配方开发和PF614-MPAR的第一阶段临床研究,这是一种带有口服阿片类药物过量保护的氧化前药物
D Lynn Kirkpatrick1, Linda A Pestano1, Cari Evans1
1Ensysce Biosciences, Inc., La Jolla, California.
Journal of opioid management
|March 3, 2026
概括
这项研究开发了PF614-MPAR,一种内置过量保护的阿片类药物. 这种新型配方在高剂量下抑制了氧化的释放,为疼痛管理提供了更安全的替代方案.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物开发 药物开发
- 疼痛管理 疼痛管理
背景情况:
- 预防阿片类药物过量服用是一个至关重要的未满足的需求.
- PF614-多药药滥用抵抗 (MPAR®) 使用素激活的前药剂方法来控制氧化释放.
- PF614-MPAR将PF614 (氧化原药) 与纳法莫斯塔特 (素抑制剂) 结合使用,以减轻过量风险.
研究的目的:
- 为了确定最佳的PF614-nafamostat配方,以提供有效的过量保护.
- 评估PF614-MPAR的滥用威和过量保护性质.
主要方法:
- 在健康受试者中进行的第一阶段研究,评估PF614与各种纳法莫斯塔特配方.
- 测量了血氧的度,以评估PF614的激活和纳法莫斯塔的疗效.
- 通过向被阻断的纳尔特雷克森受试者给予最佳PF614-MPAR配方的升级剂量来评估过量保护.
主要成果:
- 最佳的PF614-MPAR 25毫克配方在单剂和双剂中提供了治疗性氧化水平.
- 同时使用3x,5x或8x剂量PF614-MPAR抑制氧化释放的药物.
- 在超治疗剂量时,纳法莫斯塔特有效地减少了氧的释放.
结论:
- PF614-MPAR显示出作为第一个具有滥用耐药性和口服过量保护的阿片类药物的潜力.
- 这种新的配方解决了阿片类药物安全方面的至关重要的未满足需求.
- 进一步开发PF614-MPAR可以显著提高患者在疼痛管理中的安全性.
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