a Department of Maternal and Child Health and Urological Sciences, "Sapienza" University of Rome , Policlinico Umberto I, Rome , Italy.
b Division of Gynecologic Oncology, Fondazione Policlinico Universitario A. Gemelli, IRCCS , Rome , Italy.
Expert Opin Investig Drugs. 2019 Aug;28(8):667-673. doi: 10.1080/13543784.2019.1648430. Epub 2019 Jul 30.
: A PEGylated form of irinotecan, a topoisomerase I inhibitor, is now available in commerce; its safety and efficacy have been tested in platinum resistant/refractory ovarian cancer (PROC) patients. This novel agent is known as Etirinotecan Pegol (EP). EP, like irinotecan, exerts its action through its principal metabolite SN-38. : This drug evaluation article focuses on the most recent investigations and clinical progress regarding EP, a long-acting polymer conjugate of irinotecan for the treatment of PROC. : EP provides prolonged and continuous exposure of SN-38 in tumors, when compared to its parent drug irinotecan. Results from phase II studies are comparable in terms of efficacy to other agents of proven use in PROC. A limitation of the use of EP is the schedule-dependent toxicities (mainly diarrhea and dehydration). In the future, EP could be investigated in association with other agents, even in attempts to restore sensitivity to other treatments. PROC remains a very difficult setting and EP might be a valid agent for patients with good performance status that have exhausted therapeutic options. In such a setting, participation in clinical trials is strongly encouraged.
一种聚乙二醇化的伊立替康(拓扑异构酶 I 抑制剂)目前已上市,其安全性和疗效已在铂类耐药/难治性卵巢癌(PROC)患者中得到验证。这种新型药物被称为依立替康聚乙二醇化(EP)。与伊立替康一样,EP 通过其主要代谢物 SN-38 发挥作用。本文重点介绍了 EP 的最新研究进展和临床进展,EP 是一种用于治疗 PROC 的伊立替康长效聚合物缀合物。与母体药物伊立替康相比,EP 可使 SN-38 在肿瘤中的持续暴露时间延长。II 期研究的结果在疗效方面与其他在 PROC 中已证实有效的药物相当。EP 的使用受限与其剂量依赖性毒性(主要是腹泻和脱水)有关。在未来,EP 可能与其他药物联合使用,甚至尝试恢复对其他治疗方法的敏感性。PROC 仍然是一个非常困难的治疗环境,EP 可能是治疗选择已经耗尽且体能状态良好的患者的有效药物。在这种情况下,强烈鼓励患者参与临床试验。