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[摘要]：Sagopilone is a fully synthetic epothilone. Epothilones are cytotoxic antimicrotubule drugs, six of which have been studied in clinical trials. Sagopilone has potential advantages over other antimicrotubule agents such as taxanes as it is water-soluble, evades multidrug resistance efflux pumps in vitro and may be able to cross the blood-brain barrier in humans. Sagopilone has been shown to be active in taxane-resistant models in vitro and in vivo. There are little published data on the clinical efficacy of sagopilone and the currently available preclinical and clinical data are reviewed here. Proof of concept was achieved in a phase II trial in platinum-resistant ovarian cancer; results from several ongoing phase II and future phase III studies are required to confirm whether the advantages of sagopilone seen in preclinical and early clinical studies will translate into a clear clinical benefit for patients. |
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