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首页> 外文期刊>Current oncology reports. >Etirinotecan pegol: Development of a novel conjugated topoisomerase i inhibitor topical collection on evolving therapies
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Etirinotecan pegol: Development of a novel conjugated topoisomerase i inhibitor topical collection on evolving therapies

机译：Etirinotecan pegol：发展的新型共轭拓扑异构酶i抑制剂在局部治疗中的应用

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摘要

Irinotecan is a very active chemotherapeutic agent used for the treatment of several malignancies, including colorectal cancer, gastroesophageal tumors, lung cancer, breast cancer, ovarian cancer, and primary brain tumors. Irinotecan exerts its antineoplastic effects through its active metabolite 7-ethyl-10-hydroxycamptothecin. This metabolite is also responsible for the classic side effects associated with irinotecan that include diarrhea and neutropenia. A pegylated form of this agent, etirinotecan pegol, is undergoing clinical development with the main goal of increasing its therapeutic efficacy and its safety. This agent decreases the maximal exposure to 7-ethyl-10-hydroxycamptothecin while providing continuous exposure to the treated tumor. The half-life of etirinotecan pegol is 50 days and it has been studied in different schedules: weekly, every other week, and once every 3 weeks. The maximum tolerated dose of etirinotecan pegol was found to be 145 mg/m2. There have already been two phase II clinical trials published showing the efficacy of this novel agent in the treatment of metastatic ovarian and breast cancer. The side effect profile was acceptable for most patients, with a number of patients experiencing diarrhea and even neutropenia.
机译：伊立替康是一种非常活跃的化学治疗剂，用于治疗多种恶性肿瘤，包括结肠直肠癌，胃食管肿瘤，肺癌，乳腺癌，卵巢癌和原发性脑肿瘤。伊立替康通过其活性代谢物7-乙基-10-羟基喜树碱发挥其抗肿瘤作用。这种代谢产物还导致与伊立替康有关的经典副作用，包括腹泻和中性粒细胞减少。该试剂的聚乙二醇化形式，依替立替康聚乙二醇正在临床开发中，其主要目的是提高其治疗功效和安全性。该药物降低了对7-乙基-10-羟基喜树碱的最大暴露量，同时提供了对治疗肿瘤的连续暴露。依替立替康聚乙二醇的半衰期为50天，并且已按照不同的时间表进行了研究：每周一次，隔周一次以及每3周一次。依替立替康聚乙二醇的最大耐受剂量为145 mg / m2。已经有两项II期临床试验发表，表明该新型药物在治疗转移性卵巢癌和乳腺癌中的功效。对于大多数患者来说，副作用是可以接受的，许多患者出现腹泻甚至中性粒细胞减少症。

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