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ADME-TOX

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.

Overview

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.

Key benefits

  • High throughput ADME data for informed decision making
  • Combine full flexibility with smart automation
  • Scalable to fit your specific throughput needs

PAMPA cell-free permeability assay

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.

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pION and Tecan

It’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

  • A complete assay solution, including lipid membrane plastic ware, Gut-Box™ stirring device and software (pION)
  • Scalable solutions – PAMPA Explorer™ and PAMPA Evolution™ (pION)
  • Fully scalable liquid handling, with 8- or 96-channel pipetting to fit your throughput needs
  • Integrated multimode reader for automated data reporting

Highlights

  • Fully automated generation of transporter data
  • Access to the world leader in PAMPA technology, including the PAMPA Explorer Test System
  • Cost-effective, reproducible data
  • Increased throughput – run up to 600 assays per day

What can it be used for?

  • Evaluation of biorelevant lipid compositions
  • Permeability measurement over a large pH gradient (3-10)
  • Determination of sink conditions (binding to serum proteins)
  • Detection of lipid charges

Automated data reporting

PAMPA Evolution data analysis is an integral part of the pION-Tecan solution, providing clear visual data reporting for fast interpretation of results.

Comparable 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

Caco-2 MDCK cell-based permeability

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.

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Highlights

  • Generation of highly descriptive data
  • Automated cell seeding
  • Integration of temperature controlled plate, media and reagent carriers to increase process security

What can it be used for?

  • Passive diffusion
  • Active transport
  • Active efflux and influx
  • Paracellular permeability

Manual vs automated

Radiometric 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.

Overview

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.

Key benefits

  • Early solubility data to assess the effects of functional groups on the solubility of a compound family
  • Prevent delays to save costs

Compound solubility

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.

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Highlights

  • Assay flexibility – test multiple compounds at a single pH or multiple pH values for a single compound
  • Robust and fast data generation
  • Full workflow automation with the integration of a Tecan multimode reader

Data analysis made easy

µSOL 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).

pH-Mapping™

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.

Overview

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.

Key benefits

  • Comprehensive automation solution for high throughput metabolism testing
  • Integrated reader for ‘sample in-data out’ solution

Drug metabolism

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.

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Highlights

  • Automation of CYP450 assays provides a high throughput option key to drug discovery
  • Test more isoforms of the CYP450 family in less time
  • Combine automated liquid handling with detection devices for a complete ‘sample in-data out’ solution

Get information fast

  • Set up library screening or compound profiling experiments on the Fluent with ease
  • Fully automate P450-Glo™ (Promega) in a 384-well high density assay format
  • Run 12 plates unattended in just 6.5h to screen 614 compounds
  • Run 9 plates of multiplexing experiment in only 6h with a library screen of 143 compounds and dose response of 19 compounds on one plate

Keep control

Keep 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.

Overview

Add plasma protein binding data to your compound’s ADME profile to speed up time-to-clinic.

Key benefits

  • Reduce slow and laborious manual pipetting
  • Improved drug design
  • Free yourself from bottlenecks

Plasma protein binding

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.

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Increase your throughput

Eliminate 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.

Highlights

  • Determine free vs plasma protein bound drugs
  • Easy to use – disposable tubes require no pre-soaking, assembly or specialized equipment
  • Equilibrium reached in just four hours
  • Optimal membrane surface-to-volume ratio
  • Compartmentalized to eliminate cross-contamination or leakage

Detect your compound

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.

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High throughput and label-free

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.

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Brochures

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.

Application Notes

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.

Tecan Journal Articles

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 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.