首个获批的迟发性运动障碍治疗药物valbenazine

Valbenazine, the first global approal for treatment of tardive dyskinesia

Valbenazine是一种选择性的囊泡单胺转运体2(vesicular monoamine transporter 2,VMAT2)抑制剂。2017年4月,FDA批准valbenazine用于成人迟发性运动障碍的治疗,是全球首个获批的针对此适应证的药物。Valbenazine由丁苯那嗪的代谢物酯化而成,较丁苯那嗪的半衰期长,无需频繁给药。其疗效明确,安全性和耐受性良好,应用前景广阔。本文对valbenazine的药理学特性、药动学、临床研究等进行综述。

Valbenazine is a selective inhibitor of vesicular monoamine transporter 2（VMAT2）. On April2017,oral capsule of valbenazine（IngrezzaTM） was approved in the USA for the treatment of adults with tardive dyskinesia（TD）,which become the first global approval for the disease. Valbenazine is the valine ester of the metabolites of tetrabenazine,and has a longer half-life than the latter,so it has no need for frequent administration.Valbenazine has shown its effective,safe and well tolerated characteristics,and has a wide application prospect on treatment of TD. In this article,we reviewed the pharmacologic characterization,pharmacokinetics,and clinical trials of valbenazine.