牛磺脱氧胆酸钠(Shaperon Co., Ltd.)(Sodium taurodeoxycholic acid(Shaperon Co., Ltd.)) - 药物靶点：TGR5_在研适应症：特应性皮炎_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Taurodeoxycholic acid

靶点

TGR5

作用机制

TGR5激动剂(G蛋白偶联胆汁酸受体1激动剂)

治疗领域

免疫系统疾病遗传病与畸形皮肤和肌肉骨骼疾病

在研适应症

非在研适应症

原研机构

在研机构

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C26H45NO6S

InChIKeyAWDRATDZQPNJFN-VAYUFCLWSA-N

CAS号516-50-7

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关联

4

项与牛磺脱氧胆酸钠(Shaperon Co., Ltd.) 相关的临床试验

NCT06024499 / Recruiting临床2期

A Randomized, Double-blind, Placebo-controlled, Multicenter, Phase 2 Study to Evaluate the Efficacy and Safety of HY209 Gel in Patients With Mild to Moderate Atopic Dermatitis(AD)

This is a randomized, double-blind, placebo-controlled, multi-center, phase 2 study in patients with mild to moderate Atopic Dermatitis(AD), which consists of 2 parts.

开始日期2024-03-01

申办/合作机构

Shaperon, Inc.

NCT04530643 / Completed临床2期

A Randomized, Double-blinded, Placebo-controlled, Parallel, Multi-Center Phase II Clinical Study to Evaluate the Efficacy and Safety of HY209 Gel for Patients With Atopic Dermatitis

A Randomized, Double-blinded, Placebo-controlled, Parallel, Multi-Center Phase II Clinical Study to Evaluate the Efficacy and Safety of HY209 gel for Patients with Atopic Dermatitis

开始日期2020-08-26

申办/合作机构

Shaperon, Inc.

NCT04255979 / Completed临床1期

A Randomized, Double-blind, Placebo-controlled Single Dosing, Dose Escalation Phase I Clinical Trial to Investigate the Safety/Tolerability and Pharmacokinetics of HY209 After Intravenous Administration in Healthy Male Volunteers

A randomized, double-blind, placebo-controlled single dosing, dose escalation phase I clinical trial to investigate the safety/tolerability and pharmacokinetics of HY209 after intravenous administration in healthy male volunteers

开始日期2019-12-05

申办/合作机构

Shaperon, Inc.

100 项与牛磺脱氧胆酸钠(Shaperon Co., Ltd.) 相关的临床结果

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100 项与牛磺脱氧胆酸钠(Shaperon Co., Ltd.) 相关的转化医学

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100 项与牛磺脱氧胆酸钠(Shaperon Co., Ltd.) 相关的专利（医药）

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200

项与牛磺脱氧胆酸钠(Shaperon Co., Ltd.) 相关的文献（医药）

2024-05-01·Journal of Controlled Release

Tumor-targeted and stimulus-responsive polymeric prodrug nanoparticles to enhance the anticancer therapeutic efficacy of doxorubicin

Article

作者: Lee, Dongwon ; Kwon, Gayoung ; Song, Nanhee ; Jo, Hanui ; Kwon, Soonyoung ; Park, Sangjun ; Kim, Chunho ; Kim, Nuri

Polymeric prodrug nanoparticles have gained increasing attention in the field of anticancer drug delivery because of their dual functions as a drug carrier and a therapeutic agent. Doxorubicin (DOX) is a highly effective chemotherapeutic agent for various cancers but causes cardiotoxicity. In this work, we developed polymeric prodrug (pHU) nanoparticles that serve as both a drug carrier of DOX and a therapeutic agent. The composition of pHU includes antiangiogenic hydroxybenzyl alcohol (HBA) and ursodeoxycholic acid (UDCA), covalently incorporated through hydrogen peroxide (H₂O₂)-responsive peroxalate. To enhance cancer cell specificity, pHU nanoparticles were surface decorated with taurodeoxycholic acid (TUDCA) to facilitate p-selectin-mediated cancer targeting. TUDCA-coated and DOX-loaded pHU nanoparticles (t-pHUDs) exhibited controlled release of DOX triggered by H₂O₂, characteristic of the tumor microenvironment. t-pHUDs also effectively suppressed cancer cell migration and vascular endothelial growth factor (VEGF) expression in response to H₂O₂. In animal studies, t-pHUDs exhibited highly potent anticancer activity. Notably, t-pHUDs, with their ability to accumulate preferentially in tumors due to the p-selectin targeting, surpassed the therapeutic efficacy of equivalent DOX and pHU nanoparticles alone. What is more, t-pHUDs significantly suppressed VEGF expression in tumors and mitigated hepato- and cardiotoxicity of DOX. Given their cancer targeting ability, enhanced therapeutic efficacy and minimized off-target toxicity, t-pHUDs present an innovative and targeted approach with great translational potential as an anticancer therapeutic agent.

2024-04-16·mSystems

Alterations in the gut microbiota and its metabolites contribute to metabolic maladaptation in dairy cows during the development of hyperketonemia

Article

作者: Wu, Dan ; Wang, Baoning ; Shen, Liuhong ; Huang, Yixin ; Yong, Kang ; Luo, Zhengzhong ; Yao, Xueping ; Cao, Suizhong ; Yu, Shumin ; Zhou, Tao ; Du, Zhenlong

ABSTRACT Metabolic maladaptation in dairy cows after calving can lead to long-term elevation of ketones, such as β-hydroxybutyrate (BHB), representing the condition known as hyperketonemia, which greatly influences the health and production performance of cows during the lactation period. Although the gut microbiota is known to alter in dairy cows with hyperketonemia, the association of microbial metabolites with development of hyperketonemia remains unknown. In this study, we performed a multi-omics analysis to investigate the associations between fecal microbial community, fecal/plasma metabolites, and serum markers in hyperketonemic dairy cows during the transition period. Dynamic changes in the abundance of the phyla Verrucomicrobiota and Proteobacteria were detected in the gut microbiota of dairy cows, representing an adaptation to enhanced lipolysis and abnormal glucose metabolism after calving. Random forest and univariate analyses indicated that Frisingicoccus is a key bacterial genus in the gut of cows during the development of hyperketonemia, and its abundance was positively correlated with circulating branched-chain amino acid levels and the ketogenesis pathway. Taurodeoxycholic acid, belonging to the microbial metabolite, was strongly correlated with an increase in blood BHB level, and the levels of other secondary bile acid in the feces and plasma were altered in dairy cows prior to the diagnosis of hyperketonemia, which link the gut microbiota and hyperketonemia. Our results suggest that alterations in the gut microbiota and its metabolites contribute to excessive lipolysis and insulin insensitivity during the development of hyperketonemia, providing fundamental knowledge about manipulation of gut microbiome to improve metabolic adaptability in transition dairy cows. IMPORTANCEAccumulating evidence is pointing to an important association between gut microbiota-derived metabolites and metabolic disorders in humans and animals; however, this association in dairy cows from late gestation to early lactation is poorly understood. To address this gap, we integrated longitudinal gut microbial (feces) and metabolic (feces and plasma) profiles to characterize the phenotypic differences between healthy and hyperketonemic dairy cows from late gestation to early lactation. Our results demonstrate that cows underwent excessive lipid mobilization and insulin insensitivity before hyperketonemia was evident. The bile acids are functional readouts that link gut microbiota and host phenotypes in the development of hyperketonemia. Thus, this work provides new insight into the mechanisms involved in metabolic adaptation during the transition period to adjust to the high energy and metabolic demands after calving and during lactation, which can offer new strategies for livestock management involving intervention of the gut microbiome to facilitate metabolic adaptation.

2023-11-01·Journal of Controlled Release

Targeted echogenic and anti-inflammatory polymeric prodrug nanoparticles for the management of renal ischemia/reperfusion injury

Article

作者: Jun, Hayoung ; Jo, Hanui ; Lee, Dongwon ; Yang, Manseok ; Lee, Suyeon ; Kim, Sooyeon ; Lee, Youngjong ; Kim, Gi-Wook

Ischemia/reperfusion (IR) injury is an inevitable pathological event occurring when blood is resupplied to the tissues after a period of ischemia. One of major causes of IR injury is the overproduction of reactive oxygen species (ROS) including hydrogen peroxide (H₂O₂), which mediates the expression of various inflammatory cytokines to exacerbate tissue damages. The overproduced H₂O₂ could therefore serve as a diagnostic and therapeutic biomarker of IR injury. In this study, poly(boronated methacrylate) (pBMA) nanoparticles were developed as nanotheranostic agents for renal IR injury, which not only generate CO₂ bubbles to enhance the ultrasound contrast but also provide potent preventive effects in a H₂O₂-triggered manner. The surface of pBMA nanoparticles was decorated with taurodeoxycholic acid (TUDCA) that binds P-selectin overexpressed in inflamed tissues. In the mouse model of renal IR injury, TUDCA-coated pBMA (T-pBMA) nanoparticles preferentially accumulated in the injured kidney and markedly enhanced the ultrasound contrast. T-pBMA nanoparticles also effectively prevented renal IR injury by scavenging H₂O₂ and suppressing the expression of inflammatory cytokines. Treatment progress of IR injury could be also monitored by echogenic T-pBMA nanoparticles. Given their targeting ability, excellent H₂O₂-responsiveness, anti-inflammatory activity and H₂O₂-triggered echogenicity, T-pBMA nanoparticles have excellent translational potential for the management of various H₂O₂-related diseases including IR injury.

100 项与牛磺脱氧胆酸钠(Shaperon Co., Ltd.) 相关的药物交易

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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
特应性皮炎	药物发现	韩国	Shaperon, Inc.	2020-08-26
脓毒症	药物发现	韩国	Shaperon, Inc.	2019-12-05

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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


NCT03492398 (CTgov)	临床1期	特应性皮炎	56	HY209 (Cohort A HY209 0.05% Gel)	(糧選鏇顧構餘鑰顧艱襯) = 範壓餘製願襯顧壓衊襯製獵積觸襯製壓繭膚蓋 (廠蓋艱壓網網襯膚淵鬱, 襯衊顧窪築顧淵網鑰築 ~ 簾構鹽願夢衊獵繭遞憲) 更多	-	2020-10-19
				HY209 (Cohort A HY209 0.1% Gel)	(糧選鏇顧構餘鑰顧艱襯) = 繭衊簾憲繭餘積簾餘積製獵積觸襯製壓繭膚蓋 (廠蓋艱壓網網襯膚淵鬱, 築網製齋壓網襯鏇衊獵 ~ 夢膚窪鏇繭餘齋夢獵獵) 更多