Yang Xiaoqin, Chen Jiamei, Wang Yitao, Wu Yihan, Zhang Jinming
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.
State Key Laboratory of Quality Research in Traditional Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau SAR 999078, China.
Pharmaceuticals (Basel). 2025 Mar 2;18(3):359. doi: 10.3390/ph18030359.
Irinotecan (CPT-11), an inhibitor of DNA topoisomerase I, stands as a pivotal therapeutic agent in oncology. However, its use is primarily constrained by side effects such as neutropenia and the onset of delayed diarrhea. Despite the effective management of neutropenia, CPT-11-induced diarrhea (CID) is often severe, leading to hospitalization, dosage adjustments, and in some cases, treatment discontinuation, which can significantly impact therapeutic outcomes. A multitude of pharmacological agents have been investigated in preclinical and clinical studies with the aim of reducing or preventing the onset of delayed diarrhea associated with CPT-11. This comprehensive review examines the underlying mechanisms of CPT-11-triggered delayed diarrhea and discusses the experimental medications and strategies that have been utilized to combat this adverse effect. This review encompasses an exploration of chemical formulations, the application of traditional Chinese medicine, and the advent of innovative drug delivery systems. It is anticipated that this article will serve as a valuable resource for both novice researchers in the realm of irinotecan chemotherapy and for those who are well-versed in the field, including experts and practicing clinicians.
伊立替康（CPT-11），一种DNA拓扑异构酶I抑制剂，是肿瘤学中的关键治疗药物。然而，其应用主要受到诸如中性粒细胞减少和迟发性腹泻发作等副作用的限制。尽管中性粒细胞减少得到了有效控制，但CPT-11诱导的腹泻（CID）往往很严重，导致住院、剂量调整，在某些情况下还会导致治疗中断，这会显著影响治疗效果。在临床前和临床研究中已经研究了多种药物，目的是减少或预防与CPT-11相关的迟发性腹泻的发作。这篇综述全面探讨了CPT-11引发迟发性腹泻的潜在机制，并讨论了用于对抗这种不良反应的实验药物和策略。该综述涵盖了化学制剂的探索、中药的应用以及创新药物递送系统的出现。预计本文将为伊立替康化疗领域的新手研究人员以及该领域的资深人士（包括专家和临床医生）提供有价值的参考。
