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Updated: Jun 27, 2025

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Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
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长效卡博特格拉维尔的药理动力学,有或没有口服的HIV PrEP的先导
Kelong Han1, Parul Patel2, Scott McCallister3
1GSK, Collegeville, Pennsylvania, USA.
Antimicrobial agents and chemotherapy
|May 6, 2024
概括
长期起作用的卡博特格拉维尔的药理动力学特征与口服领入剂或不带领的药理动力特征相似. 可选的口服引入可以跳过,因为卡博特格拉维尔暴露在短时间的注射间隔中仍然有效.
科学领域:
- 药理动力学 药理动力学
- 预防和治疗艾滋病病毒
背景情况:
- 长效卡博特格拉维尔已被批准用于HIV暴露前预防 (PrEP) 和治疗.
- 长效卡博特格拉维尔的启动包括一个可选的口服引入 (OLI) 阶段.
- 需要评估OLI对长期起作用的卡博特格拉维尔药理学的影响.
研究的目的:
- 评估OLI对长效卡博特格拉维尔药理动学的影响.
- 为了比较不同研究群体中含有和没有OLI的卡博特格拉维尔血度.
- 在各种OLI注射缺口场景下模拟药物动力学概况.
主要方法:
- 在HIV阳性和HIV阴性参与者中比较卡博特格拉维尔的血度,这些参与者开始注射有或没有OLI.
- 利用了第三阶段治疗研究FLAIR和关键PrEP研究HPTN 083和HPTN 084的数据.
- 在不同的OLI注射缺口场景下,在分配男性出生时和分配女性出生时的种群中模拟的药理动力学概况.
主要成果:
- 观察到的卡博特格拉维尔的最低度与OLI和没有OLI相似 (P > 0.3).
- 模拟的注射前最低度仍然高于药理动力学目标,有3天的OLI-注射间隔.
- 在所有场景中,PK概况在第一次注射后大约1-2周变得几乎相同.
结论:
- 观察到的长效卡博特格拉维尔暴露与OLI或没有OLI相似,支持可选的OLI使用.
- 预计卡博特格拉维尔暴露在OLI注射间隔≤3天的药理动力学目标以上.
- 结果在分配的男性出生和分配的女性出生人群中一致,支持灵活的OLI启动.
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