CovX/Pfizer Worldwide Research and Development, 9381 Judicial Drive, Suite 200, San Diego, CA 92121, USA.
Drug Discov Today. 2013 Sep;18(17-18):807-17. doi: 10.1016/j.drudis.2013.05.011. Epub 2013 May 28.
The notable expansion of peptide therapeutics development in the late 1990s and the 2000s led to an unprecedented number of marketing approvals in 2012 and has provided a robust pipeline that should deliver numerous approvals during the remainder of the 2010s. To document the current status of the pipeline, we collected data for peptide therapeutics in clinical studies and regulatory review, as well as those recently approved. In this Foundation review, we provide an overview of the pipeline, including therapeutic area and molecular targets, with a focus on glucagon-like peptide 1 receptor agonists. Areas for potential expansion, for example constrained peptides and peptide-drug conjugates, are profiled.
在 20 世纪 90 年代末和 21 世纪初,肽类治疗药物的开发取得了显著进展,这导致 2012 年获得了前所未有的批准数量,并提供了一个强大的研发管线,预计在 21 世纪 10 年代剩余时间内将有许多批准。为了记录研发管线的现状,我们收集了临床研究和监管审查中肽类治疗药物的数据,以及最近获得批准的药物的数据。在本次基金会综述中,我们概述了研发管线,包括治疗领域和分子靶点,并重点介绍了胰高血糖素样肽 1 受体激动剂。还介绍了潜在的扩展领域,例如约束肽和肽药物偶联物。