伦达莫西提尼布 (AZD4604) 的首次在人体内进行研究,伦达莫西提尼布是一种吸入性选择性JAK1抑制剂
Tina Jellesmark Jensen1, Camille Riff2, Julia Lund2
1Clinical Development, Respiratory and Immunology, BioPharmaceuticals R&D, AstraZeneca, Gothenburg, Sweden.
The Journal of allergy and clinical immunology
|January 14, 2026
概括
伦达莫西提尼布是一种选择性的Janus激酶 (JAK) 1抑制剂,在轻度喘患者中有效降低了部分排气的氧化 (FeNO). 吸入药物在第一阶段研究中显示出良好的安全性和耐受性.
科学领域:
- 药理学和治疗学 药理学和治疗学
- 呼吸系统医学 呼吸系统医学
- 免疫学 免疫学 免疫学
背景情况:
- 简氏激酶 (JAK) 1是治疗喘的潜在治疗标,特别是对吸入性皮质类固醇耐药的炎症.
- 隆达莫西提尼布 (AZD4604) 是一种用于治疗喘而开发的吸入性选择性JAK1抑制剂.
研究的目的:
- 为了评估吸入伦达莫西提尼布的安全性,耐受性,药理动力学和目标参与.
- 评估伦达莫西提尼布对轻度喘参与者的微分排气氧化 (FeNO) 的影响.
主要方法:
- 这是一项由健康志愿者和轻度喘患者参与的三部分随机,安慰剂控制的第一阶段研究.
- 单次和多次吸入剂量的伦达莫西提尼布 (0.025-6mg) 的管理.
- 评估FeNO水平在参与者FeNO和系统目标参与度升高.
主要成果:
- 伦达莫西提尼布在所有剂量中都能很好地耐受.
- 吸入后观察到快速吸收和剂量相称的全身暴露.
- 显著的FeNO减少 (约. 50%) 观察到1.4mg和3mg剂量,持续10天.
- 在3mg剂量时,观察到系统性标参与的最小,短暂的抑制.
结论:
- 每天两次服用隆达莫西提尼布,可以有效地降低FeNO在轻度喘患者的FeNO升高.
- 隆达莫西提尼布具有可接受的安全性和耐受性,表明其作为喘治疗的潜力.
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