The cardiac action potential is the output of multiple ion channels. Cardiac ion channels are a target for cardiac channelopathies and are essential to any cardiac safety assessment in drug development.
Assessment of cardiac risk is traditionally performed close to the clinical stages of drug development. However, with the introduction of high throughput automated patch clamp systems like Qube 384, it is becoming increasingly common for companies to perform a cardiac safety screening early in the drug discovery cascade. This is also called ‘early-cardiac risk assessment’ and ensures that compounds with a cardiac risk are removed at an earlier stage.
Dysfunction of cardiac ion channels can lead to cardiac diseases (or channelopathies), such as arrhythmias (irregular heartbeats), heart failure, and cardiomyopathy. In addition, mutations of cardiac ion channels can cause inherited disorders, such as long QT syndrome and catecholaminergic polymorphic ventricular tachycardia.
Key cardiac Ion channels:
- KV11.1 (hERG)
- KV7.1 (KvLQT/MinK)