NO-Ursodeoxycholic Acid(NO-Ursodeoxycholic Acid) - 药物靶点：caspase 3 x caspase 8 x caspase 9_专利_临床

概要

基本信息

药物类型

小分子化药

别名

,no-udca、NO-ursodiol

+ [2]

靶点

caspase 3 x caspase 8 x caspase 9

作用方式

抑制剂

作用机制

caspase 3抑制剂(半胱天冬酶-3抑制剂)、caspase 8抑制剂(半胱天冬酶-8抑制剂)、caspase 9抑制剂(半胱天冬酶-9抑制剂)

治疗领域

消化系统疾病

在研适应症-

非在研适应症

门静脉高血压

原研机构

Nicox SA

在研机构-

非在研机构

Nicox SAForest Laboratories, Inc.

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C38H55NO10

InChIKeyWTAVOESJEWSDJC-DNVPPMEBSA-N

CAS号301828-26-2

关联

4

项与 NO-Ursodeoxycholic Acid 相关的临床试验

NCT03512821

/ Completed临床1期

A Single-dose, Comparative Bioavailability Study of Two Formulations of Ursodiol 500mg Tablets Under Fed Conditions

single-dose, comparative bioavailability study of two formulations of ursodiol 500mg tablets under fed conditions

开始日期2017-10-01

申办/合作机构

Daewoong Pharmaceutical Co., Ltd.

NCT03512808

/ Completed临床1期

A Single-dose, Comparative Bioavailability Study of Two Formulations of Ursodiol 500mg Tablets Under Fasting Conditions

A single-dose, comparative bioavailability study of two formulations of ursodiol 500mg tablets under fasting conditions

开始日期2017-06-01

申办/合作机构

Daewoong Pharmaceutical Co., Ltd.

EUCTR2005-003483-31-ES

/ Not yet recruiting临床2期

Eficacia y tolerabilidad preliminar del NCX-1000 oral después de repetidas administraciones a pacientes con hipertensión portal. Estudio a doble ciego con dosis creciente

开始日期2005-11-17

申办/合作机构-

100 项与 NO-Ursodeoxycholic Acid 相关的临床结果

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100 项与 NO-Ursodeoxycholic Acid 相关的转化医学

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100 项与 NO-Ursodeoxycholic Acid 相关的专利（医药）

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13

项与 NO-Ursodeoxycholic Acid 相关的文献（医药）

2022-01-25·Gastroenterology Report

Co-administration of ursodeoxycholic acid with rosuvastatin/ezetimibe in a non-alcoholic fatty liver disease model

Article

作者: Lee, Da Hyun ; Seo, Sang Hyun ; Bae, Soo Han ; Kim, Do Young ; Cho, Kyung Joo ; Ahn, Sang Hoon ; Kim, Seung Up ; Park, Hye Jung ; Lee, Hye Won ; Kim, Beom Kyung ; Lee, Yu Seol ; Park, Jun Yong

AbstractBackgroundUrsodeoxycholic acid (UDCA), statins, and ezetimibe (EZE) have demonstrated beneficial effects against non-alcoholic fatty liver disease (NAFLD). We investigated the efficacy of the combination of UDCA and the mix of rosuvastatin (RSV)/EZE in the treatment of NAFLD.MethodsNAFLD mouse models were developed by injecting thioacetamide, fasting, and high-carbohydrate refeeding, high-fat diet, and choline-deficient L-amino acid-defined high-fat diet (CDAHFD). Low-dose UDCA (L-UDCA; 15 mg/kg) or high-dose UDCA (H-UDCA; 30 mg/kg) was administered with RSV/EZE. We also employed an in vitro model of NAFLD developed using palmitic acid-treated Hepa1c1c7 cells.ResultsCo-administration of RSV/EZE with UDCA significantly decreased the collagen accumulation, serum alanine aminotransferase (ALT) levels, and mRNA levels of fibrosis-related markers than those observed in the vehicle group in thioacetamide-treated mice (all P < 0.01). In addition, in the group fasted and refed with a high-carbohydrate diet, UDCA/RSV/EZE treatment decreased the number of apoptotic cells and serum ALT levels compared with those observed in the vehicle group (all P < 0.05). Subsequently, H-UDCA/RSV/EZE treatment decreased the number of ballooned hepatocytes and stearoyl-CoA desaturase 1 (SCD-1) mRNA levels (P = 0.027) in the liver of high-fat diet-fed mice compared with those observed in the vehicle group. In the CDAHFD-fed mouse model, UDCA/RSV/EZE significantly attenuated collagen accumulation and fibrosis-related markers compared to those observed in the vehicle group (all P < 0.05). In addition, UDCA/RSV/EZE treatment significantly restored cell survival and decreased the protein levels of apoptosis-related markers compared to RSV/EZE treatment in palmitic acid-treated Hepa1c1c7 cells (all P < 0.05).ConclusionCombination therapy involving UDCA and RSV/EZE may be a novel strategy for potent inhibition of NAFLD progression.

2011-01-01·International Journal of Hepatology

NCX 1000 Alone or in Combination with Vitamin E Reverses Experimental Nonalcoholic Steatohepatitis in the Rat Similarly to UDCA

Article

作者: Brault, Antoine ; Vallerand, Diane ; Haddad, Yara ; Haddad, Pierre S. ; Spénard, Jean

We explored the therapeutic effect of NCX 1000, a derivative of ursodeoxycholic acid (UDCA) with nitric oxide (NO) donating properties, alone or in combination with vitamin E, in an experimental model of NASH in the rat.Methods. A control group was fed a standard liquid diet (Control), and the NASH groups were fed a high-fat liquid diet for 12 weeks without (NASH) or with simultaneous daily gavage with either NCX 1000 at 15 or 30 mg/kg (N15 and N30, resp.), or N15 plus vitamin E 100 mg/kg (N15 + VitE) for the last 6 weeks; UDCA 17.2 mg/kg was used as a reference.Results. NASH rats developed all key features of the disease. Treatments with N30 improved liver histology, decreased lipid peroxidation, and completely suppressed increases in LDH release, plasma insulin, and TNF-α. It also decreasedO2∙-release and returned liver weight and glutathione back to normal. All effects were similar to the reference treatment, UDCA. The N15 treatment was less efficient than the N30 group, but became comparable to the latter when combined to vitamin E.Conclusion. Our study demonstrates that NCX 1000 has potent cytoprotective, antioxidant, and hypoinsulinemic properties that can be enhanced by combination with vitamin E.

2010-12-01·Yao xue xue bao = Acta pharmaceutica Sinica

[Synthesis and biological evaluation of nitrate-oleanolic acid hybrids as inhibitors of HepG2 cell apoptosis].

Article

作者: Chen, Li ; Shang, Juan ; Zhang, Yi-hu ; Tian, Ji-de ; Wang, Zhi-feng

To find novel antihepatitis drugs, a series of nitrate-oleanolic acid (OA) hybrids (10a, 10b, 11a-11e and 12a-12c) were designed and synthesized on the basis of previous studies using OA as lead compound, which is widely found in natural plants and liver-specific metabolism. In the present study, ten novel NO-releasing derivatives of OA were synthesized by connecting nitrate to the OA-3-OH through varying lengths of linkers containing antioxidants which were designed to increase the ability of these target compounds to scavenge free radicals. The structures of these objective compounds were determined by IR, MS, 1H NMR and elemental analysis. Their protective effects on anti-Fas mediated HepG2 cell apoptosis were in vitro evaluated by LDH assay. Compound 12a is the most potent inhibitor. Its effect on anti-Fas mediated HepG2 cell apoptosis and amount of NO-releasing in vitro are similar to those of positive control NCX-1000.

100 项与 NO-Ursodeoxycholic Acid 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	NO-Ursodeoxycholic Acid	-	DB16026

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
门静脉高血压	临床2期	西班牙	Forest Laboratories, Inc.	2005-11-01

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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


PANURSO STUDY (UEGW2021)	N/A	胰腺炎	422	UDCA	願窪觸簾艱鬱蓋艱廠繭(淵觸糧鹹窪廠廠範構糧) = 糧齋鬱顧鏇獵齋憲鬱繭構衊顧獵繭膚鏇獵膚觸 (蓋觸淵憲憲顧壓齋衊廠, 660 ~ 790) 更多	积极	2021-10-02
				No UDCA	願窪觸簾艱鬱蓋艱廠繭(淵觸糧鹹窪廠廠範構糧) = 鑰獵鹽鹽觸襯夢鹽遞廠構衊顧獵繭膚鏇獵膚觸 (蓋觸淵憲憲顧壓齋衊廠, 525 ~ 664)
EHA2017	N/A	血栓性微血管病	671	Ursodeoxycholic acid	願築製築製蓋衊糧餘顧(遞廠窪製夢壓鏇鹽鹹齋) = 餘築膚簾憲築範顧鏇醖選壓淵範襯範膚獵選壓 (願鏇壓蓋鬱衊鹹範齋鏇, 5.9 ~ 14.3)	-	2017-05-18
				Non-ursodeoxycholic acid	願築製築製蓋衊糧餘顧(遞廠窪製夢壓鏇鹽鹹齋) = 願鏇構齋顧憲壓糧選築選壓淵範襯範膚獵選壓 (願鏇壓蓋鬱衊鹹範齋鏇, 11.7 ~ 18.1)