Cardoso Fatima, de Azambuja Evandro, Lago Lissandra Dal
Department of Medicine, Medical Oncology Clinic, Jules Bordet Institute, Rue Heger-Bordet, 1, 1000 Brussels, Belgium.
Eur J Cancer. 2008 Feb;44(3):341-52. doi: 10.1016/j.ejca.2007.11.019.
Taxanes have been broadly used in the treatment of breast cancer. However, the majority of initially responsive breast cancer patients eventually develop resistance to taxanes (acquired resistance) and a non-negligible percentage of patients are primarily resistant to these agents (de novo resistance). Additionally, taxanes require pre-medication and may cause important side effects such as febrile neutropenia and neuropathy. Hence, new agents with better efficacy and/or a better toxicity profile and/or are easier to administer need to be developed. Epothilones are a novel class of microtubule-targeting agents sharing a similar mechanism of action to the taxanes and having a more potent antiproliferative activity in various tumour cells lines, particularly in cases of taxane-resistant breast cancer. This review will focus on clinical development of epothilones in breast cancer, particularly ixabepilone which is in the late stages of development, their potential impact in clinical practice, advantages and limitations.
紫杉烷类药物已广泛应用于乳腺癌的治疗。然而，大多数最初对紫杉烷类药物有反应的乳腺癌患者最终会对其产生耐药性（获得性耐药），并且有不可忽视比例的患者对这些药物原发性耐药（原发性耐药）。此外，紫杉烷类药物需要进行预处理，并且可能会引起重要的副作用，如发热性中性粒细胞减少和神经病变。因此，需要研发疗效更好、毒性特征更佳和/或更易于给药的新型药物。埃坡霉素是一类新型的微管靶向药物，其作用机制与紫杉烷类药物相似，并且在各种肿瘤细胞系中具有更强的抗增殖活性，尤其是在对紫杉烷耐药的乳腺癌病例中。本综述将聚焦于埃坡霉素在乳腺癌中的临床开发，特别是处于开发后期的伊沙匹隆，它们在临床实践中的潜在影响、优势和局限性。
