Delving into the Latest Updates on Oglufanide disodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Glufanide disodium, Glutamyltryptophan, L-Glu-L-Trp

+ [9]

Target-

Mechanism

Angiogenesis inhibitors, Immunomodulators

Therapeutic Areas

NeoplasmsImmune System DiseasesInfectious Diseases+ [5]

Active Indication-

Inactive Indication

Acquired Immunodeficiency SyndromeBacterial InfectionsColorectal Cancer+ [5]

Originator Organization

ALZA Corp.

Active Organization-

Inactive Organization

Cytran, Inc.

Implicit Bioscience Ltd.

ALZA Corp.

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC16H19N3NaO5

InChIKeyUOKXDTZUCQYLHK-JZKFLRDJSA-N

CAS Registry237068-57-4

View All Structures (2)

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.

Start Date01 Jan 2001

Sponsor / Collaborator

Cytran, Inc.

NCT00006037 / TerminatedPhase 2IIT

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.

Start Date01 Nov 1999

Sponsor / Collaborator

University of Southern California

[+1]

100 Clinical Results associated with Oglufanide disodium

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100 Translational Medicine associated with Oglufanide disodium

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100 Patents (Medical) associated with Oglufanide disodium

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1,507

Literatures (Medical) associated with Oglufanide disodium

01 Feb 2025·Meat Science

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

Article

Author: 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.

01 Dec 2024·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

Author: 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.

01 Dec 2024·Microbiological Research

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

Article

Author: 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 Deals associated with Oglufanide disodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D05235	-	-	DB05779

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acquired Immunodeficiency Syndrome	Phase 3	AU	Cytran, Inc.	31 Aug 2001
Acquired Immunodeficiency Syndrome	Phase 3	CA	Cytran, Inc.	31 Aug 2001
Acquired Immunodeficiency Syndrome	Phase 3	BE	Cytran, Inc.	31 Aug 2001
Acquired Immunodeficiency Syndrome	Phase 3	US	Cytran, Inc.	31 Aug 2001
Colorectal Cancer	Phase 3	US	Implicit Bioscience Ltd.	-
Kaposi Sarcoma	Phase 3	-	Implicit Bioscience Ltd.	-
Kaposi Sarcoma	Phase 3	-	Implicit Bioscience Ltd.	-
Kaposi Sarcoma	Phase 3	-	ALZA Corp.	-
Kaposi Sarcoma	Phase 3	-	ALZA Corp.	-
Ovarian Cancer	Phase 3	US	Implicit Bioscience Ltd.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


UEGW	Not Applicable	Gastritis, Atrophic H. pylori	116	Alpha-glutamyl-tryptophan	kdfvdfpvdj(fbcwyfiyuc) = 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 xajjbnylzs (kjrvnljrhi ) View more	Positive	13 Oct 2024
ASCO2005	Phase 2	Castration-sensitive prostate cancer	-	IM862	zjivvduqtj(zeviugufqw) = sldsutenbg qcuqojieff (pfkjaziuxj )	Negative	01 Jun 2005
ASCO2005	Phase 2	Castration-sensitive prostate cancer	-	Placebo	zjivvduqtj(zeviugufqw) = ccjhcybbhw qcuqojieff (pfkjaziuxj )	Negative	01 Jun 2005