Orantinib(Orantinib) - 药物靶点：FGFRs x PDGFR x VEGFR2_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

+ [4]

靶点

FGFRs x PDGFR x VEGFR2

作用机制

FGFRs拮抗剂(成纤维细胞生长因子受体家族拮抗剂)、PDGFR拮抗剂(血小板衍生生长因子受体拮抗剂)、VEGFR2拮抗剂(血管内皮细胞生长因子受体2拮抗剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Taiho Pharmaceutical Co., Ltd.

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)终止

特殊审评-

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结构

分子式C18H18N2O3

InChIKeyNHFDRBXTEDBWCZ-UHFFFAOYSA-N

CAS号252916-29-3

关联

13

项与 Orantinib 相关的临床试验

JPRN-JapicCTI-101354 / Unknown status临床3期

A Randomized, Double-Blind, Placebo-Controlled Phase III Trial Of TSU-68 In Combination With Transcatheter Arterial Chemoembolization In Patients With Unresectable Hepatocellular Carcinoma

开始日期2010-12-01

申办/合作机构

Taiho Pharmaceutical Co., Ltd.

NCT01465464 / Terminated临床3期

A Randomized, Double-Blind, Placebo-Controlled Phase III Trial Of TSU-68 In Combination With Transcatheter Arterial Chemoembolization In Patients With Unresectable Hepatocellular Carcinoma

The purpose of this study is to compare the overall survival (OS) for Orantinib in combination with transcatheter arterial chemoembolization (TACE) versus placebo in combination with TACE in patients with unresectable hepatocellular carcinoma (HCC).

开始日期2010-12-01

申办/合作机构

Taiho Pharmaceutical Co., Ltd.

JPRN-jRCT2080221054 / Unknown status临床2期

A Phase II study of TSU-68 in patient with hepatocellular carcinoma who are treated by transcatheter arterial chemoembolization (TACE)

开始日期2010-04-01

申办/合作机构

Taiho Pharmaceutical Co., Ltd.

100 项与 Orantinib 相关的临床结果

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100 项与 Orantinib 相关的转化医学

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100 项与 Orantinib 相关的专利（医药）

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130

项与 Orantinib 相关的文献（医药）

2024-10-01·Journal of Controlled Release

Biomimetic nanocomplex based corneal neovascularization theranostics

Article

作者: Su, Min ; Chen, Chuan ; Han, Yun ; Ye, Jinfa ; Liu, Gang ; Wei, Xingyuan ; Chu, Chengchao ; Wen, Xiaofei ; Cai, Shundong ; Pan, Jintao ; Cheng, Yuhang ; Wu, Yiming

Corneal neovascularization (CNV) is a major cause of blindness worldwide. However, the recent drug treatment is limited by repeated administration and low drug bioavailability. In this work, SU6668 (an inhibitor of receptor tyrosine kinases) and indocyanine green (ICG) are loaded onto poly(lactic-co-glycolic acid) (PLGA) nanoparticles, and then coated with anti-VEGFR2 single chain antibody (AbVr2 scFv) genetically engineered cell membrane vesicles. The nanomedicine is delivered via eye drops, and the hyperthermia induced by laser irradiation could block the blood vessels. Meanwhile, the photothermal effect can also cause the degradation of nanomaterials and release chemotherapeutic drugs in the blocked area, thereby continuously inhibit the neovascularization. Furthermore, SU6668 could inhibit the expression of heat shock protein 70 (HSP70), promoting the cell death induced by photothermal effect. In conclusion, the combination of photothermal and chemotherapy drugs provides a novel, effective and safe approach for the treatment of CNV.

2023-05-01·Chemico-Biological Interactions

Structure-based virtual screening of chemical libraries as potential MELK inhibitors and their therapeutic evaluation against breast cancer

Article

作者: Uppal, Sheetal ; Das, Amiya ; Lather, Viney ; Prajapati, Anita ; Agarwal, Pallavi ; Karna, Amarnath ; Pandita, Deepti ; Sharma, Hitesh Kumar

New targeted therapy for triple negative breast cancer (TNBC) is an urgent need, as advanced disease responds poorly to conventional chemotherapy. Genomic and proteomic studies are currently investigating new genes and proteins as promising therapeutic targets. One of such therapeutic targets is a cell cycle regulatory kinase; Maternal Embryonic Leucine Zipper Kinase (MELK), overexpressed in TNBC and correlated with cancer development. We performed molecular docking for virtual screening of chemical libraries (phytochemicals/synthetic drugs) against MELK protein structure and identified 8 phytoconstituents (isoxanthorin, emodin, gamma-coniceine, quercetin, tenuazonic acid, isoliquiritigenin, kaempferol, and Nobiletin) and 8 synthetic drugs (tetrahydrofolic acid, alfuzosin, lansoprazole, ketorolac, ketoprofen, variolin B, orantinib, and firestein) as potential hits interacting with the active site residues of MELK based on bound poses, hydrogen bond, hydrophobic interactions and MM/GBSA binding free energies. ADME and drug-likeness prediction further identified few hits with high drug-likeness properties and were further tested for anti-tumorigenic potential. Two phytochemicals isoliquiritigenin and emodin demonstrated growth inhibitory effects on TNBC MDA-MB-231 cells while much lower effect was observed on non-tumorigenic MCF-10A mammary epithelial cells. Treatment with both molecules downregulated MELK expression, induced cell cycle arrest, accumulated DNA damage and enhanced apoptosis. The study identified isoliquiritigenin and emodin as potential MELK inhibitors and provides a basis for subsequent experimental validation and drug development against cancer.

2023-01-01·Frontiers in pharmacology

A new molecular subclassification and in silico predictions for diagnosis and prognosis of papillary thyroid cancer by alternative splicing profile.

Article

作者: Guo, Yanzhi ; Li, Haiyan ; Lan, Hao ; Pu, Xuemei ; Li, Menglong

Introduction: Papillary thyroid cancer (PTC) is the most common endocrine malignancy. However, different PTC variants reveal high heterogeneity at histological, cytological, molecular and clinicopathological levels, which complicates the precise diagnosis and management of PTC. Alternative splicing (AS) has been reported to be potential cancer biomarkers and therapeutic targets. Method: Here, we aim to find a more sophisticated molecular subclassification and characterization for PTC by integrating AS profiling. Based on six differentially expressed alternative splicing (DEAS) events, a new molecular subclassification was proposed to reclassify PTC into three new groups named as Cluster0, Cluster1 and Cluster2 respectively. Results: An in silico prediction was performed for accurate recognition of new groups with the average accuracy of 91.2%. Moreover, series of analyses were implemented to explore the differences of clinicopathology, molecular and immune characteristics across them. It suggests that there are remarkable differences among them, but Cluster2 was characterized by poor prognosis, higher immune heterogeneity and more sensitive to anti-PD1 therapy. The splicing correlation networks proved the complicated regulation relationships between AS events and splicing factors (SFs). An independent prognostic indicator for PTC overall survival (OS) was established. Finally, three compounds (orantinib, tyrphostin-AG-1295 and AG-370) were discovered to be the potential therapeutic agents. Discussion: Overall, the six DEAS events are not only potential biomarkers for precise diagnosis of PTC, but also the probable prognostic predictors. This research would be expected to highlight the effect of AS events on PTC characterization and also provide new insights into refining precise subclassification and improving medical therapy for PTC patients.

100 项与 Orantinib 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12072

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
乳腺癌	临床2期	-	Taiho Pharmaceutical Co., Ltd.	-
乳腺癌	临床2期	-	Pfizer Inc.	-
乳腺癌	临床1期	韩国	Taiho Pharmaceutical Co., Ltd.	-
胃癌	临床1期	日本	Taiho Pharmaceutical Co., Ltd.	-
肝细胞癌	药物发现	中国	Taiho Pharmaceutical Co., Ltd.	2010-12-01
不可切除的肝细胞癌	药物发现	中国台湾	Taiho Pharmaceutical Co., Ltd.	2010-12-01
不可切除的肝细胞癌	药物发现	韩国	Taiho Pharmaceutical Co., Ltd.	2010-12-01
不可切除的肝细胞癌	药物发现	日本	Taiho Pharmaceutical Co., Ltd.	2010-12-01
结直肠癌	药物发现	韩国	Taiho Pharmaceutical Co., Ltd.	-
肝癌	药物发现	-	Pfizer Inc.	-

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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


NCT01465464 (ORIENTAL, CTgov)	临床3期	不可切除的肝细胞癌	888	Orantinib (TSU-68) (Orantinib)	(選積糧廠襯廠餘繭觸製) = 遞顧築鹹淵積鏇齋顧觸膚獵鏇餘繭衊壓觸餘壓 (積顧齋願廠壓獵醖築廠, 鹽範觸齋積鬱廠鹹網鏇 ~ 夢淵簾廠選餘艱繭糧獵) 更多	-	2019-08-07
NCT01465464 (ORIENTAL, CTgov)	临床3期	不可切除的肝细胞癌	888	Placebo (Placebo)	(選積糧廠襯廠餘繭觸製) = 憲壓選遞繭廠製構艱醖膚獵鏇餘繭衊壓觸餘壓 (積顧齋願廠壓獵醖築廠, 網鹽遞觸構製築選醖襯 ~ 鹹艱艱憲鑰廠襯淵鏇積) 更多	-	2019-08-07
NCT01465464 (ORIENTAL, Pubmed \| Lancet Gastroenterol Hepatol) 人工标引	临床3期	不可切除的肝细胞癌	889	Orantinib+ cTACE+Orantinib	(構選構淵齋築簾積築淵) = 艱襯衊鬱艱糧選廠選願範膚窪艱壓襯夢遞窪襯 (顧獵夢網醖膚齋構膚製, 26.5 ~ 34.5) 更多	不佳	2018-01-01
	临床3期	不可切除的肝细胞癌	889	Placebo	(構選構淵齋築簾積築淵) = 願網製鹹積製窪窪遞鑰範膚窪艱壓襯夢遞窪襯 (顧獵夢網醖膚齋構膚製, 28.4 ~ NR) 更多	不佳	2018-01-01
JPRN-JapicCTI-121970 (ASCO_GI2013)	临床1期	晚期肝细胞癌	18	TSU-68 plus S-1 combination	(鏇壓膚餘醖壓繭簾壓願) = 鬱襯鬱鏇鏇憲簾繭繭淵衊構獵憲築選鑰遞鬱壓 (餘襯衊築艱願簾齋憲網 ) 更多	-	2013-02-01
NCT00784290 (Pubmed \| Cancer Chemother Pharmacol)	临床1/2期	晚期肝细胞癌	35	TSU-68 200 mg bid	(選鏇製獵願構廠齋淵繭) = 範襯廠範鏇醖糧簾觸獵醖壓餘構衊築鹹範餘淵 (構衊繭繭憲憲簾鬱艱範 ) 更多	积极	2011-02-01
ASCO2010	临床2期	肝细胞癌	101	TSU-68 400 mg/d	(鏇壓壓壓膚餘鏇選壓淵) = 餘網窪壓製製鏇製鏇憲糧遞齋鹽鹽築選鹽鹽範 (遞醖範艱齋憲醖積構窪 )	-	2010-05-20
ASCO2010	临床2期	肝细胞癌	101	No antitumor therapy	(鏇壓壓壓膚餘鏇選壓淵) = 齋齋鑰鑰蓋鏇範夢簾積糧遞齋鹽鹽築選鹽鹽範 (遞醖範艱齋憲醖積構窪 )	-	2010-05-20
ASCO2008	临床1/2期	晚期肝细胞癌	35	TSU-68 400 mg/d	(廠夢衊鹽範醖構選糧鬱) = 襯獵構觸築鏇積蓋鬱鏇襯製餘糧齋蓋構蓋繭製 (鏇鏇餘構憲網網餘遞襯 ) 更多	积极	2008-05-20