Amcasertib(Amcasertib) - 药物靶点：NANOG_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Amcasertib (USAN/INN)

+ [3]

靶点

NANOG

作用机制

NANOG调节剂(Nanog homeobox modulators)

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [3]

在研适应症-

非在研适应症

晚期癌症晚期肝细胞癌晚期恶性实体瘤+ [7]

原研机构

Avania LLC

在研机构-

非在研机构

Sumitomo Pharma America, Inc.

Avania LLC

北京强新生物科技有限公司

+ [1]

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C31H33N5O2S

InChIKeyQDWKGEFGLQMDAM-UHFFFAOYSA-N

CAS号1129403-56-0

关联

9

项与 Amcasertib 相关的临床试验

NCT02232620

/ Terminated临床2期

A Phase II Clinical Study of BBI503 in Adult Patients With Advanced Gastrointestinal Stromal Tumors

This is an open label, multi-center, phase II study of BBI503 administered to adult patients with advanced gastrointestinal stromal tumor who have exhausted all currently approved standard anti-cancer treatment options. BBI503 will be administered orally, daily, in continuous 28-day cycles at a dose of 300 mg once daily. Cycles will be repeated until patients are no longer clinically benefiting from therapy due to disease progression, adverse events, or another discontinuation criterion.
Safety, tolerability and efficacy of BBI503 will be assessed for the duration of study treatment.

开始日期2017-03-13

申办/合作机构

Sumitomo Pharma America, Inc.

NCT02232646

/ Withdrawn临床2期

A Phase II Clinical Study of BBI503 in Adult Patients With Advanced Urologic Malignancies

This is an open label, multi-center, Phase II study of BBI503 administered to adult patients with selected advanced urologic malignancies. The primary objective of this study is to evaluate the disease control rate of patients with renal cell cancer and urothelial carcinoma treated with BBI503.

开始日期2017-01-01

申办/合作机构

Sumitomo Pharma America, Inc.

NCT02483247

/ Completed临床1期

A Phase Ib/II Clinical Study of BBI503 in Combination With Selected Anti-Cancer Therapeutics in Adult Patients With Advanced Cancer

This is an open label, multi-center, Phase 1/2 study of BBI503 administered in combination with selected anti-cancer therapeutics in adult patients with advanced cancer. The goal of the study is to determine the safety, tolerability, and RP2D of BBI503 in combination with each of the selected anti-cancer agents.

开始日期2015-09-01

申办/合作机构

Sumitomo Pharma America, Inc.

100 项与 Amcasertib 相关的临床结果

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100 项与 Amcasertib 相关的转化医学

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100 项与 Amcasertib 相关的专利（医药）

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1

项与 Amcasertib 相关的文献（医药）

Medical Oncology

Cancer stemness kinase inhibitor amcasertib: a promising therapeutic agent in ovarian cancer stem and cancer cell models with different genetic profiles

Article

作者: Asik, Aycan ; Guler Kara, Hale ; Gunduz, Cumhur ; Ozates, Neslihan Pinar

Ovarian cancer, often referred to as the 'silent killer,' is a significant contributor to mortality rates. Emerging evidence implicates Nanog as a potential therapeutic target in ovarian cancer. Amcasertib (BBI-503) is an orally administered primary class stemness kinase inhibitor that effectively targets NANOG and various cancer stem cell pathways by specifically inhibiting serine-threonine stemness kinases. This study aimed to evaluate the antineoplastic effects of Nanog inhibition, a critical transcription factor associated with pluripotency and its role in ovarian cancer tumorigenesis, using the novel therapeutic agent Amcasertib in ovarian cancer cells characterized by distinct genetic profiles. The cytotoxicity of Amcasertib was assessed in both ovarian cancer and cancer stem cell models utilizing the Xelligence-RTCA system. The impact of the determined IC50 dose on apoptosis, invasion, migration, epithelial-mesenchymal transition (EMT), cell cycle progression, colony formation, and spheroid growth was evaluated using appropriate analytical techniques. Our findings revealed that Amcasertib exhibited significant antiproliferative effects and induced apoptosis in ovarian cancer and cancer stem cells. Moreover, Amcasertib caused G1 phase arrest and impeded colony formation in MDAH-2774 cells. Additionally, Amcasertib effectively inhibited spheroid growth in OVCAR-3 and OCSC cells. Notably, it demonstrated the ability to suppress invasion and migration in MDAH-2774 and OCSC cells. Furthermore, the suppression of Nanog-mediated stem cell-like features by Amcasertib was particularly pronounced in ER-negative ovarian cancer and cancer stem cells, highlighting its high anticancer efficacy in this subgroup. These results suggest that Amcasertib holds promise as a potential standalone or combination therapy agent for the treatment of ER-negative ovarian cancer.

100 项与 Amcasertib 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10903	-	-	DB14866

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
胆管癌	临床3期	-	北京强新生物科技有限公司	-
肝胆癌	临床2期	加拿大	Sumitomo Pharma America, Inc.	2015-02-01
晚期肝细胞癌	临床2期	美国	Sumitomo Pharma America, Inc.	2014-12-01
胆管癌	临床2期	-	Avania LLC	-
胆管癌	临床2期	-	北京强新生物科技有限公司	-
胆管癌	临床2期	-	Avania LLC	-
肝细胞癌	临床2期	-	Avania LLC	-
肝细胞癌	临床2期	-	Avania LLC	-
肝细胞癌	临床2期	-	北京强新生物科技有限公司	-
肝细胞癌	临床1期	-	北京强新生物科技有限公司	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02432690 (CTgov)	临床2期	复发性卵巢癌	13	BBI503	衊範構選窪獵淵淵遞鏇(襯繭窪積鹽獵鬱鏇艱壓) = 膚鑰網夢獵鬱鹹壓網獵鑰衊襯憲範壓廠鏇獵簾 (襯築構蓋範鑰鏇醖觸繭, 築築範遞醖窪醖鑰構鏇 ~ 積網廠鏇襯艱簾膚網築) 更多	-	2022-08-29
NCT01781455 (ASCO2017)	临床1/2期	腺样囊性癌	14	Amcasertib	(廠蓋蓋顧醖鑰齋壓衊構) = 鑰膚壓築襯遞餘願餘範襯襯製餘鑰觸鏇鑰憲鏇 (獵蓋餘網膚蓋窪壓醖築 ) 更多	-	2017-05-30
NCT01781455 (ASCO2017)	临床1/2期	晚期头颈癌	21	Amcasertib	(獵鹹繭壓餘憲齋艱製遞) = 窪範壓選鹹積選膚壓鏇繭醖獵窪獵鏇淵艱艱鏇 (糧範淵壓觸構艱淵簾鑰 ) 更多	-	2017-05-30
NCT01781455 (ASCO2016)	临床1期	晚期头颈癌	33	BB503	(蓋窪窪醖構築憲醖網廠) = Grade 3 AE included rapidly reversible diarrhea (n = 5) and nausea/vomiting (n = 1) 襯艱築壓獵鹽鬱艱廠廠 (鑰餘糧夢築鏇願願遞選 )	积极	2016-05-20
NCT01781455 (ASCO2015)	临床1期	晚期结直肠腺癌	47	BBI503 monotherapy	(醖廠蓋窪顧衊餘觸網構) = 齋糧鹹鹽糧遞網顧窪繭衊淵鏇襯鬱餘蓋糧糧襯 (壓淵鬱壓製築壓窪範衊 )	-	2015-05-20
NCT01781455 (ASCO2014)	临床1期	HR阳性/HER2低表达实体瘤	26	BBI503	(鬱遞醖窪壓觸網齋鬱製) = 窪蓋淵願糧齋鹹鏇衊憲鏇製製衊窪鏇獵網積齋 (觸鹹蓋積餘襯艱構壓鬱 ) 更多	-	2014-05-20