首页> 外国专利> METHODS FOR PREPARING HIGH THROUGHPUT PEPTIDOMIMETICS, ORALLY BIOAVAILABLE DRUGS AND COMPOSITIONS CONTAINING SAME

METHODS FOR PREPARING HIGH THROUGHPUT PEPTIDOMIMETICS, ORALLY BIOAVAILABLE DRUGS AND COMPOSITIONS CONTAINING SAME

机译:制备高通透性肽假药,口服可生物利用的药物和包含相同成分的组合物的方法

摘要

Provided herein are methods to generate and screen peptides that exhibit drug like stabilities in vitro and in vivo. By selecting for enzyme resistance, Applicants are able to derive peptides that are not only stable to a broad spectrum of proteases, but also stable to other drug processing enzymes such as cytochrome P450s. This approach provides a general method to the rapid development of highly stable peptides for therapeutic development and diagnosis. The peptides are further modified for oral bioavailability. The methods can be applied to similar peptides for the making of therapeutic compositions.
机译:本文提供了产生和筛选在体外和体内表现出药物样稳定性的肽的方法。通过选择酶抗性,申请人能够获得不仅对多种蛋白酶稳定的肽,而且对其他药物加工酶例如细胞色素P450稳定的肽。该方法为快速开发用于治疗开发和诊断的高度稳定的肽提供了一种通用方法。进一步修饰这些肽以提高口服生物利用度。所述方法可以应用于用于制备治疗组合物的类似肽。

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