奥谷法奈二钠(Oglufanide disodium)

概要

基本信息

药物类型

小分子化药

别名

Glufanide disodium、Glutamyltryptophan、L-Glu-L-Trp

+ [9]

靶点-

作用机制

血管生成抑制剂、免疫调节剂

治疗领域

肿瘤免疫系统疾病感染+ [5]

在研适应症-

非在研适应症

获得性免疫缺陷综合征细菌感染结直肠癌+ [5]

原研机构

ALZA Corp.

在研机构-

非在研机构

Cytran, Inc.

Implicit Bioscience Ltd.

ALZA Corp.

最高研发阶段终止临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构

分子式C16H19N3NaO5

InChIKeyUOKXDTZUCQYLHK-JZKFLRDJSA-N

CAS号237068-57-4

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关联

5

项与奥谷法奈二钠相关的临床试验

ACTRN12607000418471 / Completed临床2期

In patients with chronic hepatitis C, does treatment with oglufanide disodium reduce viral load from baseline value?

开始日期2007-08-08

申办/合作机构-

NCT00017303 / Unknown status临床2期

A Phase II Trial Of IM862 Combined With Paclitaxel And Carboplatin In Newly Diagnosed Advanced Epithelial Ovarian Or Primary Peritoneal Carcinoma Followed By IM862 Consolidation Therapy

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die. IM-862 may kill tumor cells by stopping blood flow to the tumor and by stimulating a person's white blood cells to kill tumor cells. Combining chemotherapy and IM-862 may kill more tumor cells.
PURPOSE: Randomized phase II trial to study the effectiveness of combination chemotherapy and IM-862 in treating patients who have resected stage III ovarian cancer or primary peritoneal cancer.

开始日期2001-01-01

申办/合作机构

Cytran, Inc.

NCT00006037 / Terminated临床2期IIT

Phase II Randomized Placebo-Controlled Double-Blinded Study With 5-FU vs. 5-FU With IM862 With Cross-Over to CPT-11 vs. CPT-11 With IM862

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die. IM-862 may stop the growth of colorectal cancer by stopping blood flow to the tumor. It is not yet known if chemotherapy is more effective with or without IM-862 in treating colorectal cancer.
PURPOSE: Randomized phase II trial to study the effectiveness of chemotherapy plus IM-862 in treating patients who have metastatic colorectal cancer.

开始日期1999-11-01

申办/合作机构

University of Southern California

[+1]

100 项与奥谷法奈二钠相关的临床结果

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100 项与奥谷法奈二钠相关的转化医学

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100 项与奥谷法奈二钠相关的专利（医药）

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1,507

项与奥谷法奈二钠相关的文献（医药）

2025-02-01·Meat Science

High leucine bioavailability improves beef quality by altering serum metabolism in beef cattle

Article

作者: Shen, Weijun ; He, Huitian ; Wang, Zuo ; Lan, Xinyi ; Ge, Yu ; Liu, Lei ; Zhao, Xiangchao ; Wan, Fachun ; Cheng, Anwei ; An, Jishan ; Song, Yang

This study aimed to investigate the effect of dietary L-Leu supplementation on amino acid composition, serum metabolism, and meat quality characteristics in beef cattle. Twenty-four Angus cows of similar initial weight (575.5 ± 22.1 kg) were randomly assigned to two treatment groups with six replicate pens (two cattle per pen). The groups were fed a basal diet (CON) or a basal diet supplemented with 6.0 g/100 kg BW per day of L-Leu for 120 days pre-slaughter. Feeding L-Leu significantly increased average daily gain and decreased feed-to-weight-gain ratio (P < 0.05). L-Leu improved plasma free leucine bioavailability (P < 0.05), increased the concentrations of tyrosine and glutamine (P < 0.05), and decreased the concentrations of threonine and valine (P < 0.05). It also increased the content of total protein in plasma (P < 0.05). Supplementation with L-Leu tended to increase the marbling score (P = 0.06) and decrease subcutaneous fat thickness (P = 0.06), as well as the content of C10:0 (P < 0.05), C14:0 (P = 0.05), C20:0 (P < 0.05), and C18:2n-6 t (P = 0.07) in the longissimus thoracis muscle. However, L-Leu significantly increased the crude protein content in the longissimus thoracis muscle (P < 0.05). Correlation analysis revealed that L-Leu downregulated the relative abundance of metabolites associated with subcutaneous fat thickness and beef fatty acid synthesis (P < 0.01), and upregulated the relative abundance of metabolites associated with crude protein and ether extract in the longissimus thoracis muscle (P < 0.01). In conclusion, dietary L-Leu supplementation increases leucine bioavailability and improves meat quality in fattening beef cattle by altering host serum metabolism.

2024-12-01·The Journal of Nutritional Biochemistry

Tryptophan supplements in high-carbohydrate diets by improving insulin response and glucose transport through PI3K-AKT-GLUT2 pathways in blunt snout bream (Megalobrama amblycephala)

Article

作者: Chang, Le ; Jia, Xiaoyan ; Xiao, Kang ; Qiang, Wei ; Zhang, Dingdong ; Liu, Wenbin

The aim of this experiment was to elucidate the metabolic ramifications of tryptophan supplementation in the context of high-carbohydrate diet-feeding, which is important for improving feeding strategies in aquaculture in order to improve fish carbohydrate metabolism. Juvenile blunt snout bream with an initial mean body mass of 55.0±0.5 g were allocated to consume one of three experimental diets: CN, a normal diet with carbohydrate content of 30% (w/w); HC, a diet with high carbohydrate content of 43% (w/w); and HL, a high-carbohydrate diet to which 0.8% L-tryptophan (L-trp) had been added. These diets were fed for 8 weeks, and the effects of the carbohydrate and tryptophan contents of the diets were assessed. Histological analysis using Hematoxylin and Eosin (H&E) and Oil Red O staining revealed that high-carbohydrate intake was associated with abnormal hepatocyte morphology and excessive liver lipid accumulation, which were notably ameliorated by tryptophan supplementation. A significant increase in plasma glucose, glucagon, AGEs (advanced glycation end products), triglycerides, total cholesterol, and a significant decrease in insulin and hepatic glycogen after a high-carbohydrate diet in terms of plasma indices, compared to the control group. Almost all of them were restored to the normal level in the HL group. The present study might preliminarily suggest that tryptophan supplementation ameliorates the imbalance in glucose metabolism of this species induced by a high-carbohydrate diet. Transcriptomics showed that glucose metabolism under high carbohydrate was mainly regulated by the PI3K-AKT signaling pathway. The mRNA expression and protein levels of GLUT2 also varied with this pathway, which would suggest that sustained activation of this pathway with the addition of tryptophan accelerates glucose transport and insulin secretion under high-carbohydrate diet. Subsequent GTT and ITT experiments have also demonstrated that tryptophan improves glucose tolerance and insulin tolerance in blunt snout bream on a high-carbohydrate diet. In conclusion, these findings elucidate the positive regulatory effect of tryptophan on the PI3K-AKT-GLUT2 pathway under a high carbohydrate diet and provide a theoretical basis for the subsequent rational application of high carbohydrate diets in the future.

2024-12-01·Microbiological Research

Chemoreceptor MCP4580 of Vibrio splendidus mediates chemotaxis toward L-glutamic acid contributing to bacterial virulence

Article

作者: Li, Ya ; Zhang, Weiwei ; Shi, Weibo ; Sun, Zihao

Chemotaxis has an essential function in flagellar bacteria that allows them to sense and respond to specific environmental signals, enabling their survival and colonization. Vibrio splendidus is an important opportunistic pathogen that infects a wide range of hosts including fish, bivalve, and sea cucumber. Our study demonstrated that V. splendidus AJ01 exhibited chemotaxis toward L-glutamic acid (L-Glu), an abundant amino acid in the intestinal and respiratory tree tissues of the sea cucumber. Bacterial samples collected from two locations in soft agar swimming plates were subjected to RNA-sequencing (RNA-Seq) analysis to identify the methyl-accepting chemotaxis protein (MCP) respond to L-Glu. Among the 40 annotated chemoreceptors, MCP4580 was identified as the MCP that mediates L-Glu-response. Molecular docking and site-directed mutagenesis revealed that L-arginine at residue 81 (R81) and L-glutamine at residue 88 (Q88) in the ligand-binding domain (LBD) are crucial for L-Glu recognition. Bacterial two-hybrid assay (BTH) showed that MCP4580 forms dimers and interacts with the histidine kinase CheA via the coupling protein CheW1 and CheW2. Phosphorylation analysis showed that the binding of L-Glu to MCP4580 results in the inhibition of CheA phosphorylation mainly via CheW1. Notably, sea cucumbers stimulated with each mutant strain of chemotaxis protein exhibited reduced mortality, highlighting the importance of chemotaxis in V. splendidus virulence. The present study provides valuable insights into the molecular components and signal transduction involved in the chemotaxis of V. splendidus toward L-Glu, and highlights the importance of chemotaxis in its virulence.

100 项与奥谷法奈二钠相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D05235	-	-	DB05779

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
获得性免疫缺陷综合征	临床3期	澳大利亚	Cytran, Inc.	2001-08-31
获得性免疫缺陷综合征	临床3期	加拿大	Cytran, Inc.	2001-08-31
获得性免疫缺陷综合征	临床3期	比利时	Cytran, Inc.	2001-08-31
获得性免疫缺陷综合征	临床3期	美国	Cytran, Inc.	2001-08-31
结直肠癌	临床3期	美国	Implicit Bioscience Ltd.	-
卡波西肉瘤	临床3期	-	Implicit Bioscience Ltd.	-
卡波西肉瘤	临床3期	-	Implicit Bioscience Ltd.	-
卡波西肉瘤	临床3期	-	ALZA Corp.	-
卡波西肉瘤	临床3期	-	ALZA Corp.	-
卵巢癌	临床3期	美国	Implicit Bioscience Ltd.	-

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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


UEGW	N/A	萎缩性胃炎 H. pylori	116	Alpha-glutamyl-tryptophan	齋鹽膚夢鹹膚鬱繭遞糧(夢鏇鬱衊獵壓網糧鑰觸) = decrease of GM edema and hyperemia by endoscopy data, reduction of the number of inflammatory infiltration cells per 1 mm 2 of GM: eosinophilic granulocytes â 3 times, neutrophilic leukocytes â 4 times, macrophages â 1.5 times, lymphocytes â 28.2%, plasmocytes â 29.6% by histological study 築襯積鏇憲簾廠網範夢 (範壓衊壓窪膚鏇製鏇遞 ) 更多	积极	2024-10-13
ASCO2005	临床2期	去势敏感前列腺癌	-	IM862	鬱製鏇願淵願鏇蓋夢廠(壓範觸淵鑰鑰範壓鑰簾) = 網糧糧窪構鬱網膚積範鬱簾廠範膚簾獵顧獵夢 (醖鹹鏇蓋醖選窪積願餘 )	不佳	2005-06-01
ASCO2005	临床2期	去势敏感前列腺癌	-	Placebo	鬱製鏇願淵願鏇蓋夢廠(壓範觸淵鑰鑰範壓鑰簾) = 夢簾鹽艱膚構艱壓齋製鬱簾廠範膚簾獵顧獵夢 (醖鹹鏇蓋醖選窪積願餘 )	不佳	2005-06-01