Jenkins Julian M, Williams Daphne, Deng Yanli, Uhl Joanne, Kitchen Valerie, Collins David, Erickson-Miller Connie L
GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA.
Blood. 2007 Jun 1;109(11):4739-41. doi: 10.1182/blood-2006-11-057968. Epub 2007 Feb 27.
Eltrombopag (SB-497 115) is a first-in-class, oral, small-molecule, nonpeptide agonist of the thrombopoietin receptor (TpoR), being developed as a treatment for thrombocytopenia of various etiologies. In this phase 1 placebo-controlled clinical trial in 73 healthy male subjects, eltrombopag was administered as once-daily oral capsules for 10 days at doses of 5, 10, 25, 30, 50, and 75 mg. The pharmacokinetics of eltrombopag were dose dependent and linear, and eltrombopag increased platelet counts in a dose-dependent manner. There were no apparent differences in the incidence or severity of adverse events in subjects receiving active or placebo study medication. These observations indicate that eltrombopag is a once-daily, oral TpoR agonist with demonstrated thrombopoietic activity in human subjects, encouraging further studies in patients with thrombocytopenia.
艾曲泊帕（SB - 497115）是一种一流的口服小分子非肽类血小板生成素受体（TpoR）激动剂，正被开发用于治疗各种病因引起的血小板减少症。在这项针对73名健康男性受试者的1期安慰剂对照临床试验中，艾曲泊帕以每日一次口服胶囊的形式给药，剂量分别为5、10、25、30、50和75毫克，持续10天。艾曲泊帕的药代动力学呈剂量依赖性且为线性，并且艾曲泊帕以剂量依赖性方式增加血小板计数。接受活性或安慰剂研究药物的受试者中不良事件的发生率或严重程度没有明显差异。这些观察结果表明，艾曲泊帕是一种每日一次的口服TpoR激动剂，在人类受试者中已显示出促血小板生成活性，这鼓励了对血小板减少症患者进行进一步研究。
