BCD-115(BCD-115) - 药物靶点：CDK19 x CDK8_在研适应症：乳腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

JSC BIOCAD、JSC-BIOCAD

+ [1]

靶点

CDK19 x CDK8

作用机制

CDK19抑制剂(细胞周期蛋白依赖性激酶19抑制剂)、CDK8抑制剂(细胞周期蛋白依赖性激酶8抑制剂)

治疗领域

肿瘤皮肤和肌肉骨骼疾病

在研适应症

乳腺癌

非在研适应症-

原研机构

Biocad Medical, Inc.

在研机构

Biocad Medical, Inc.

非在研机构

Biocad CJSC

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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关联

1

项与 BCD-115 相关的临床试验

NCT03065010 / Completed临床1期

A Multicenter Open-label Non-comparative 2-Stage Phase 1a/1b Study to Assess the Safety and Pharmacokinetics of BCD-115 (JSC BIOCAD, Russia) in Combination With Endocrine Therapy in Women With ER(+) HER2(-) Local Advanced and Metastatic Breast Cancer

A Multicenter Open-label Non-comparative 2-Stage Phase 1a/1b Study to Assess the Safety and Pharmacokinetics of Oral BCD-115 (JSC BIOCAD, Russia) in Combination with Endocrine Therapy in Women with ER(+) HER2(-) Local Advanced and Metastatic Breast Cancer

开始日期2016-11-01

申办/合作机构

Biocad CJSC

100 项与 BCD-115 相关的临床结果

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100 项与 BCD-115 相关的转化医学

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100 项与 BCD-115 相关的专利（医药）

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1

项与 BCD-115 相关的文献（医药）

2021-11-11·ACS Medicinal Chemistry Letters3区 · 医学

Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19

3区 · 医学

Article

作者: Wang, Eric ; Gray, Nathanael S. ; Vatsan, Prasanna S. ; Jiang, Jie ; Hatcher, John M.

CDK8 and its paralog CDK19 are cyclin-dependent kinases that are core components of the so-called Mediator complex that has essential roles as a positive and negative regulator of gene expression. Several efforts to develop inhibitors have yielded natural and synthetic ATP-competitive compounds including cortistatin A, Sel120, BCD-115, CCT251921 (1), and MSC2530818 (2). Here, we used a hybridization approach starting from CCT251921 and MSC2530818 to derive new inhibitors with the aim of developing highly potent and selective inhibitors of CDK8/19. Initial compounds suffered from rapid aldehyde oxidase-mediated metabolism. This liability was overcome by utilizing a pyrazolopyridine hinge binder with a chlorine at the C-3 position. These efforts resulted in JH-XVI-178 (compound 15), a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.

100 项与 BCD-115 相关的药物交易

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