 | Acquired long QT syndrome is a major cause of
drug withdrawals and failures during development.
Traditionally, in vitro cardiac liability screens are low
throughput, expensive and use primary animal cells
or tissues that are not necessarily predictive of the
human heart. Automated patch clamp platforms
have enabled early liability screening of individual
ion channels at medium throughput and acceptable
fidelity. To date cardiac safety screening has been
focused on the human ether-a-go-go related gene
(hERG). The primary use of early hERG assays is
to rank early stage compounds for progression
during medicinal chemistry lead optimization. Here
we show validation of our eight medium-throughput
electrophysiology cardiac profiler assays in a
consortium with major pharma companies and a
healthcare provider. These assays are offered in a
flexible format (from one to all eight) to easily
identify potential cardiac liabilities early so that the
lower-capacity tissue and organ studies can
subsequently be triggered when compounds
approach the costlier stages of development. |
