AZ-23(AZ-23) - 药物靶点：TrkA x TrkB_在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

TrkA x TrkB

作用机制

TrkA 拮抗剂(神经生长因子受体Trk-A 拮抗剂)、TrkB抑制剂(神经营养性酪氨酸激酶受体-2型抑制剂)

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构

AstraZeneca R&D Boston, Inc.

在研机构

AstraZeneca R&D Boston, 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

分子式C17H19ClFN7O

InChIKeyLBVKEEFIPBQIMD-JTQLQIEISA-N

CAS号915720-21-7

关联

100 项与 AZ-23 相关的临床结果

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100 项与 AZ-23 相关的转化医学

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100 项与 AZ-23 相关的专利（医药）

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1

项与 AZ-23 相关的文献（医药）

2009-07-01·Molecular Cancer Therapeutics2区 · 医学

Identification and preclinical characterization of AZ-23, a novel, selective, and orally bioavailable inhibitor of the Trk kinase pathway

2区 · 医学

Article

作者: Dave Whitston ; Charles Omer ; Kenneth Thress ; Zhong Ying Liu ; Terry MacIntyre ; Patrick A. Zweidler-McKay ; Peter E. Zage ; Tao Wang ; Ethan Hoffmann ; Kevin Webster ; Haiyun Wang ; Jeffrey L. Brown ; Lizhi Zeng

AbstractTropomyosin-related kinases (TrkA, TrkB, and TrkC) are receptor tyrosine kinases that, along with their ligands, the neurotrophins, are involved in neuronal cell growth, development, and survival. The Trk-neurotrophin pathway may also play a role in tumorigenesis through oncogenic fusions, mutations, and autocrine signaling, prompting the development of novel Trk inhibitors as agents for cancer therapy. This report describes the identification of AZ-23, a novel, potent, and selective Trk kinase inhibitor. In vitro studies with AZ-23 showed improved selectivity over previous compounds and inhibition of Trk kinase activity in cells at low nanomolar concentrations. AZ-23 showed in vivo TrkA kinase inhibition and efficacy in mice following oral administration in a TrkA-driven allograft model and significant tumor growth inhibition in a Trk-expressing xenograft model of neuroblastoma. AZ-23 represents a potent and selective Trk kinase inhibitor from a novel series with the potential for use as a treatment for cancer. [Mol Cancer Ther 2009;8(7):1818–27]

100 项与 AZ-23 相关的药物交易

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