A Phase IIa Study of the Safety and Clinical Proof-of-concept of NC-503 (Eprodisate Disodium) in Patients With Type II Diabetes and Features of Metabolic Syndrome

The main objectives of the current study are to establish the safety and clinical proof-of-concept of NC-503 in inadequately controlled patients with Type 2 diabetes and features of metabolic syndrome treated with either metformin, a sulfonylurea agent, or metformin in combination with a sulfonylurea agent.

开始日期2008-04-01

申办/合作机构

BELLUS Health, Inc.

100 项与伊罗地塞相关的临床结果

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100 项与伊罗地塞相关的转化医学

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100 项与伊罗地塞相关的专利（医药）

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项与伊罗地塞相关的文献（医药）

2023-01-31·ACS omega

Cyclohexane-1,3-dione Derivatives as Future Therapeutic Agents for NSCLC: QSAR Modeling, In Silico ADME-Tox Properties, and Structure-Based Drug Designing Approach

Article

作者: Elkhattabi, Souad ; Shaik, Afzal B. ; Bakhouch, Mohamed ; Chtita, Samir ; Belaidi, Salah ; Daoui, Ossama ; Bhandare, Richie R. ; Mali, Suraj N.

The abnormal expression of the c-Met tyrosine kinase has been linked to the proliferation of several human cancer cell lines, including non-small-cell lung cancer (NSCLC). In this context, the identification of new c-Met inhibitors based on heterocyclic small molecules could pave the way for the development of a new cancer therapeutic pathway. Using multiple linear regression (MLR)-quantitative structure-activity relationship (QSAR) and artificial neural network (ANN)-QSAR modeling techniques, we look at the quantitative relationship between the biological inhibitory activity of 40 small molecules derived from cyclohexane-1,3-dione and their topological, physicochemical, and electronic properties against NSCLC cells. In this regard, screening methods based on QSAR modeling with density-functional theory (DFT) computations, in silico pharmacokinetic/pharmacodynamic (ADME-Tox) modeling, and molecular docking with molecular electrostatic potential (MEP) and molecular mechanics-generalized Born surface area (MM-GBSA) computations were used. Using physicochemical (stretch-bend, hydrogen bond acceptor, Connolly molecular area, polar surface area, total connectivity) and electronic (total energy, highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) energy levels) molecular descriptors, compound 6d is identified as the optimal scaffold for drug design based on in silico screening tests. The computer-aided modeling developed in this study allowed us to design, optimize, and screen a new class of 36 small molecules based on cyclohexane-1,3-dione as potential c-Met inhibitors against NSCLC cell growth. The in silico rational drug design approach used in this study led to the identification of nine lead compounds for NSCLC therapy via c-Met protein targeting. Finally, the findings are validated using a 100 ns series of molecular dynamics simulations in an aqueous environment on c-Met free and complexed with samples of the proposed lead compounds and Foretinib drug.

2023-01-01·The Journal of pharmacology and experimental therapeutics

Transport of the Proinflammatory Chemokines C-C Motif Chemokine Ligand 2 (MCP-1) and C-C Motif Chemokine Ligand 5 (RANTES) across the Intact Mouse Blood-Brain Barrier Is Inhibited by Heparin and Eprodisate and Increased with Systemic Inflammation

Article

作者: Omer, Mohamed ; Williams, Lindsey M ; Fujimoto, Takashi ; Quaranta, Daniel V ; Reed, May J ; Weaver, Riley R ; Banks, William A ; Erickson, Michelle A ; Baumann, Kristen K ; Kim, Hyung Chan ; Logsdon, Aric F

One important function of the vascular blood-brain barrier (BBB) is to facilitate neuroimmune communication. The BBB fulfills this function, in part, through its ability to transport cytokines and chemokines. C-C motif chemokine receptor 2 (CCL2) (MCP-1) and C-C motif chemokine receptor 5 (CCL5) (RANTES) are proinflammatory chemokines that mediate neuroimmune responses to acute insults and aspects of brain injury and neurodegenerative diseases; however, a blood-to-brain transport system has not been evaluated for either chemokine in vivo. Therefore, we determined whether CCL2 and CCL5 in blood can cross the intact BBB and enter the brain. Using CD-1 mice, we found that ¹²⁵I-labeled CCL2 and CCL5 crossed the BBB and entered the brain parenchyma. We next aimed to identify the mechanisms of ¹²⁵I-CCL2 and ¹²⁵I-CCL5 transport in an in situ brain perfusion model. We found that both heparin and eprodisate inhibited brain uptake of ¹²⁵I-CCL2 and ¹²⁵I-CCL5 in situ, whereas antagonists of their receptors, CCR2 or CCR5, respectively, did not, suggesting that heparan sulfates at the endothelial surface mediate BBB transport. Finally, we showed that CCL2 and CCL5 transport across the BBB increased following a single injection of 0.3 mg/kg lipopolysaccharide. These data demonstrate that CCL2 and CCL5 in the brain can derive, in part, from the circulation, especially during systemic inflammation. Further, binding to the BBB-associated heparan sulfate is a mechanism by which both chemokines can cross the intact BBB, highlighting a novel therapeutic target for treating neuroinflammation. SIGNIFICANCE STATEMENT: Our work demonstrates that C-C motif chemokine ligand 2 (CCL2) and C-C motif chemokine ligand 5 (CCL5) can cross the intact blood-brain barrier and that transport is robustly increased during inflammation. These data suggest that circulating CCL2 and CCL5 can contribute to brain levels of each chemokine. We further show that the transport of both chemokines is inhibited by heparin and eprodisate, suggesting that CCL2/CCL5-heparan sulfate interactions could be therapeutically targeted to limit accumulation of these chemokines in the brain.

2020-10-01·Toxicology letters2区 · 医学

In vitro and in vivo assessment of the genotoxic effects of ceric ammonium nitrate and 1,3-propane sultone

2区 · 医学

Article

作者: Kim, Ji-Young ; Moon, Kyoung-Sik ; Lee, A-Ram ; Kim, Sang Kyum ; Choi, Young Jae ; Back, Sen-Min ; Kim, Ok-Hee

A variety of methods have been developed for accurate and systematic evaluation of chemical genotoxicity. Ceric ammonium nitrate (CAN) and 1,3-propane sultone (1,3-PS) have been extensively applied in industrial fields. Although 1,3-PS, but not CAN, has been reported as a potent carcinogen, systematic assessment of the genotoxic properties of these chemicals has not been conducted. The purpose of this study was to establish a decision tree for evaluating genotoxicity based on the good laboratory practices (GLP) system using 1,3-PS and CAN as test chemicals. In vitro studies were performed including the bacterial reverse mutation assay, chromosomal aberration assay, and micronucleus assay. We conducted in vivo studies using a combined micronucleus and alkaline comet (MN-CMT) assay and the Pig-a gene mutation assay, which is a promising method for detecting gene mutations in vivo. CAN showed negative responses in all in vitro genotoxicity assays and the in vivo combined MN-CMT assay. Meanwhile, 1,3-PS had positive results in all in vitro and in vivo genotoxicity assays. In this study, we confirmed the genotoxicity of 1,3-PS and CAN using both in vitro and in vivo assays. We propose a decision tree for evaluating chemical-induced genotoxicity.

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2021-07-09

·GlobeNewswire

Sarcoidosis Drug Market Global Sales are Expected to Grow

PUNE, India, July 09, 2021 (GLOBE NEWSWIRE) -- The Global Sarcoidosis Drug Market Share, Trends, Analysis and Forecasts, 2021-2031 provides insights on key developments, business strategies, research & development activities, supply chain analysis, competitive landscape, and market composition analysis. Sarcoidosis is an uncommon condition that causes little granulomas in the different organs of the body. It typically influences the lungs and skin. The etiology of the sickness is not yet understood which makes the diagnosis about sarcoidosis vital. The expansion in the number of associations and foundations that provides knowledge about sarcoidosis among individuals is rising and is relied upon to drive the development of the worldwide sarcoidosis therapeutics market during the forecast period of 2021-2031. The reason for this sickness is yet unidentified, and it is acknowledged that it results from the body's immune system reacting to an obscure substance. Therapy of sarcoidosis begins by controlling the outset of granuloma evolution by suppressing antigen manipulation, foreclosing fibrosis processes, restricting torrid traumas causing organ resistance, serious persistent tiredness, repressing recognized signs like coughing along with exertional dyspnea. View the Entire report with Table of Contents: Growth driving factors of Sarcoidosis Drug Market Drug manufacturing organizations are collaborating for the advancement of prescription ethical medicine for the therapeutics of sarcoidosis. These unions are looking forward to improving the Research and development exercises of new drugs for the administration of sarcoidosis and will assist governances with inventing drugs for accurate and effective treatment. In this manner, such essential agreements are required to assist the worldwide sarcoidosis therapeutics market to evolve. The amount of clinical explorative attempts undertaken for sarcoidosis has boomed since past certain years. The disorder can be profoundly undetected for longer period and thus offers a potential for industry players to fortify their market proximity. A few organizations, namely, Auven Therapeutics have sustained rights from research colleges to additional complete clinical explorative attempts on better treatment option. Auven Therapeutics acquired rights to further surrogate KIACTA from the Icahn Institute of Medication. The exploration is presently fetched as a cooperative exertion between Auven Therapeutics and BELLUS Welfare. Access Sample Pages of this Report: The organizations are assessing the expected utilization of KIACTA for the treatment of patients experiencing pneumonic sarcoidosis. They have fostered a Phase2/3 group meeting to assess the practicality and security of KIACTA in sarcoidosis. The leading market segments of Global Sarcoidosis Drug Market Region wise, sarcoidosis therapeutics market is segmented into regions namely North America, South America, Europe, Asia Pacific, and Middle East & Africa. North America area is projected to rule the sarcoidosis therapeutics market over the forecast period 2021- 2031. Related report: Global Clear Aligners Market: Global Blood Transfusion Diagnostics Market: Global Phoropters Market: The advanced Sarcoidosis Drug segment is believed upon to lead the worldwide Sarcoidosis Drug market over the forecast period. By end client use, Lung treatment providing facilities are relied upon to contribute a high share in the worldwide Sarcoidosis Drug market attributable to their availability along with the significant amount of patients being prescribed to further continue their treatments in these, respiratory treatment providing centers. Specialty clinics are relied upon to notice consistent improvement in the acceptance of Sarcoidosis Drug, resulting from the expanding number of eye issues registered worldwide. Europe is the second-biggest region as far as income share is considered as it likewise has the number of clinical studies come along. Asia Pacific is expected to be the quickest developing region for the sarcoidosis therapeutics drug market. The area is relied upon to boom attributable to the normalcy rate and awards got from different global affiliations. An educator from Public Jewish health, gotten USD 40,000 for each two-year long time from the Establishment for Sarcoidosis Exploration (FSR) award/American Thoracic Society. The Sarcoidosis Drug market in Asia Pacific excluding Japan is required to develop at a critical CAGR because of the expansion of contributions by central players. Europe is expected to have the second-biggest share in the worldwide Sarcoidosis Drug market all through the forecast period. Buy This Report: The key players of the Global Sarcoidosis Drug Market are: Relief therapeutics holding SA, Firststring research, Bellus health, Araim Pharmaceuticals, Inc. Merck & Co., Inc, Novartis AG, PharmaIN, Corp, Adaptimmune Therapeutics plc, Epizyme, Inc, Advenchen Laboratories, LLC, Fresenius Umwelttechnik GmbH, Horizon Therapeutics plc, Johnson & Johnson Services, Inc, Pfizer Inc, Mallinckrodt LLC and others. Global Sarcoidosis Drug Market Key Segments: By Type By Mechanism of Action Type By Drug Type Stages Type By Route of Administration By End users By Region insightSLICE is a market intelligence and strategy consulting company. The company provides tailor-made and off the shelf market research studies. The prime focus of the company is on strategy consulting to provide end-to-end solutions. For more details, please contact our research and consulting team at info@insightslice.com. Contact Us: Alex, insightSLICE Phone (USA): +1 707 736 6633 Email address: alex@insightslice.com Web:

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KEGG	Wiki	ATC	Drug Bank
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适应症	最高研发状态	国家/地区	公司	日期
2型糖尿病	临床2期	加拿大	BELLUS Health, Inc.	2008-04-01
代谢综合征	临床2期	加拿大	BELLUS Health, Inc.	2008-04-01

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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


EFAAT (EULAR2007)	N/A	继发性淀粉样变性	183	Eprodisate	願淵鏇製夢襯顧壓夢築(憲衊廠襯餘選餘壓構鏇) = 壓衊襯糧範憲網淵憲顧蓋齋鹽衊齋製網醖淵鏇 (構網鑰鏇獵築膚齋鏇衊 )	积极	2007-06-13
				Placebo	願淵鏇製夢襯顧壓夢築(憲衊廠襯餘選餘壓構鏇) = 艱觸網選鬱鹽積簾願繭蓋齋鹽衊齋製網醖淵鏇 (構網鑰鏇獵築膚齋鏇衊 )