ANG1009(ANG1009) - 药物靶点：Top II_在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

多肽偶联药物（PDC）

别名

靶点

Top II

作用机制

Top II抑制剂(拓扑异构酶II抑制剂)

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构

Angiochem, Inc.

在研机构

Angiochem, Inc.

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

使用我们的ADC技术数据为新药研发加速。

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序列信息

Sequence Code 49342

关联

100 项与 ANG1009 相关的临床结果

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100 项与 ANG1009 相关的转化医学

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100 项与 ANG1009 相关的专利（医药）

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1

项与 ANG1009 相关的文献（医药）

2010-04-08·Journal of Medicinal Chemistry1区 · 医学

New Angiopep-Modified Doxorubicin (ANG1007) and Etoposide (ANG1009) Chemotherapeutics With Increased Brain Penetration

1区 · 医学

Article

作者: Che, Christian ; Demeule, Michel ; Thiot, Carine ; Currie, Jean-Christophe ; Lacoste, Marie-Claude ; Beliveau, Richard ; Regina, Anthony ; Yang, Gaoqiang ; Castaigne, Jean-Paul

This report describes the synthesis and preliminary biological characterization of 2 (ANG1007) and 3 (ANG1009), two new chemical entities under development for the treatment of primary and secondary brain cancers. 2 consists of three doxorubicin molecules conjugated to Angiopep-2, a 19-mer peptide that crosses the blood-brain barrier (BBB) by an LRP-1 receptor-mediated transcytosis mechanism. 3 has a similar structure, with the exception that three etoposide moieties are conjugated to Angiopep-2. Both agents killed cancer cell lines in vitro with similar IC(50) values and with apparently similar cytotoxic mechanisms as unconjugated doxorubicin and etoposide. 2 and 3 exhibited dramatically higher BBB influx rate constants than unconjugated doxorubicin and etoposide and pooled within brain parenchymal tissue. Passage through the BBB was similar in Mdr1a (-/-) and wild type mice. These results provide further evidence of the potential of this drug development platform in the isolation of novel therapeutics with increased brain penetration.

100 项与 ANG1009 相关的药物交易

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