Princess Margaret Hospital, Bras Family Drug Development Program, Division of Medical Oncology, 610 University Avenue, Room 5-700, Toronto, ON M5G 2M9, Canada.
Future Oncol. 2011 Apr;7(4):559-68. doi: 10.2217/fon.11.26.
Epothilones are a new group of microtubule-stabilizing agents that have demonstrated antitumor activity in taxane-resistant models. Taxanes remain some of the most active cytotoxic agents in current cancer therapy. Primary or acquired resistance to taxanes in tumor cells partly prevents their long-term efficacy. Certain side effects, such as myelosupression or irreversible neuropathy, can also limit prolonged taxane administration. Epothilone B (EPO906; patupilone), a natural compound, and its semisynthetic derivative, ixabepilone (BMS-247550), differ in their pharmacokinetic and toxicity profiles. Ovarian cancer patients frequently relapse after first-line treatment based on platinum-taxane doublets. Therefore, epothilones might represent a therapeutic alternative in this setting. Patupilone and ixabepilone have undergone parallel clinical development, but their future role in ovarian cancer therapeutics remains ill defined.
埃坡霉素是一组新型的微管稳定剂，在紫杉烷类耐药模型中显示出抗肿瘤活性。紫杉烷类仍然是目前癌症治疗中最有效的细胞毒性药物之一。肿瘤细胞对紫杉烷类的原发性或获得性耐药在一定程度上阻碍了它们的长期疗效。某些副作用，如骨髓抑制或不可逆的神经病，也会限制紫杉烷类的长期给药。天然化合物埃坡霉素 B（EPO906；帕他泊隆）及其半合成衍生物伊沙匹隆（BMS-247550）在药代动力学和毒性特征上有所不同。卵巢癌患者在基于铂类-紫杉烷类二联方案的一线治疗后经常复发。因此，埃坡霉素类药物可能在这种情况下代表一种治疗选择。帕他泊隆和伊沙匹隆已进行平行的临床开发，但它们在卵巢癌治疗中的未来作用仍不明确。
Zotero 插件