艾曲波帕的药理与临床评价

Pharmacology and clinical evaluation of eltrombopag

特发性血小板减少性紫癜是一种自身免疫性疾病,抗血小板抗体引起血小板破坏而导致严重的出血。常规的治疗是使用糖皮质激素、免疫抑制剂、抗人CD20单克隆抗体或脾切除,但引起复发或者许多不良反应。最近的研究显示:血小板生成素是能调节血小板产生的细胞因子,艾曲波帕为小分子口服非肽血小板生成素激动剂,能刺激血小板生成素受体,引起巨核细胞分化,血小板生成。本文介绍艾曲波帕的作用机制、药效学、药动学和临床评价。

Idiopathic thrombocytopenic purpura （｜TP） is an autoimmune disease, in which platelets were destructed due to the effects of antiplatelet antibodies, and severe blooding could be caused. Corticosteroids, immunosuppressants, anti-CD20 antibody and splenectomy have been used for the conventional therapy of ITP. But re- lapse and side effects occurred frequently. Eltrombopag is a nonpeptide small molecule for oral use, and have been proven to act on the receptors of thrombopoietin （a thrombopoiesis regulating cytokine） and could lead to megakaryocyte differentiation and platelet production. The mechanism, pharmacodynamics, pharmacokinetics and clinical therapeutics of eltrombopag were reviewed in this paper.