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Assessment of the role of protein transporters in drug toxicity studies.
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1  Department of Organic Chemistry, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń


According to the research of International Union of Primary and Clinical Pharmacology and the British Pharmacological Society, ion channels are the third-largest target group for drugs. They participate in controlling physiological and pathological processes in the body. Voltage Gated Ion Channels (VGICs) take part in generating and transmitting information within the cells of the central and peripheral nervous and cardiovascular systems.

Statistically, one of the most common reasons for drug withdrawal is the risk of cardiotoxicity, so drug safety guidelines are constantly being tightened. Many heart diseases result from disruption of the normal function of ion channels, so a thorough investigation of their role and function in the cardiovascular system is essential. In the recently proposed changes to the cardiovascular safety assessment paradigm by indicating the need to assess drug interactions with cardiac VGIC (such as: KV11.1, NaV1.5, and CaV1.2) and their impact on the electrophysiology of human ventricular cells.

This paper presents the latest guidelines on the safety of cardiac drugs. Three ion channels, KV11.1, NaV1.5, and CaV1.2, were assessed as potential targets for cardiac disrupting drugs. New advanced compound toxicity testing guidelines require specialized knowledge and tools, that quickly and reliably provide information about the test drug. Therefore, a methodology is presented for the use of in silico techniques, in the process of compound toxicity testing.

Keywords: safety pharmacology, ion channels
Comments on this paper
Iwona Kowalska
The use of computer methods in the assessment of toxicity in children
As a pediatrician, I would like to know if the methods described by you can be used in assessing the safety of use in children?
Magdalena Kowalska
Thank you for your interest in my research topic. Research conducted using ProTOX II and AdmetSAR software unfortunately does not take patient age into account. Therefore, when examining the safety of your chosen medication in children, you would need to perform additional testing. Nonetheless, the above-mentioned programs will be applicable in the preliminary assessment of drug toxicity, which may help to select further testing methods.