用VX-548对急性疼痛进行NaV1.8的选择性抑制
Jim Jones1, Darin J Correll1, Sandra M Lechner1
1From Vertex Pharmaceuticals (J.J., D.J.C., S.M.L., I.J., X.M., D.S., C.S., J.D.O., B.H., C.B., P.N.) and Brigham and Women's Hospital (S.G.W.) - both in Boston; Lotus Clinical Research, Pasadena (A. Beaton), Cedars-Sinai Medical Center, Los Angeles (P.F.W.), and White Mountain Institute, Sea Ranch (P.F.W.) - all in California; JBR Clinical Research, Salt Lake City (T.B.); Rush University Medical Center, Chicago (A. Buvanendran); Duke University School of Medicine, Durham, NC (A.S.H.); the University of Pittsburgh Medical Center, Pittsburgh (L.J.P.); and Endeavor Clinical Trials, San Antonio, TX (R.A.P.).
高剂量的VX-548有效地减少了手术后的急性疼痛,超过了安慰剂. 较低剂量的VX-548没有显著缓解疼痛,报告的副作用轻微,如头痛和便秘.
科学领域:
- 疼痛管理 疼痛管理
- 临床药理学 临床药理学
- 神经科学是一个神经科学.
背景情况:
- 在外围神经元中,NaV1.8通道对于传输疼痛信号至关重要.
- VX-548是一种口服选择性抑制剂,向NaV1.8.
研究的目的:
- 评估VX-548在手术后治疗急性疼痛的疗效和安全性.
- 为了比较VX-548的不同剂量与安慰剂和可二甲酸乙胺.
主要方法:
- 进行了两项2期随机试验 (腹腔整形和骨切除术).
- 参与者在48小时内接受了不同剂量的VX-548,可二甲酸乙胺或安慰剂.
- 主要终点是疼痛强度差异的时间加权总和 (SPID48).
主要成果:
- 与安慰剂相比,高剂量的VX-548在腹部整形和骨髓切除试验中显著降低了急性疼痛.
- 较低剂量的VX-548与安慰剂相比没有显著减轻疼痛.
- 常见的不良事件包括头痛和便秘,严重程度一般为轻度至中度.
结论:
- 高剂量的VX-548在控制急性术后疼痛方面表现出有效性.
- 止痛效果似乎取决于剂量,较低剂量效果较差.
- VX-548为急性疼痛管理提供了一个潜在的新选择,具有可管理的安全性.
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