Wang Conan K, Craik David J
Institute for Molecular Bioscience, The University of Queensland, Brisbane, Queensland, 4072, Australia.
Biopolymers. 2016 Nov;106(6):901-909. doi: 10.1002/bip.22878.
Achieving high oral bioavailability for drugs is a key design objective in drug development. It is not surprising then that with the growing expectation of peptides as future drugs, there has also been an increasing interest in developing oral peptide therapeutics. Brought to the fore are questions such as what makes peptides orally bioavailable and how this can be achieved; questions which have inspired research into the area for decades. Early research in the area focused on linear peptides with more recent literature focusing on cyclic peptides, motivated in part by cyclic peptides like cyclosporine A that have demonstrated drug-like oral bioavailability. In this review, we take a look at research on the oral bioavailability of peptides, focusing on factors that affect passive permeability. © 2016 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 106: 901-909, 2016.
实现药物的高口服生物利用度是药物研发中的一个关键设计目标。因此，随着人们对肽类作为未来药物的期望不断增加，开发口服肽类疗法的兴趣也日益浓厚，这并不奇怪。诸如哪些因素使肽类具有口服生物利用度以及如何实现这一点等问题被提上了议程；这些问题已经激发了该领域数十年的研究。该领域的早期研究集中在线性肽上，而最近的文献则聚焦于环肽，部分原因是像环孢素A这样的环肽已显示出类似药物的口服生物利用度。在这篇综述中，我们将探讨肽类口服生物利用度的研究，重点关注影响被动通透性的因素。© 2016威利期刊公司。生物聚合物（肽科学）106: 901 - 909, 2016。
