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IDN 5390:紫杉烷类药物研发的新概念。

IDN 5390: a new concept in taxane development.

作者信息

Taraboletti Giulia, Micheletti Gianluca, Giavazzi Raffaella, Riva Antonella

机构信息

Department of Oncology, Mario Negri Institute for Pharmacological Research, Bergamo, Italy.

出版信息

Anticancer Drugs. 2003 Apr;14(4):255-8. doi: 10.1097/00001813-200304000-00001.

Abstract

IDN 5390 is a seco-derivative cytostatic taxane. Originally selected for its ability to affect endothelial cell motility, the anti-angiogenic properties of IDN 5390 have been documented in experimental models, in vivo and in vitro. Preclinical studies indicate that, in vivo, oral IDN 5390 has a favorable bioavailability, is well tolerated and shows a significant anti-neoplastic activity on a panel of different tumor models, including paclitaxel-resistant tumors. According to its cytostatic rather than cytotoxic nature, frequent administrations of non-toxic doses have proven to be the optimal schedule for IDN 5390 treatment. Preliminary findings suggest the use of this compound in combination with conventional anti-neoplastic therapy. IDN 5390 can be considered the prototype of a new class of well-tolerated, orally available anti-angiogenic taxane derivatives with cytostatic properties.

摘要

IDN 5390是一种裂环二萜类细胞生长抑制剂紫杉烷。最初因其影响内皮细胞运动的能力而被筛选出来,IDN 5390的抗血管生成特性已在体内和体外实验模型中得到证实。临床前研究表明,在体内,口服IDN 5390具有良好的生物利用度,耐受性良好,并且在一系列不同的肿瘤模型中,包括对紫杉醇耐药的肿瘤,都显示出显著的抗肿瘤活性。根据其细胞生长抑制而非细胞毒性的性质,多次给予无毒剂量已被证明是IDN 5390治疗的最佳方案。初步研究结果表明该化合物可与传统抗肿瘤疗法联合使用。IDN 5390可被视为一类新型耐受性良好、口服可用的具有细胞生长抑制特性的抗血管生成紫杉烷衍生物的原型。

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