更新于：2024-11-01

Pyragrel Sodium

吡拉格雷钠

更新于：2024-11-01

概要

概要

基本信息

药物类型

小分子化药

别名

TSF

靶点

TXA2 synthase

作用机制

TXA2 synthase抑制剂(血栓素A2合成酶抑制剂)

治疗领域

神经系统疾病心血管疾病

在研适应症

急性缺血性卒中血栓性脑梗塞大脑梗塞

非在研适应症-

原研机构

合肥医工医药股份有限公司

在研机构

合肥医工医药股份有限公司

非在研机构-

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)临床3期

特殊审评特殊审批 (中国)

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结构

分子式C18H20N2O4

InChIKeyGKIIUOKTDCNMFK-SOFGYWHQSA-N

CAS号1018438-91-9

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关联

项与吡拉格雷钠相关的临床试验

CTR20231309 / Recruiting临床3期

吡拉格雷钠注射液治疗急性缺血性脑卒中的多中心、随机、双盲、安慰剂平行对照Ⅲ期临床试验

评价吡拉格雷钠注射液治疗发病在48 h以内的急性缺血性脑卒中患者的有效性和安全性

开始日期2023-08-04

申办/合作机构

合肥医工医药股份有限公司

[+1]

CTR20180545 / Recruiting临床2期

吡拉格雷钠注射液治疗急性缺血性脑卒中多中心、随机、双盲、安慰剂对照II期临床试验

探索吡拉格雷钠注射液不同剂量治疗发病在48h以内的急性缺血性脑卒中患者的有效性和安全性

开始日期2018-07-16

申办/合作机构

合肥医工医药股份有限公司

[+1]

CTR20160215 / Completed临床1期

吡拉格雷钠注射液在健康志愿者中的单次给药药动学及24 h连续给药的耐受性及药动学研究

1）研究单次给予吡拉格雷钠注射液在低、中、高给药剂量时，其在中国健康成年志愿者体内的药代动力学规律。 2）研究连续24h静脉给予吡拉格雷钠注射液360mg后受试者的耐受性及药代动力学特征

开始日期2015-06-12

申办/合作机构

合肥医工医药股份有限公司

[+1]

100 项与吡拉格雷钠相关的临床结果

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100 项与吡拉格雷钠相关的转化医学

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100 项与吡拉格雷钠相关的专利（医药）

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234

项与吡拉格雷钠相关的文献（医药）

2024-04-01·Journal of Ethnopharmacology

Tangshen formula protects against podocyte apoptosis via enhancing the TFEB-mediated autophagy-lysosome pathway in diabetic nephropathy

Article

作者: Peng, Liang ; Zhang, Haojun ; Zhan, Yongli ; Lu, Xiaoguang ; Liu, Tongtong ; Li, Ping ; Yang, Liping ; Zhao, Hailing ; Ma, Fang ; Wang, Yuyang ; Mao, Huimin ; Zhao, Tingting

ETHNOPHARMACOLOGICAL RELEVANCEDiabetic nephropathy (DN) is the leading cause of end-stage kidney disease and currently there are no specific and effective drugs for its treatment. Podocyte injury is a detrimental feature and the major cause of albuminuria in DN. We previously reported Tangshen Formula (TSF), a Chinese herbal medicine, has shown therapeutic effects on DN. However, the underlying mechanisms remain obscure.AIM OF THE STUDYThis study aimed to explore the protective effect of TSF on podocyte apoptosis in DN and elucidate the potential mechanism.MATERIALS AND METHODSThe effects of TSF were assessed in a murine model using male KKAy diabetic mice, as well as in advanced glycation end products-stimulated primary mice podocytes. Transcription factor EB (TFEB) knockdown primary podocytes were employed for mechanistic studies. In vivo and in vitro studies were performed and results assessed using transmission electron microscopy, immunofluorescence staining, and western blotting.RESULTSTSF treatment alleviated podocyte apoptosis and structural impairment, decreased albuminuria, and mitigated renal dysfunction in KKAy mice. Notably, TSF extracted twice showed a more significant reduction in proteinuria than TSF extracted three times. Accumulation of autophagic biomarkers p62 and LC3, and aberrant autophagic flux in podocytes of DN mice were significantly altered by TSF therapy. Consistent with the in vivo results, TSF prevented the apoptosis of primary podocytes exposed to AGEs and activated autophagy. However, the anti-apoptosis capacity of TSF was countered by the autophagy-lysosome inhibitor chloroquine. We found that TSF increased the nuclear translocation of TFEB in diabetic podocytes, and thus upregulated transcription of its several autophagic target genes. Pharmacological activation of TFEB by TSF accelerated the conversion of autophagosome to autolysosome and lysosomal biogenesis, further augmented autophagic flux. Conversely, TFEB knockdown negated the favorable effects of TSF on autophagy in AGEs-stimulated primary podocytes.CONCLUSIONSThese findings indicate TSF appears to attenuate podocyte apoptosis and promote autophagy in DN via the TFEB-mediated autophagy-lysosome system. Thus, TSF may be a therapeutic candidate for DN.

2024-04-01·Biomedicine & Pharmacotherapy

Tangshen formula targets the gut microbiota to treat non-alcoholic fatty liver disease in HFD mice: A 16S rRNA and non-targeted metabolomics analyses

Article

作者: Wan, Yuzhou ; Gao, Mengqi ; Li, Yuxi ; Liu, Lin ; Rong, Jin ; Chen, Kexu ; Li, Xin ; Zhao, Tingting ; Wang, Shaopeng ; Yan, Meihua ; Dong, Xi ; Ma, Liang ; Li, Ping ; Qi, Huimin ; Zhang, Bo

BACKGROUNDTangshen formula (TSF) has an ameliorative effect on hepatic lipid metabolism in non-alcoholic fatty liver disease (NAFLD), but the role played by the gut microbiota in this process is unknown.METHODWe conducted three batches of experiments to explore the role played by the gut microbiota: TSF administration, antibiotic treatment, and fecal microbial transplantation. NAFLD mice were induced with a high-fat diet to investigate the ameliorative effects of TSF on NAFLD features and intestinal barrier function. 16S rRNA sequencing and serum untargeted metabolomics were performed to further investigate the modulatory effects of TSF on the gut microbiota and metabolic dysregulation in the body.RESULTSTSF ameliorated insulin resistance, hypercholesterolemia, lipid metabolism disorders, inflammation, and impairment of intestinal barrier function. 16S rRNA sequencing analysis revealed that TSF regulated the composition of the gut microbiota and increased the abundance of beneficial bacteria. Antibiotic treatment and fecal microbiota transplantation confirmed the importance of the gut microbiota in the treatment of NAFLD with TSF. Subsequently, untargeted metabolomics identified 172 differential metabolites due to the treatment of TSF. Functional predictions suggest that metabolisms of choline, glycerophospholipid, linoleic acid, alpha-linolenic acid, and arachidonic acid are the key metabolic pathways by which TSF ameliorates NAFLD and this may be influenced by the gut microbiota.CONCLUSIONTSF treats the NAFLD phenotype by remodeling the gut microbiota and improving metabolic profile, suggesting that TSF is a functional gut microbial and metabolic modulator for the treatment of NAFLD.

2024-04-01·Experimental Gerontology

Tangshen Formula alleviates inflammatory injury against aged diabetic kidney disease through modulating gut microbiota composition and related amino acid metabolism

Article

作者: Chen, Dan-Qian ; Li, Ping ; Zhang, Hao-Jun ; Zhang, Wen ; Liu, Hui ; Zhao, Hai-Ling ; Feng, Kai

Diabetic kidney disease (DKD) is leading causes and one of the fastest growing causes of chronic kidney disease worldwide, and leads to high morbidity and mortality. Emerging evidences have revealed gut microbiota dysbiosis and related metabolism dysfunction play a dominant role in DKD progression and treatment through modulating inflammation. Our previous studies showed that Tangshen Formula (TSF), a Chinese herbal prescription, exhibited anti-inflammatory effect on DKD, but underlying mechanism that involved gut microbiota and related metabolism in aged model remained obscure. Here, BTBR ob/ob mice were used to establish aged DKD model, and 16S rRNA sequence and untargeted metabolomic analyses were employed to investigate the correlation between colonic microbiota and serum metabolism. The aged ob/ob mice exhibited obvious glomerular and renal tubule injury and kidney function decline in kidney, while TSF treatment significantly attenuated these abnormalities. TSF also exhibited potent anti-inflammatory effect in aged ob/ob mice indicating by reduced proinflammatory factor IL-6 and TNF-α, MCP-1 and COX-2 in serum, kidney and intestine, which suggested the involvement of gut microbiota with TSF effect. The 16S rDNA sequencing of the colonic microbiome and untargeted serum metabolomics analysis revealed significant differences in gut microbiota structure and serum metabolomic profiles between WT and ob/ob mice. Notably, TSF treatment reshaped the structure of gut microbiota and corrected the disorder of metabolism especially tryptophan metabolism and arginine biosynthesis. TSF increased Anaeroplasma and Barnesiella genera and decreased Romboutsia, Akkermansia, and Collinsella genera, and further elevated tryptophan, 5-hydroxyindoleacetate, glutamic acid, aspartate and reduced 4-hydroxy-2-quinolinecarboxylic acid, indole-3-acetic acid, xanthurenic acid, glutamine. Further correlation analysis indicated that disturbed gut microbiota was linked to tryptophan metabolism and arginine biosynthesis to regulate inflammation in aged DKD. Our data revealed that TSF attenuated renal inflammation by modulating gut microbiota and related amino acid metabolism in aged DKD model, highlighting gut microbiota and related metabolism functioned as potential therapeutic target for DKD in elderly patients.

100 项与吡拉格雷钠相关的药物交易

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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
急性缺血性卒中	临床3期	中国	合肥医工医药股份有限公司	2023-08-04
血栓性脑梗塞	临床3期	中国	合肥医工医药股份有限公司	2023-08-04
大脑梗塞	临床2期	中国	合肥医工医药股份有限公司	2018-07-16