Foslinanib(Xingtai Ruizhuang Biotechnology Co Ltd)(Foslinanib(Xingtai Ruizhuang Biotechnology Co Ltd)) - 在研适应症：不可切除的肝细胞癌，晚期神经内分泌肿瘤，胃肠胰神经内分泌肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Foslinanib、Foslinanib (USAN/INN)、Trx-818 free acid

+ [2]

靶点-

作用机制

血管生成抑制剂、细胞凋亡刺激剂

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [1]

在研适应症

不可切除的肝细胞癌晚期神经内分泌肿瘤胃肠胰神经内分泌肿瘤+ [5]

非在研适应症

晚期肝细胞癌晚期恶性实体瘤肺癌+ [1]

原研机构

邢台睿壮生物科技有限公司

在研机构

台睿生物科技股份有限公司邢台睿壮生物科技有限公司

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)无进展

特殊审评-

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结构

分子式C16H13FNNa2O6P

InChIKeyHANFVYCDGRSZSD-UHFFFAOYSA-N

CAS号1256037-62-3

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关联

6

项与 Foslinanib(Xingtai Ruizhuang Biotechnology Co Ltd) 相关的临床试验

NCT05257590 / Recruiting临床2期

A Phase 2, Open-Label Study of CVM-1118 in Combination With Nivolumab in Subjects With Unresectable Advanced Hepatocellular Carcinoma

CVM-1118 is a new small molecule chemical entity being developed as a potential anti-cancer therapeutic by TaiRx, Inc. CVM-1118 is a potent anti-cancer agent in numerous human cancer cell lines. The safety of administrating CVM-1118 on human has been evaluated from the phase 1 study. The objective of the phase 2 study is to further investigate the efficacy of CVM-1118 with nivolumab for subjects with unresectable advanced hepatoma.

开始日期2022-05-23

申办/合作机构

台睿生物科技股份有限公司

NCT04336124 / Completed临床1期

A Phase I Safety and Pharmacokinetic Study of CVM-1118 Extended-Release Capsules Administered Orally to Patients With Advanced Cancers

CVM-1118 Immediate-release (IR) Capsule and CVM-1118 Extended-release (ER) Capsule are proprietary oncology products developed by TaiRx, Inc. for the treatment of patients suffering from advanced cancer. Due to the short elimination half-life of CVM-1118 IR capsules, the extended release (ER) formulation, containing mini-tablets in hard capsule, has been developed to prolong the drug absorption and longer exposure after oral administration. The designed dose of CVM-1118 ER was 200 mg per capsule to provide a more patient-compliant and safe dosage of CVM-1118. The clinical study CVMEX-001 is therefore designed to evaluate the safety and pharmacokinetics of CVM-1118 extend release (ER) Capsule (200 mg/capsule) in patients with advanced cancer.

开始日期2020-05-25

申办/合作机构

台睿生物科技股份有限公司

NCT03600233 / Active, not recruiting临床2期

A Phase II, Open-label Study of CVM-1118 Administered Orally to Patients With Advanced Neuroendocrine Tumors

CVM-1118 (TRX-818) is a new small molecule chemical entity being developed as a potential anti-cancer therapeutic by TaiRx, Inc. CVM-1118 is a potent anti-cancer agent in numerous human cancer cell lines. The safety of administrating CVM-1118 on human is evaluated from the phase 1 study. The objectives of the phase 2 study is to further investigate the efficacy of CVM-1118 for patients with advanced neuroendocrine tumors.

开始日期2018-12-15

申办/合作机构

台睿生物科技股份有限公司

100 项与 Foslinanib(Xingtai Ruizhuang Biotechnology Co Ltd) 相关的临床结果

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100 项与 Foslinanib(Xingtai Ruizhuang Biotechnology Co Ltd) 相关的转化医学

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100 项与 Foslinanib(Xingtai Ruizhuang Biotechnology Co Ltd) 相关的专利（医药）

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5

项与 Foslinanib(Xingtai Ruizhuang Biotechnology Co Ltd) 相关的文献（医药）

2024-08-01·Angiogenesis

Vascular mimicry in zebrafish fin regeneration: how macrophages build new blood vessels

Article

作者: Fazzari, Jennifer ; Djonov, Valentin ; Senk, Anita

AbstractVascular mimicry has been thoroughly investigated in tumor angiogenesis. In this study, we demonstrate for the first time that a process closely resembling tumor vascular mimicry is present during physiological blood vessel formation in tissue regeneration using the zebrafish fin regeneration assay. At the fin-regenerating front, vasculature is formed by mosaic blood vessels with endothelial-like cells possessing the morphological phenotype of a macrophage and co-expressing both endothelial and macrophage markers within single cells. Our data demonstrate that the vascular segments of the regenerating tissue expand, in part, through the transformation of adjacent macrophages into endothelial-like cells, forming functional, perfused channels and contributing to the de novo formation of microvasculature. Inhibiting the formation of tubular vascular-like structures by CVM-1118 prevents vascular mimicry and network formation resulting in a 70% shorter regeneration area with 60% reduced vessel growth and a complete absence of any signs of regeneration in half of the fin area. Additionally, this is associated with a significant reduction in macrophages. Furthermore, depleting macrophages using macrophage inhibitor PLX-3397, results in impaired tissue regeneration and blood vessel formation, namely a reduction in the regeneration area and vessel network by 75% in comparison to controls.

2016-11-01·American Journal of Physiology-Gastrointestinal and Liver Physiology3区 · 医学

Somatostatin regulates NHE8 protein expression via the ERK1/2 MAPK pathway in DSS-induced colitis mice

3区 · 医学

Article

作者: Li, Xiao ; Wang, Chunhui ; Lu, Jing ; Xu, Hua ; Sun, Dan ; Tao, Liping ; Cai, Lin ; Geng, Chong ; Ghishan, Fayez K.

Previous studies reported that administration of somatostatin (SST) to human patients mitigated their diarrheal symptoms. Octreotide (an analog of SST) treatment in animals resulted in upregulation of sodium/hydrogen exchanger 8 (NHE8). NHE8 is important for water/sodium absorption in the intestine, and loss of NHE8 function results in mucosal injury. Thus we hypothesized that NHE8 expression is inhibited during colitis and that SST treatment during pathological conditions can restore NHE8 expression. Our data showed for the first time that NHE8 is expressed in the human colonic tissue and that NHE8 expression is decreased in ulcerative colitis (UC) patients. We also found that octreotide could stimulate colonic NHE8 expression in colitic mice. Furthermore, the somatostatin receptor 2 (SSTR2) agonist seglitide and the somatostatin receptor 5 (SSTR5) agonist L-817,818 could restore NHE8 expression via its role in suppressing ERK1/2 phosphorylation. Our study uncovered a novel mechanism of SST stimulation of NHE8 expression in colitis.

2016-03-01·Pharmacology & Therapeutics1区 · 医学

Tumor cell vascular mimicry: Novel targeting opportunity in melanoma

1区 · 医学

Review

作者: Seftor, Richard E B ; Chao, Jun-Tzu ; Chien, Du-Shieng ; Hendrix, Mary J C ; Chu, Yi-Wen ; Seftor, Elisabeth A

In 1999, the American Journal of Pathology published an article, entitled "Vascular channel formation by human melanoma cells in vivo and in vitro: vasculogenic mimicry" by Maniotis and colleagues, which ignited a spirited debate for several years and earned the journal's distinction of a "citation classic" (Maniotis et al., 1999). Tumor cell vasculogenic mimicry (VM), also known as vascular mimicry, describes the plasticity of aggressive cancer cells forming de novo vascular networks and is associated with the malignant phenotype and poor clinical outcome. The tumor cells capable of VM share the commonality of a stem cell-like, transendothelial phenotype, which may be induced by hypoxia. Since its introduction as a novel paradigm for melanoma tumor perfusion, many studies have contributed new findings illuminating the underlying molecular pathways supporting VM in a variety of tumors, including carcinomas, sarcomas, glioblastomas, astrocytomas, and melanomas. Of special significance is the lack of effectiveness of angiogenesis inhibitors on tumor cell VM, suggesting a selective resistance by this phenotype to conventional therapy. Facilitating the functional plasticity of tumor cell VM are key proteins associated with vascular, stem cell, extracellular matrix, and hypoxia-related signaling pathways--each deserving serious consideration as potential therapeutic targets and diagnostic indicators of the aggressive, metastatic phenotype. This review highlights seminal findings pertinent to VM, including the effects of a novel, small molecular compound, CVM-1118, currently under clinical development to target VM, and illuminates important molecular pathways involved in the suppression of this plastic, aggressive phenotype, using melanoma as a model.

100 项与 Foslinanib(Xingtai Ruizhuang Biotechnology Co Ltd) 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11639	-	-	DB16172

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
晚期神经内分泌肿瘤	临床2期	中国台湾	台睿生物科技股份有限公司	2018-12-15
胃肠胰神经内分泌肿瘤	临床2期	中国台湾	台睿生物科技股份有限公司	2018-12-15
神经内分泌癌	临床2期	中国台湾	台睿生物科技股份有限公司	2018-12-15
肺神经内分泌肿瘤	临床2期	中国台湾	台睿生物科技股份有限公司	2018-12-15
晚期癌症	临床2期	中国台湾	台睿生物科技股份有限公司	2018-07-12
肝癌	临床2期	-	邢台睿壮生物科技有限公司	-
肺癌	临床1期	中国	台睿生物科技股份有限公司	2018-12-15
晚期癌症	临床1期	美国	台睿生物科技股份有限公司	2018-07-12
晚期肝细胞癌	临床1期	中国台湾	台睿生物科技股份有限公司	2018-07-12
晚期肝细胞癌	临床1期	美国	台睿生物科技股份有限公司	2018-07-12

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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


NCT03600233 (ESMO2024) 人工标引	临床2期	晚期神经内分泌肿瘤	34	CVM-1118	(鹽鏇餘鏇築顧積襯艱築) = 築襯積製淵繭積醖齋襯簾獵鹹蓋獵齋鏇遞繭衊 (夢簾繭顧積鏇鹹壓鏇窪, 5.9 ~ 23.8) 更多	积极	2024-09-13
NCT05257590 (ASCO2024) 人工标引	临床2期	晚期肝细胞癌	31	CVM-1118 200 mg BID + nivolumab 240 mg Q2W	(膚廠鹽鹽遞齋夢鏇淵遞) = 糧繭網觸獵蓋願糧製鏇築醖淵艱鑰醖廠選構簾 (餘窪積繭夢積糧廠醖鏇 ) 更多	积极	2024-05-24
NCT03600233 (ASCO2023) 人工标引	临床2期	晚期神经内分泌肿瘤	21	CVM-1118 200-300 mg BID	(獵製憲觸願鬱淵艱衊淵) = 餘構鏇築艱齋鹽鏇蓋衊壓憲醖廠獵醖鑰製鹹襯 (獵膚蓋積繭繭糧簾遞鏇, 14–50) 更多	积极	2023-05-31
NCT02507544 \| NCT02703298 (ASCO2017) 人工标引	临床1期	晚期癌症	28	CVM-1118 (US)	(齋襯遞廠蓋憲窪鹽膚鏇) = 2 DLTs (grade 5 dehydration and grade 3 fatigue) were reported at cohort 6 (800 mg/daily) 廠餘製積鏇艱淵網製餘 (膚壓醖鏇遞築壓顧簾夢 ) 更多	积极	2017-06-05
NCT02507544 \| NCT02703298 (ASCO2017) 人工标引	临床1期	晚期癌症	28	CVM-1118 (Taiwan)		积极	2017-06-05