A Phase II Prospective, Randomized, Double-Masked, Parallel-Group, Multi-centered Study Assessing the Safety and Efficacy of Two Concentrations of DE-101 Ophthalmic Suspension Compared to Placebo for the Treatment of Dry Eye Disease

To investigate the safety and efficacy of DE-101 to improve the signs and symptoms in dry-eye disease.

开始日期2011-10-01

申办/合作机构

Santen Pharmaceutical Co., Ltd.

NCT01118754 / Completed临床1/2期

Phase I/II Prospective, Randomized, Double Masked, Parallel-Group, Multi-centered Study Assessing the Safety and Efficacy of Two Concentrations of DE-101 Compared to Placebo for the Treatment of Dry Eye Disease

The purpose of this study is to evaluate if DE-101 ophthalmic suspension will safely and effectively improve signs and or symptoms of dry eye disease.

开始日期2010-04-01

申办/合作机构

Santen Pharmaceutical Co., Ltd.

NCT00571519 / Terminated临床3期

A Randomized, Double-blind, Placebo, and Active Comparator-controlled, Parallel-group Study of the Efficacy and Safety of Rivoglitazone as Monotherapy Treatment of Type 2 Diabetes Mellitus

This is a 26-week, multicenter, randomized, double-blind, placebo and active comparator-controlled, parallel-group study in participants with type 2 diabetes currently sub-optimally controlled by diet and exercise or with non-thiazolidinedione antihyperglycemic monotherapy. Pioglitazone is used as active comparator. The total duration of a participant's participation will be approximately 30 weeks, including a 2-week placebo lead-in period, a 26-week double-blind treatment period, and a 2-week post-treatment follow-up period. Participants who complete the randomized portion of the study per protocol may have the opportunity to continue in a long-term extension study of active treatments.

开始日期2007-11-14

申办/合作机构

Daiichi Sankyo Co., Ltd.

100 项与利格列酮相关的临床结果

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100 项与利格列酮相关的转化医学

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100 项与利格列酮相关的专利（医药）

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项与利格列酮相关的文献（医药）

2022-09-01·Animal : an international journal of animal bioscience

The amino acid profile of Camelina sativa seeds correlates with the strongest immune response in dairy ewes

Article

作者: Tedeschi, T ; Christodoulou, C ; Sforza, S ; Mavrommatis, A ; Prandi, B ; Tsiplakou, E ; Simoni, M ; Righi, F

Camelina sativa is an alternative protein source (with a specific amino acid profile) rich also in bioactive compounds (such as polyunsaturated fatty acids and antioxidants), which have immunomodulatory properties. This study aimed to assess the impact of the dietary inclusion level of Camelina seeds, on the expression levels of key genes involved in ewes' innate immunity. Forty-eight dairy ewes were assigned into four homogenous groups of 12 animals that were fed individually with alfalfa hay, wheat straw, and concentrate. The concentrate of the control group (CON) had no Camelina seeds, while in the treated groups, Camelina seeds (CSs) were incorporated at 6 (CS6), 11 (CS11), and 16% (CS16) in the concentrates, respectively, as partial substitution of both soybean meal and maize grain. The relative transcript levels of the immune-related genes were determined using a real-time PCR platform. The relative transcript levels of toll-interleukin receptor-domain-containing adapter-inducing interferon-β, tumour necrosis factor receptor-associated factor 3, Interferon regulatory factor 5, and Mitogen-activated protein kinase were upregulated in monocytes of the CS11-fed ewes. Furthermore, in the CS6-fed ewes, the relative transcript levels of Interleukin-1 beta (IL1B) were upregulated in monocytes compared to the CON, while those of IL1B, Interleukin-8, and Interleukin-10 were upregulated in neutrophils compared to the CON and the CS11-fed ewes. The highest inclusion level of CS (CS16) did not have a negative impact on ewes' innate immunity. The response of monocytes on dietary amino acid (mainly threonine, tyrosine, serine, and lysine) changes related to Camelina inclusion is different from that of neutrophils. The observed responses need to be further investigated.

2019-10-01·Medical hypotheses4区 · 医学

Possible role of rivoglitazone thiazolidine class of drug as dual-target therapeutic agent for bacterial infections: An in silico study

4区 · 医学

Article

作者: Md, Afzal Azam ; Yele, Vidyasrilekha ; Saha, Niladri

Infections due to resistant bacteria are the life-threatening and leading cause of mortality worldwide. The current therapy for bacterial infections includes treatment with various drugs and antibiotics. The misuse and over usage of these antibiotics leads to bacterial resistance. There are several mechanisms by which bacteria exhibit resistance to some antibiotics. These include drug inactivation or modification, elimination of antibiotics through efflux pumps, drug target alteration, and modification of metabolic pathway. However, it is difficult to treat infections caused by resistant bacteria by conventional existing therapy. In the present study binding affinities of some glitazones against ParE and MurE bacterial enzymes are investigated by in silico methods. As evident by extra-precision docking and binding free energy calculation (MM-GBSA) results, rivoglitazone exhibited higher binding affinity against both ParE and MurE enzymes compared to all other selected compounds. Further molecular dynamic (MD) simulations were performed to validate the stability of rivoglitazone/4MOT and rivoglitazone/4C13 complexes and to get insight into the binding mode of inhibitor. Thus, we hypothesize that structural modifications of the rivoglitazone scaffold can be useful for the development of an effective antibacterial agent.

2017-08-01·Biochimica et biophysica acta. General subjects3区 · 生物学

X-ray crystal structure of rivoglitazone bound to PPARγ and PPAR subtype selectivity of TZDs

3区 · 生物学

Article

作者: Rajapaksha, Harinda ; Bhatia, Harpreet ; Petrovsky, Nikolai ; Wegener, Kate ; Bruning, John B

Thiazolidinedione (TZD) compounds targeting the nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) demonstrate unique benefits for the treatment of insulin resistance and type II diabetes. TZDs include rosiglitazone, pioglitazone and rivoglitazone, with the latter being the most potent. The TZDs are only marginally selective for the therapeutic target PPARγ as they also activate PPARα and PPARδ homologues to varying degrees, causing off-target effects. While crystal structures for TZD compounds in complex with PPARγ are available, minimal structural information is available for TZDs bound to PPARα and PPARδ. This paucity of structural information has hampered the determination of precise structural mechanisms involved in TZD selectivity between PPARs. To help address these questions molecular dynamic simulations were performed of rosiglitazone, pioglitazone and rivoglitazone in complex with PPARα, PPARδ, and PPARγ in order to better understand the mechanisms of PPAR selectivity. The simulations revealed that TZD interactions with residues Tyr314 and Phe318 of PPARα and residues Phe291 and Thr253 of PPARδ as well as the omega loop, are key determinants of TZD receptor selectivity. Notably, in this study, we solve the first X-ray crystal structure of rivoglitazone bound to any PPAR. Rivoglitazone forms a unique hydrogen bond network with the residues of the PPARγ co-activator binding surface (known as AF2) and makes more extensive contacts with helix 3 and the β-sheet as compared to model TZD compounds such as rosiglitazone.

项与利格列酮相关的新闻（医药）

2024-09-12

·GlobeNewswire-Health Care

Elevar Therapeutics Reports Advances in HCC and Other Oncology Clinical Programs for Rivoceranib Plus Camrelizumab at the European Society for Medical Oncology Congress 2024

FORT LEE, N.J., Sept. 12, 2024 (GLOBE NEWSWIRE) -- Elevar Therapeutics, Inc., a majority-owned subsidiary of HLB Co., Ltd., today announced the presentation of three posters at the European Society for Medical Oncology (ESMO) Congress 2024 in Barcelona, Spain, Sept. 13-17. “The results to be presented at ESMO continue to support the safety and efficacy of rivoceranib in combination with camrelizumab as a first-line systemic treatment option for patients with hepatocellular carcinoma; as well as the potential of combining rivoceranib with other immune checkpoint inhibitors as a therapeutic option for many types of solid tumors,” commented Chris Galloway, M.D., senior vice president of clinical and medical affairs at Elevar Therapeutics. Camrelizumab and rivoceranib were granted Orphan Drug Designation by the U.S. Food and Drug Administration and the European Medical Association. ESMO Presentation 985P (Abstract 5451): Analysis of antidrug antibodies (ADA) to camrelizumab in CARES-310: The pivotal phase III study of camrelizumab + rivoceranib in unresectable hepatocellular carcinoma (uHCC) The poster reports an analysis of antidrug antibodies (ADAs) in the CARES-310 (NCT03764293) Phase 3 clinical study for the treatment of unresectable hepatocellular carcinoma (uHCC). There was minimal impact of ADAs on PK, efficacy and safety. Therefore, follow-up monitoring of ADAs to cam is not warranted. CARES-310 was the first trial to demonstrate significant progression-free survival (PFS) and overall survival benefits with immunotherapy plus an anti-angiogenic tyrosine kinase inhibitor (TKI) over standard TKI as a first-line treatment for uHCC. Speaker: Ahmed O. Kaseb (Houston, United States of America)Onsite poster display date: Mon., Sept. 16Link to Abstract 5451 / Presentation 985P ESMO Presentation 963P (Abstract 5635): Quality-adjusted time without symptoms or toxicity (Q-TWiST) analysis to assess the impact of treatment with camrelizumab + rivoceranib (cam+rivo) on quality-of-life vs sorafenib (sora) in patients (pts) with unresectable hepatocellular carcinoma (uHCC): Study CARES-310 The poster reports results from Phase 3 CARES-310 study, concluding cam + rivo had clinically meaningful quality-adjusted survival benefits over sorafenib. The higher incidence of adverse effects in patients treated with cam + rivo was likely due to longer time on treatment versus sorafenib. Speaker: Andrew Moon (Chapel Hill, United States of America)Onsite poster display date: Mon., Sept. 16Link to Abstract 5635 / Presentation 963P ESMO Presentation 1013P (Abstract 2318): A phase I study of rivoceranib combined with nivolumab in patients with unresectable or metastatic cancer The poster reports results from Phase 1 (NCT03396211) clinical study of rivoceranib plus nivolumab (rivo + nivo) in patients with advanced metastatic solid tumors. The study concluded that rivo + nivo demonstrated a manageable safety profile and promising antitumor efficacy across many solid tumors as measured by reduction in tumor burden over time. Further studies are needed to confirm the safety and efficacy of rivo + nivo therapy. Speaker: Neal S. Chawla (Duarte, United States of America)Onsite poster display date: Sat., Sept. 14Link to Abstract 2318 / Presentation 1013P About Hepatocellular Carcinoma More than 800,000 people worldwide are diagnosed with liver cancer each year. Liver cancer is a leading cause of cancer accounting for more than 700,000 deaths annually.[i] Hepatocellular Carcinoma (HCC) is the most common type of primary liver cancer. It most frequently develops in people with chronic underlying liver inflammation which may be from viral and non-viral causes. HCC typically has a poor prognosis with limited treatment options and continues to be a diagnosis with an ongoing urgent medical need. About Rivoceranib Rivoceranib, a small-molecule tyrosine kinase inhibitor (TKI), is a highly potent inhibitor of vascular endothelial growth factor receptor (VEGFR), a primary pathway for tumor angiogenesis. VEGFR inhibition is a clinically validated target to limit tumor growth and disease progression. Rivoceranib is currently being studied as a monotherapy and in combination with chemotherapy and immunotherapy in various solid tumor indications. Ongoing clinical studies include uHCC (in combination with camrelizumab), gastric cancer (as a monotherapy and in combination with paclitaxel), adenoid cystic carcinoma (as a monotherapy) and colorectal cancer (in combination with Lonsurf®). Rivoceranib was the first TKI approved in gastric cancer in China (November 2014). It is also approved in China in combination with camrelizumab as a first-line treatment for uHCC (January 2023). The drug has been studied in more than 6,000 patients worldwide and was well tolerated in clinical trials with a comparable safety profile to other TKIs and VEGF inhibitors. Orphan drug designations have been granted in gastric cancer (U.S., EU and South Korea), in adenoid cystic carcinoma (U.S.) and in uHCC (U.S. and EU). Elevar Therapeutics, Inc. holds the global rights (excluding China) to rivoceranib and has partnered for its development and marketing with HLB-LS in South Korea. Rivoceranib, under the name apatinib, is also approved in China for advanced gastric cancer and in second-line advanced HCC by the Chinese -territory license-holder, Jiangsu Hengrui Pharmaceuticals Company Ltd., (Hengrui Pharma), under the brand name Aitan®. About Camrelizumab Camrelizumab (SHR-1210) is a humanized monoclonal antibody that binds to the programmed death-1 (PD-1) receptor. Blockade of the PD-1/PD-L1 signaling pathway is a therapeutic strategy showing success in a wide variety of solid and hematological cancers. Camrelizumab is developed by Hengrui Pharma and has been studied in more than 5,000 patients. Currently, 50 clinical trials are underway in a broad range of tumors (including liver cancer, lung cancer, gastric cancer, and breast cancer, etc.) and treatment settings. Camrelizumab, under the brand name AiRuiKa®, is currently approved for eight indications in China, including monotherapy for the treatment of HCC (second-line), in combination with rivoceranib as a treatment for uHCC (first-line), relapsed/refractory classic Hodgkin’s lymphoma (third-line), esophageal squamous cell carcinoma (second-line) and nasopharyngeal carcinoma (third-line or further) and in combination with chemotherapy for the treatment of non-small cell lung cancer (non-squamous and squamous), esophageal squamous cell carcinoma and nasopharyngeal carcinoma in the first-line setting. The U.S. Food and Drug Administration granted Orphan Drug Designation to camrelizumab for advanced HCC in April 2021 and by the EMA in August 2024. In October 2023, Elevar licensed camrelizumab, an anti-PD-1 antibody, for commercialization from Jiangsu Hengrui Pharmaceuticals Co., Ltd. (Hengrui Pharma) worldwide excluding Greater China and Korea. Media Contact Jeanette Bressi Head, Corporate Communications, Elevar Therapeutics jbressi@elevartherapeutics.com609-439-3997 Investor Relations Contact Wade SmithChief Financial & Business Officer, Elevar Therapeuticswsmith@elevartherapeutics.com [i] Key Statistics About Liver Cancer | American Cancer Society

临床结果免疫疗法临床3期孤儿药临床1期

100 项与利格列酮相关的药物交易

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KEGG	Wiki	ATC	Drug Bank
-	利格列酮	-	DB09200

研发状态

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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3期	波多黎各	Daiichi Sankyo Co., Ltd.	2007-04-01
DED	临床2期	美国	Santen Pharmaceutical Co., Ltd.	2011-10-01

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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


NCT00484198 (CTgov)	临床3期	2型糖尿病	1,912	placebo+Rivoglitazone+Pioglitazone (Placebo)	夢獵淵蓋糧蓋廠獵襯夢(觸蓋窪製壓憲壓觸憲構) = 餘觸願鬱築鹽艱衊鬱鏇蓋鏇獵鑰鏇鑰製選壓選 (鬱衊夢艱糧遞遞衊糧襯, 夢顧構築窪積糧觸遞遞 ~ 衊艱鹽鹹簾構糧選餘鬱) 更多	-	2021-07-27
				Rivoglitazone (Rivoglitazone 1.0 mg)	夢獵淵蓋糧蓋廠獵襯夢(觸蓋窪製壓憲壓觸憲構) = 窪範繭鑰簾蓋壓網選獵蓋鏇獵鑰鏇鑰製選壓選 (鬱衊夢艱糧遞遞衊糧襯, 鬱憲鹽願衊襯簾積簾築 ~ 憲構構鬱繭夢壓簾廠鑰) 更多
NCT00571519 (CTgov)	临床3期	2型糖尿病	94	placebo+Rivoglitazone+Pioglitazone (Placebo)	觸鹽餘廠鬱艱築範範糧(衊淵築築網膚構艱夢鏇) = 艱壓積壓獵糧鹽醖壓壓鬱餘築襯簾積廠選廠淵 (襯壓築網鏇遞遞鏇觸製, 獵積蓋襯簾鹹蓋獵築鹹 ~ 觸鹹餘繭築鏇鹽窪襯鏇) 更多	-	2021-02-26
				Rivoglitazone (Rivoglitazone 0.5mg)	觸鹽餘廠鬱艱築範範糧(衊淵築築網膚構艱夢鏇) = 鏇願簾製鏇憲鹽繭顧繭鬱餘築襯簾積廠選廠淵 (襯壓築網鏇遞遞鏇觸製, 餘膚淵顧蓋鏇醖夢選鏇 ~ 獵顧膚築夢鏇選範構鹽) 更多