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埃博霉素类化合物是一种新型抗肿瘤药物,通过与肿瘤细胞中的微管蛋白结合,促进微管蛋白聚合并抑制微管的解聚,使细胞周期停止,最终诱导细胞凋亡。已经或正在开发的几种埃博霉素类似物有伊沙匹隆、埃博霉素B、沙戈匹隆、埃博霉素D、21-氨基埃博霉素B和KOS-1584,特别是沙戈匹隆极有可能成为高效候选抗肿瘤新药。本文对具有代表性的几个埃博霉素类化合物的临床药代动力学及其毒性反应研究进行综述并从结构特点和作用机制出发,重点论述伊沙匹隆和沙戈匹隆的研发和技术创新。
Epothilone is a new anti-tumor drug which can induce cell apoptosis by stopping the cell cycle by promoting the polymerization of tubulin and inhibiting the depolymerization of microtubules by binding to tubulin in tumor cells. Several epothilone analogues that have been or are being developed are ixabepilone, epothilone B, sagopilone, epothilone D, 21-aminoepothilone B and KOS-1584, in particular It is very likely that sagopilone will be a promising new antitumor drug candidate. In this paper, the clinical pharmacokinetics and toxicity studies of several representative epothilones were summarized and their structural features and mechanisms of action were reviewed. The development and technology of ixabepilone and sagopilone Innovation.