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新开发的小循环是口服可生物利用的

Manuel L Merz¹, Sevan Habeshian¹, Bo Li¹

¹Institute of Chemical Sciences and Engineering, School of Basic Sciences, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland.

Nature chemical biology

|December 28, 2023

概括

研究人员开发了一种新方法来制造口服可用的循环. 这一突破使得开发具有高口服生物可用性的疗法成为可能,克服了药物输送中的一个主要障碍.

科学领域:

药用化学医学化学
药物发现药物发现药物发现
类治疗药物类治疗药物

背景情况:

循环为具有挑战性的疾病标提供高亲和力和特异性.
循环的口服被消化道吸收不佳和消化速度快速所限制.
这阻碍了它们作为口服可用的治疗药物的发展.

研究的目的:

开发一种用于口服可用的循环的新型组合合成和选方法.
为了克服基于的药物的口服输送的局限性.
产生具有增强稳定性和口服生物利用性的循环.

主要方法:

开发了一个组合合成和选工作流程.
采用了顺序循环和一个的基化.
同时选生物活性和胃肠道透性.
合成并选了8,448个循环的库对血栓.

主要成果:

鉴定出具有对血栓激素纳米分子亲和力的循环.
对于合成的循环类来说,实现了高稳定性.
在老鼠中,已证明可显著的口服生物利用率 (%F) 高达18%.
成功应用了图书馆综合和选的代循环.

结论:

开发的方法可以产生口服可用的循环.
这种方法克服了治疗开发中的关键障碍.
该方法是一般性的,有望释放的治疗潜力.

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