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在局部应用Everolimus减轻透镜诱导的近视通过mTORC1抑制

Ruiheng Zhang^1,2,3, Chuyao Yu^1,2,3, Yitong Li^1,2,3

¹Beijing Tongren Eye Center, Beijing Key Laboratory of Intraocular Tumor Diagnosis and Treatment, Beijing Tongren Hospital, Capital Medical University, Beijing, China.

Investigative ophthalmology & visual science

|September 24, 2025

概括

一种新的局部眼滴配方有效地将埃弗罗利马斯输送到眼睛的后部,在动物模型中显著降低了近视的进展. 这为控制近视提供了一个有前途的新疗法.

科学领域:

眼科医生眼科眼科
药理学药理学是指药理学的学科.
细胞生物学细胞生物学

背景情况:

近视,或近视,是一个日益增长的全球健康问题.
拉巴胺素复合体1 (mTORC1) 信号传递的机械标在透镜诱导近视 (LIM) 中起作用.
将像mTORC1抑制剂这样的脂友性药物输送到眼睛后部段是一个重大挑战.

研究的目的:

开发一种新型的局部眼科配方Everolimus,一个mTORC1抑制剂.
为了评估这种配方在控制近视进展方面的有效性.
评估Everolimus眼滴的眼部药理动力学和安全性.

主要方法:

优化载体配方,以向RPE-choroid复合体输送Everolimus.
在诱导近视的几内亚猪中测试了不同度的Everolimus眼滴.
分析了mTORC1信号,轴延长,折射变化, fundus 形态,药理动力学和眼睛安全性.

主要成果:

埃弗罗利莫斯眼滴 (0.001%-0.1%) 显著减弱了轴延长,以剂量依赖的方式.
该配方减少了 fundus tessellation,胆管稀释和mTORC1的激活. 这种配方减少了 fundus tessellation,胆管稀释和mTORC1的激活.
在RPE-choroid复合体中达到治疗度,没有观察到眼睛毒性或对眼内压力的不良影响.

结论:

这种新的眼科配方成功地将Everolimus输送到眼睛后部.
在临床前的模型中,Everolimus眼滴显示出显著的抗视疗效.
这种配方具有有效控制近视的临床潜力.

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