Johnson & Johnson Pharmaceutical Research & Development, Spring House, Pennsylvania 19477-0776, USA.
Curr Top Med Chem. 2009;9(11):1049-62. doi: 10.2174/156802609789630938.
TOPAMAX((R)) (topiramate) 1, is a broad-spectrum anticonvulsant that has been marketed worldwide for the treatment of epilepsy and migraine. We discovered this blockbuster drug serendipitously in a project that originally sought a new antidiabetic agent. Topiramate has useful neurological effects that derive from multiple CNS mechanisms of action, but it is basically a "neurostabilizer" by virtue of attenuating the excitability of brain neuronal pathways. During its extensive clinical use, topiramate was also found to possess antimetabolic dysfunction activity, which could be applicable in the treatment of diabetes and obesity. This article discusses research results and events surrounding the discovery and development of topiramate.
妥泰((R))(托吡酯)1，是一种广谱抗惊厥药物，已在全球范围内上市，用于治疗癫痫和偏头痛。我们最初的项目旨在寻找一种新的抗糖尿病药物，却偶然发现了这款重磅炸弹药物。托吡酯具有多种中枢神经系统作用机制，对神经系统具有有益的作用，但它基本上是一种“神经稳定剂”，通过减弱脑神经元通路的兴奋性来发挥作用。在广泛的临床应用中，还发现托吡酯具有抗代谢功能障碍活性，可适用于糖尿病和肥胖症的治疗。本文讨论了发现和开发托吡酯的研究结果和相关事件。
