Menarini Ricerche, Firenze, Italy.
Expert Opin Investig Drugs. 2009 Dec;18(12):1843-64. doi: 10.1517/13543780903379530.
Tachykinins (TKs) are small peptides widely distributed in the central and peripheral nervous systems where they act as neurotransmitters. Potent and selective TKs antagonists have been developed in the last 20 years and many efforts have been made to prove their efficacy in the treatment of various diseases. Herein the most prominent results in the clinical development are reported and discussed. For aprepitant, the only compound of this class to have been launched to date, results of clinical studies and postmarketing cost-effectiveness data for the treatment of chemotherapy-induced emesis are discussed. The field is still well active, as currently proof-of-concept studies for indications initially missed (i.e., depression) are ongoing and new targets are under investigation.
速激肽(TKs)是广泛分布于中枢和外周神经系统的小肽类物质,作为神经递质发挥作用。在过去的 20 年中,已经开发出了强效且选择性的 TKs 拮抗剂,并且已经做出了许多努力来证明它们在治疗各种疾病方面的功效。本文报告并讨论了临床开发中最突出的结果。对于 aprepitant,这是迄今为止唯一上市的此类化合物,讨论了其用于治疗化疗引起的呕吐的临床研究结果和上市后成本效益数据。该领域仍然非常活跃,因为目前正在进行针对最初错过的适应症(即抑郁症)的概念验证研究,并且正在研究新的靶点。