To achieve this, there is a growing need for higher throughput assays and automation of ADME screens to process large numbers of compounds.
The metabolism of drugs is a key factor in compound toxicity, and the cytochrome P450 (CYP) superfamily of enzymes play a very important role in this process. This application note discusses the automation of cytochrome P450 compound profiling on the Fluent® liquid handling platform.
The Double-Sink™ PAMPA assay uses an optimized mixture of phospholipids infused into lipophilic microfilters, with a net negative lipid charge, that mimics the different membrane lipid compositions of the gastro-intestinal tract or blood-brain barrier. This application note describes the easy implementation of Tecan’s Infinite® 200 multimode reader for PAMPA sample analysis.
Automated laboratory workflows are commonplace in the pharmaceutical sector, offering increased throughput and process security throughout the drug discovery process. Most of these systems are dedicated to a specific task or assay, and have been optimized to streamline these repetitive tasks. Roche has taken a different approach for drug metabolism work, creating a centralized automation facility that is agile enough to respond to the changing demands of R&D.
TES Pharma is a specialist biotechnology company which performs molecular, cellular and ADME screening for drug discovery. The Company has recently purchased an HP D300 Digital Dispenser, and is now reaping the benefits of direct titration with improved assay reproducibility and more time to perform exploratory research.
A Freedom EVO® 200 dedicated to ADME screening has transformed the workflow of the Drug Metabolism Pharmacokinetic (DMPK) Group at the Vanderbilt Center for Neuroscience Drug Discovery (VCNDD), creating a high throughput contemporary ADME facility that is driving drug discovery forward.
Tecan and FortéBio have worked together to integrate the new FortéBio Octet® 384 platform on the Freedom EVO® workstation for automated real-time, label-free assays to support bioprocessing and drug discovery workflows. Tecan has collaborated with FortéBio to deliver a robust, off-the-shelf integration that allows the user to get the most out of the Octet 384, allowing increased walkaway time as well as optional liquid handling for assay plate set-up.
Following on from the successful launch of manual assay systems for permeability and solubility, Tecan and ION INC have co-developed an automated solution for drug permeability and solubility screening. This new solution is both scalable and upgradable according to the user’s changing requirements, from the entry level manual technique to a fully automated system for high throughput applications.
Tecan and pION Inc. have combined pION’s PAMPA Explorer™ with Tecan’s microplate readers for drug permeability screening using the Double-Sink parallel artificial membrane permeability assay (PAMPA).
The German army automates the determination of acetylcholinesterase activity in whole blood.
For research use only.