Delving into the Latest Updates on Revere Pharmaceuticals, Inc. with Synapse

概览

疾病领域	数量

肿瘤	3

排名前五的药物类型	数量

小分子化药	3

排名前五的靶点	数量

RAC1(Rac1蛋白)	2
RhoA Y42C(RhoA Y42C突变)	1

关联

3

项与 Revere Pharmaceuticals, Inc. 相关的药物

RP-102124

靶点

RAC1

作用机制

RAC1抑制剂

在研机构

Revere Pharmaceuticals, Inc.初创企业

原研机构

Revere Pharmaceuticals, Inc.初创企业

在研适应症

非小细胞肺癌 [+1]

非在研适应症-

最高研发阶段临床申请

首次获批国家/地区-

首次获批日期-

RP-32661

靶点

RAC1

作用机制

RAC1抑制剂

在研机构

Revere Pharmaceuticals, Inc.初创企业

原研机构

Revere Pharmaceuticals, Inc.初创企业

在研适应症

结直肠癌 [+1]

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

RhoA Y42C(Revere)

靶点

RhoA Y42C

作用机制

RhoA Y42C抑制剂

在研机构

Revere Pharmaceuticals, Inc.初创企业

原研机构

Revere Pharmaceuticals, Inc.初创企业

在研适应症

胃癌

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

100 项与 Revere Pharmaceuticals, Inc. 相关的临床结果

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0 项与 Revere Pharmaceuticals, Inc. 相关的专利（医药）

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1

项与 Revere Pharmaceuticals, Inc. 相关的文献（医药）

2024-03-22·Cancer Research

Abstract 677: Discovery of a first-in-class allosteric inhibitor of the small GTPase Rac1

作者: Goka, Erik T. ; Shah, Mubarak Hasan ; Silverman, Robert ; Ravirala, Ramu ; Raman, Mayuri V. ; Mahankali, Sandeep ; Kar, Ronodip ; Cooper, Alan

AbstractThe Rac1 signaling pathway is known to be hyperactivated in numerous solid tumors. We developed a Rac1 AlphaLISA assay that is amenable to high-throughput screening (HTS) to screen large libraries of small molecules. Based on molecular modeling of a putative allosteric binding site for several of the hits, we optimized a series of compounds that lead to RP-102124. RP-102124 engages with Rac1 in both biochemical and cellular target engagement assays. RP-102124 has greater potency than previously reported Rac1 inhibitors in biochemical assays, with potent inhibition of phenotypic characteristics of Rac signaling such as cell migration and cytoskeletal rearrangements. RP-102124 is a Racmulti inhibitor with activity against oncogenic Rac1b. RP-102124 is orally bioavailable and shows dose dependent inhibition of tumor growth in xenograft models at doses that are well-tolerated. RP-102124 is a first-in-class allosteric Racmulti inhibitor that shows promising therapeutic potential.Citation Format: Robert Silverman, Alan Cooper, Ronodip Kar, Mayuri V. Raman, Ramu Ravirala, Mubarak Hasan Shah, Sandeep Mahankali, Erik T. Goka. Discovery of a first-in-class allosteric inhibitor of the small GTPase Rac1 [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2024; Part 1 (Regular Abstracts); 2024 Apr 5-10; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2024;84(6_Suppl):Abstract nr 677.

100 项与 Revere Pharmaceuticals, Inc. 相关的药物交易

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100 项与 Revere Pharmaceuticals, Inc. 相关的转化医学

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管线布局中药物为当前组织机构及其子机构作为药物机构进行统计，早期临床1期并入临床1期，临床1/2期并入临床2期，临床2/3期并入临床3期

临床前

2

1

临床申请

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当前项目

药物(靶点)	适应症	全球最高研发状态

RP-102124 ( RAC1 )	非小细胞肺癌更多	临床申请
RhoA Y42C(Revere) ( RhoA Y42C )	胃癌更多	临床前
RP-32661 ( RAC1 )	结直肠癌更多	临床前