Unit of Pharmacoepidemiology and Pharmacoeconomics, Faculty of Pharmacy Jagiellonian University Medical College, Medyczna 9 Street, 30-688 Krakow, Poland.
BMC Pharmacol Toxicol. 2012 Aug 13;13:6. doi: 10.1186/2050-6511-13-6.
Drugs safety issues are now recognized as being factors generating the most reasons for drug withdrawals at various levels of development and at the post-approval stage. Among them cardiotoxicity remains the main reason, despite the substantial effort put into in vitro and in vivo testing, with the main focus put on hERG channel inhibition as the hypothesized surrogate of drug proarrhythmic potency. The large interest in the IKr current has resulted in the development of predictive tools and informative databases describing a drug's susceptibility to interactions with the hERG channel, although there are no similar, publicly available sets of data describing other ionic currents driven by the human cardiomyocyte ionic channels, which are recognized as an overlooked drug safety target.
The aim of this database development and publication was to provide a scientifically useful, easily usable and clearly verifiable set of information describing not only IKr (hERG), but also other human cardiomyocyte specific ionic channels inhibition data (IKs, INa, ICa).
The broad range of data (chemical space and in vitro settings) and the easy to use user interface makes tox-database.net a useful tool for interested scientists. DATABASE URL: http://tox-database.net.
药物安全性问题现在被认为是导致各阶段药物开发和批准后撤回的主要原因。其中,尽管在体外和体内测试方面投入了大量精力,主要关注 hERG 通道抑制作为药物致心律失常潜力的假设替代物,但仍然存在心脏毒性。人们对 IKr 电流非常感兴趣,导致了预测工具和信息数据库的发展,这些工具和数据库描述了药物与 hERG 通道相互作用的易感性,尽管没有类似的、公开可用的数据集描述由人类心肌细胞离子通道驱动的其他离子电流,这些电流被认为是一个被忽视的药物安全靶点。
本数据库开发和发布的目的是提供一套科学有用、易于使用且易于验证的信息集,不仅描述 IKr(hERG),还描述其他人类心肌细胞特定离子通道抑制数据(IKs、INa、ICa)。
广泛的数据(化学空间和体外环境)和易于使用的用户界面使 tox-database.net 成为感兴趣的科学家的有用工具。数据库网址:http://tox-database.net。