药物耐药性外排泵抑制剂的研究进展

Advance in efflux pump inhibitors for multidrug resistance

外排泵抑制剂可以抑制耐药细菌和肿瘤细胞对进入胞体内药物的外排作用,提高对药物的敏感性。它在改善药物的药动学特性等方面也有广泛的作用。研制开发外排泵抑制剂,逆转现有药物的耐药性将是改善药物疗效的一种有效的治疗方法。简要阐述近年来外排泵抑制剂的研究进展。

Active efflux,one of chief resistant mechanisms of tumour cells and bacteria,can result in the resistance of tumour cells and bacteria to therapeutic agents,which is known to be one of the main reasons for the failure in clinical therapy.Efflux pump inhibitors not only reverse the active efflux of tumour cells and bacteria and recovery their sensitivity to therapeutic agents,but also improve their pharmacokinetic attributes such as enhancing oral bioavailability.Therefore,the development of efflux pump inhibitors is a promising approach to overcome the resistance of tumour cells and bacteria to therapeutic agents.The recent efflux pump inhibitors are summarized in this brief review.