Department of Drug Delivery Technology and Science, Laboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University, 5-6-1 Mitahora-Higashi, Gifu 502-8585, Japan and ThioMatrix GmbH, Research Center Innsbruck, Mitterweg 24, 6020 Innsbruck, Austria.
Expert Rev Clin Pharmacol. 2008 May;1(3):429-40. doi: 10.1586/17512433.1.3.429.
The development of novel efflux pump inhibitors is an emerging and challenging research field. Besides the use of such excipients in cancer therapy, efflux pump inhibitors are gaining increasing interest with regards to drug delivery. In particular, inhibition of efflux pumps located in the intestine and the blood-brain barrier offers promising prospects. Nowadays, third-generation inhibitors, such as elacridar, zosuquidar, laniquidar, OC144-093 and tariquidar, have been evaluated in clinical trials. Apart from these small, molecular inhibitors, which will be discussed within the current review, a focus has been set on polymeric or polymer-based inhibitors, including poly(ethylene glycol) and derivatives, poloxamers and thiomers.
新型外排泵抑制剂的开发是一个新兴且具有挑战性的研究领域。除了在癌症治疗中使用这些赋形剂外，外排泵抑制剂在药物输送方面也越来越受到关注。特别是，抑制位于肠道和血脑屏障中的外排泵具有广阔的前景。如今，第三代抑制剂，如依利达雷、唑舒达、拉尼奎达、OC144-093 和塔瑞奎达，已在临床试验中进行了评估。除了这些小分子抑制剂（将在本综述中讨论）外，还重点关注了聚合物或基于聚合物的抑制剂，包括聚乙二醇及其衍生物、泊洛沙姆和硫醚。
