Cardiotoxicity is one of the major safety concerns in drug discovery, which is the leading reason for development termination and market withdraw or restriction. Particularly, hERG ion channel inhibition or blockade is responsible for 25-40% of all preclinical lead compound discontinuance. Human ether-a-go-go (hERG), a potassium channel that is abundant in the cardiomyocytes, represents one pivotal component for IKr currents and cardiac repolarization. Drug-induced interference of hERG causes QT interval prolongation, which is associated with fatal ventricular tachyarrhythmia called Torsade de Pointes (TdP). Given the unacceptable adverse effects of hERG inhibition and the fact that many drug-like molecules exhibit hERG affinity, hERG assessment has become one priority requirement by regulatory agencies before IND submission.
Equipped with extensive expertise and impeccable technologies, Medicilon offers multiple powerful approaches for rapidly and efficiently screening candidate compounds for hERG toxicity during early preclinical stage thus benefit the speed and safety of drug development progress.
A number of drugs have been withdrawn from late stage clinical trials due to these cardiotoxic effects, therefore it is important to identify inhibitors early in drug discovery.
hERG channel inhibition can have a significant negative impact on your drug’s value and probability of success. You will benefit from our combined expertise in ion channel electrophysiology and project toxicology that allows you to move molecules away from this liability while there are still choices in chemical design.
Medicilon offers you high-quality hERG data generated by our electrophysiology experts as part of your drug discovery screening cascade. Medicilon is uniquely positioned to work with your project team to interpret your data in the context of your drug discovery program.
Medicilon also offers a more comprehensive assessment of cardiac liability with assays for cardiac sodium and calcium channels.
You will gain a deeper understanding of the potential for effects on other cardiac ion currents to refine your decision-making and deliver an optimal (de-risked) clinical candidate.
Cost-effective, short research cycle, project start fast
The team of experts has rich experience in providing constructive solutions
As a one-stop pharmaceutical R & D outsourcing service company, Medicilon could screen out the higher cardiac safety factor candidate compounds through chemical, pharmacodynamics, pharmaceutical and preparation of a set of technical means if you provide information on cardio toxicity assessment.