Vicagrel的药代学和药效学评价的耐受性,小说P2Y12拮抗剂,在中国健康志愿者。

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李X,刘C,朱X,魏H, H, H陈,陈G,杨D,太阳H,沈Z,张Y,李W,杨J,刘Y,赖X, Y锣,刘X, Y,钟D,妞妞J,刘B,丁Y

Vicagrel的药代学和药效学评价的耐受性,小说P2Y12拮抗剂,在中国健康志愿者。

杂志。2018年6月20日,9:643。doi: 10.3389 / fphar.2018.00643。eCollection 2018。

PubMed ID

29973877 (在PubMed

]

文摘

背景:Vicagrel是一种新型抗血小板药物通过酯酶和水解氯吡格雷一样的中间,而不是CYP2C19。这里,我们报告了第一个临床试验耐受性,不同剂量的药代学和药效学vicagrel,与氯吡格雷在中国健康志愿者。方法:本研究是在两个部分进行。研究我是dose-escalating(5 - 15毫克)的研究。对于每一个剂量,15名参与者被随机分成三组(n = 45总);九个参与者vicagrel,三个有氯吡格雷,三是服用安慰剂。研究二世进行了评估vicagrel和阿司匹林在15个健康的参与者之间的交互。vicagrel血浆代谢物的浓度和氯吡格雷使用质/ MS法测定。血小板聚集是使用VerifyNow-P2Y12试验评估。结果:Vicagrel(5 - 15毫克每天)10天或添加剂量阿司匹林在健康志愿者耐受性良好。 The exposure of the active metabolite increased proportionally across the dose range and was higher (~10-fold) than clopidogrel. The levels of IPA dosing 75 mg clopidogrel were between the responses of 5 mg and 10 mg vicagrel. After a single loading dose of vicagrel (30 mg) and a once-daily maintenance dose (7.5 mg) for 8 days, the maximum inhibition of platelet aggregation was similar to that seen with the combined use of vicagrel and aspirin (100 mg/day). Conclusion: Oral vicagrel demonstrated a favorable safety profile and excellent anti-platelet activity, which could be a promising P2Y12 antagonist as anti-platelet drug and can be further developed in phase II/III studies, and marketing for the unmet medical needs of cardiovascular diseases. The study was registered at http://www.chictr.org.cn (ChiCTR-IIR-16009260).

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药物靶点

药物	目标	类	生物	药理作用	行动
Vicagrel	P2Y purinoceptor 12	蛋白质	人类	未知的	拮抗剂 抑制剂	细节