PHASE I STUDY OF TAXOTERE IN PEDIATRIC PATIENTS WITH NEOPLASTIC DISEASE

简而言之，泰索帝是紫杉醇的一种新的半合成类似物， 由从针中提取的前体制备，而不是由 短叶红豆杉的树皮。 因此，泰索帝的供应量显著增加。 比母体化合物紫杉醇更稳定和可预测。在 体外实验表明，泰索帝与紫杉醇一样， 微管束的形成在存在下是稳定的 解聚剂如Ca和低温。 这导致 通过阻断细胞的G2或M期而产生的细胞毒性 周期 泰索帝已被证明比紫杉醇稍微更有效， 促进微管蛋白聚合。 此外，临床前研究 表明泰索帝在体内活性上级紫杉醇， 一些鼠肿瘤模型。

Briefly, taxotere is a novel semisynthetic analogue of taxol which is prepared from a precursor extracted from the needles, rather than the bark of Taxus brevifolia. Thus, the supply of taxotere is significantly more stable and predictable than that of the parent compound Taxol. In vitro experiments have shown that taxotere, like taxol, induces the formation of microtubule bundles that are stable in the presence of depolymerizing agents such as Ca and low temperature. This results in cytotoxicity by blocking cells at either the G2 or M phase of the cell cycle. Taxotere has been shown to be slightly more active than taxol in promoting tubulin polymerization. In addition, preclinical studies have demonstrated that taxotere has superior in vivo activity versus Taxol in some murine tumor models.