Université Paris-Sud, Faculté de Pharmacie, UMR CNRS 8612, Institut Galien Paris-Sud, 5, rue JB Clément, 92296 Châtenay-Malabry Cedex, France.
Drug Discov Today. 2013 Jan;18(1-2):93-8. doi: 10.1016/j.drudis.2012.08.006. Epub 2012 Aug 30.
Many anticancer drugs are sparingly water soluble and they show a low permeability at the intestinal level. Furthermore, their oral bioavailability is impaired because they are substrates of the cytochrome P450 and of the efflux pumps. The prodrug strategy, which is discussed in the present review, represents one of the different approaches to overcome these obstacles. In this review, we highlight the progresses of clinical development in the prodrug area for the oral administration of anticancer drugs.
许多抗癌药物的水溶性较差，在肠道水平的通透性也较低。此外，由于它们是细胞色素 P450 和外排泵的底物，因此其口服生物利用度受到损害。在本文综述中讨论的前药策略代表了克服这些障碍的不同方法之一。在本文中，我们强调了抗癌药物口服给药前药领域临床开发的进展。
