Current State of the Art of New Tubulin Inhibitors in the Clinicd
Current State of the Art of New Tubulin Inhibitors in the Clinicd
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DOI：
10.2174/157488406775268200
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发表时间：
2006-01-01
影响因子：
3.2
通讯作者：
Kuppens, Isa E. L. M.
中科院分区：
文献类型：
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作者：
Kuppens, Isa E. L. M.
近年来，微管稳定剂多西他赛和紫杉醇是临床上最成功的化疗药物。多年来，已经进行了几次尝试来平等和更好地使用这些药物。这两种紫杉烷都与臭名昭著的副作用神经毒性有关，并且通常伴随着增加的耐药性和与其他化疗剂的交叉耐药性。此外，它们的高亲脂性要求使用共溶剂，这与不太有利的副作用如超敏反应有关。为了避免这些缺点并改善紫杉烷类的临床应用，一些新的药物已进入临床试验。所讨论的药剂是盘皮内酯类的药物类别; XAA 296 A和埃博霉素类; BMS-247550、BMS-310705、epo 906、科斯-862和药剂ABT-751和D-24851。在这里，我们提出了一个最近进行的临床研究，以确定微管蛋白抑制剂，旨在扩大和改善紫杉烷类多西他赛和紫杉醇的临床使用的最新技术水平的概述。
For years the microtubule stabilizing agents docetaxel and paclitaxel belong to the most successful clinical chemotherapeutic agents. Several attempts have been made over the years to equal and better these drugs. Both taxanes are associated with the notorious side effect neurotoxicity and are often accompanied with increased drug resistance and cross resistance with other chemotherapeutic agents. In addition their high lipophilicity demands use of co-solvents, which are associated with less favorable side effects such as hypersensitivity. To prevent these disadvantages and improve the clinical application of the taxanes several new agents have entered clinical testing. The agents that are discussed are the drug class of the discodermolides; XAA296A and the epothilones; BMS-247550, BMS-310705, epo906, kos-862 and the agents ABT-751 and D-24851. Here we present an overview of recently performed clinical studies to determine the current state of the art of the tubulin inhibitors which are intended to enlarge and improve the clinical use of the taxanes docetaxel and paclitaxel.