Division of Tumor Biology and Immunology, The Netherlands Cancer Institute, Amsterdam, The Netherlands.
Department of Head and Neck Oncology and Surgery, The Netherlands Cancer Institute, Amsterdam, The Netherlands.
Mol Cancer. 2024 Jun 4;23(1):120. doi: 10.1186/s12943-024-02034-7.
The efficacy of anthracycline-based chemotherapeutics, which include doxorubicin and its structural relatives daunorubicin and idarubicin, remains almost unmatched in oncology, despite a side effect profile including cumulative dose-dependent cardiotoxicity, therapy-related malignancies and infertility. Detoxifying anthracyclines while preserving their anti-neoplastic effects is arguably a major unmet need in modern oncology, as cardiovascular complications that limit anti-cancer treatment are a leading cause of morbidity and mortality among the 17 million cancer survivors in the U.S. In this study, we examined different clinically relevant anthracycline drugs for a series of features including mode of action (chromatin and DNA damage), bio-distribution, anti-tumor efficacy and cardiotoxicity in pre-clinical models and patients. The different anthracycline drugs have surprisingly individual efficacy and toxicity profiles. In particular, aclarubicin stands out in pre-clinical models and clinical studies, as it potently kills cancer cells, lacks cardiotoxicity, and can be safely administered even after the maximum cumulative dose of either doxorubicin or idarubicin has been reached. Retrospective analysis of aclarubicin used as second-line treatment for relapsed/refractory AML patients showed survival effects similar to its use in first line, leading to a notable 23% increase in 5-year overall survival compared to other intensive chemotherapies. Considering individual anthracyclines as distinct entities unveils new treatment options, such as the identification of aclarubicin, which significantly improves the survival outcomes of AML patients while mitigating the treatment-limiting side-effects. Building upon these findings, an international multicenter Phase III prospective study is prepared, to integrate aclarubicin into the treatment of relapsed/refractory AML patients.
蒽环类化疗药物的疗效在肿瘤学领域几乎无与伦比,包括多柔比星及其结构类似物柔红霉素和伊达比星。尽管其副作用包括累积剂量依赖性心脏毒性、治疗相关恶性肿瘤和不孕,但仍具有良好的疗效。在现代肿瘤学中,解毒蒽环类药物而不影响其抗肿瘤作用是一个主要的未满足的需求,因为限制抗癌治疗的心血管并发症是美国 1700 万癌症幸存者发病率和死亡率的主要原因。在这项研究中,我们研究了不同的临床相关蒽环类药物,包括作用模式(染色质和 DNA 损伤)、生物分布、抗肿瘤疗效和在临床前模型和患者中的心脏毒性。不同的蒽环类药物具有惊人的单独疗效和毒性特征。特别是阿克拉霉素在临床前模型和临床研究中表现出色,因为它能有效地杀死癌细胞,没有心脏毒性,甚至在多柔比星或伊达比星的最大累积剂量后也能安全给药。对阿克拉霉素作为复发/难治性 AML 患者二线治疗的回顾性分析显示,其生存效果与一线治疗相似,与其他强化化疗相比,5 年总生存率显著提高了 23%。将单个蒽环类药物视为不同的实体,可以揭示新的治疗选择,例如阿克拉霉素的鉴定,这可以显著改善 AML 患者的生存结果,同时减轻治疗限制的副作用。基于这些发现,一项国际多中心 III 期前瞻性研究正在准备中,将阿克拉霉素纳入复发/难治性 AML 患者的治疗中。