ADME-TOX

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.