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Updated: Jul 4, 2025

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在高胆固醇血症中用口服的NNC0385-0434抑制PCSK9:一个随机,双盲,安慰剂控制和活性控制的2期试验

Michael J Koren¹, Olivier Descamps², Yoshiki Hata³

¹Jacksonville Center for Clinical Research, Jacksonville, FL, USA.

The lancet. Diabetes & endocrinology

|February 4, 2024

概括

一种口服的プロ蛋白转化酶亚素/素9型 (PCSK9) 抑制剂,NNC0385-0434,显示显著的LDL胆固醇降低,与注射疗法相比. 尽管有效,但由于投资组合决策,开发已停止.

科学领域:

心血管医学心血管医学
药理学药理学是指药理学的学科.
脂质代谢脂质代谢是什么

背景情况:

可注射的蛋白转化酶亚素/素9型 (PCSK9) 抑制剂有效降低LDL胆固醇,改善心血管结果.
这一第二阶段研究评估了NNC0385-0434 ,一种口服的PCSK9抑制剂,在接受口服降脂治疗的患者中进行了评估.

研究的目的:

评估NNC0385-0434的疗效和安全性,一个口服PCSK9抑制剂,在口服降脂治疗的个体中.
为了比较NNC0385-0434与安慰剂和开放标签evolocumab的LDL降胆固醇效果.

主要方法:

一个随机,双盲,安慰剂控制和活性控制的试验,涉及七个国家的267名参与者.
参与者接受了NNC0385-0434 (每天15毫克,40毫克或100毫克),安慰剂或皮下注射的evolocumab (140毫克每两周).
主要终点是LDL胆固醇从基线到第12周的百分比变化,通过β定量测量.

主要成果:

与安慰剂相比,NNC0385-0434显示了剂量依赖的LDL胆固醇降低:32.0% (15毫克),44.9% (40毫克) 和61.8% (100毫克) 在第12周,与安慰剂相比 (所有p<0.0001).
100毫克剂量的NNC0385-0434显示出与evolocumab可比的疗效,平均LDL胆固醇降低了56.2%和59.6%.
胃肠道疾病是最常见的与治疗相关的不良事件;没有报告死亡或与治疗相关的严重不良事件.

结论:

NNC0385-0434表现出显著的12周LDL胆固醇降低功效和良好的患者耐受性,与注射PCSK9抑制剂相比.
尽管有积极的临床发现,但由于投资组合考虑,赞助商暂停了NNC0385-0434的进一步开发.

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