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The Discovery of a New Chemical Class of Antiepileptic Drugs

机译：发现新的抗癫痫药化学类别

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Epilepsy is a complex neurological disorder, characterized by recurrent spontaneous seizures that affect approximately 50 million of people worldwide. It is estimated that between 1-3% of the US population will develop some form of epilepsy before age 75. Today, up to 30 drugs are available on the market for the treatment of this still widely misunderstood affliction. The first generation of antiepileptic drugs (AEDs), introduced before the 1990, suffer from severe side effects and poor tolerability. Second generation AEDs, developed and marketed after 1990 and acting on new molecular targets have markedly broaden the therapeutic option and at the same time provided considerable benefits in term of pharmacokinetics, safety and tolerability. One of the most successful second generation AEDs, levetiracetam (LEV, trademark KeppraR) was discovered in UCB in the early 90's. Following the success of LEV, second generation molecules, with improved potency, were designed and developed to address unmet medical needs in the field of epilepsy. This article highlights the important contribution of medicinal chemistry to the discovery of this new class of AEDs and also the evolving role of the medicinal chemists in the pharmaceutical industry.
机译：癫痫病是一种复杂的神经系统疾病，其特征是反复发作的自发性癫痫发作，影响全球约5000万人。据估计，美国人口中有1-3％的人会在75岁之前患上某种形式的癫痫病。如今，市场上有多达30种药物可用于治疗这种仍然被人们误解的痛苦。在1990年之前推出的第一代抗癫痫药（AED）具有严重的副作用和较差的耐受性。第二代AEDs在1990年后开发和销售，并作用于新的分子靶标，显着拓宽了治疗选择范围，同时在药代动力学，安全性和耐受性方面提供了可观的益处。最成功的第二代AED之一左乙拉西坦（LEV，商标为KeppraR）是在90年代初在UCB中发现的。随着LEV的成功，设计和开发了具有更高效能的第二代分子，以满足癫痫领域未满足的医疗需求。本文重点介绍了药物化学对这一新型AED的发现的重要贡献，以及药物化学家在制药行业中不断发展的作用。

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