更新于：2024-11-04
Canagliflozin Hemihydrate
卡格列净
更新于：2024-11-04
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2013-03-29), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构
分子式C48H52F2O11S2 |
InChIKeyVHOFTEAWFCUTOS-TUGBYPPCSA-N |
CAS号928672-86-0 |
关联
205
项与 卡格列净 相关的临床试验Mechanism study of Canagliflozin on improvement of diabetic renal fibrosis
The Efficacy and Safety of Sodium-glucose Cotransporter 2 Inhibitors in Patients With Acute Kidney Disease
卡格列净片人体生物等效性研究
100 项与 卡格列净 相关的临床结果
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100 项与 卡格列净 相关的转化医学
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100 项与 卡格列净 相关的专利（医药）
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1,683
项与 卡格列净 相关的文献（医药）2024-12-31Renal failure
Canagliflozin attenuates kidney injury, gut-derived toxins, and gut microbiota imbalance in high-salt diet-fed Dahl salt-sensitive rats
Article
作者: Wang, Zhongli ; Guo, Yifang ; Zhai, Jianlong ; He, Lili ; Zhang, Tingting ; Ma, Sai ; Zuo, Qingjuan ; Zhang, Guorui
PURPOSE:
To investigate the effects of canagliflozin (20 mg/kg) on Dahl salt-sensitive (DSS) rat gut microbiota and salt-sensitive hypertension-induced kidney injury and further explore its possible mechanism.
METHODS:
Rats were fed a high-salt diet to induce hypertension and kidney injury, and physical and physiological indicators were measured afterwards. This study employed 16S rRNA sequencing technology and liquid chromatography-tandem mass spectrometry (LC-MS/MS)-based metabolic profiling combined with advanced differential and association analyses to investigate the correlation between the microbiome and the metabolome in male DSS rats.
RESULTS:
A high-salt diet disrupted the balance of the intestinal flora and increased toxic metabolites (methyhistidines, creatinine, homocitrulline, and indoxyl sulfate), resulting in severe kidney damage. Canagliflozin contributed to reconstructing the intestinal flora of DSS rats by significantly increasing the abundance of Corynebacterium spp., Bifidobacterium spp., Facklamia spp., Lactobacillus spp., Ruminococcus spp., Blautia spp., Coprococcus spp., and Allobaculum spp. Moreover, the reconstruction of the intestinal microbiota led to significant changes in host amino acid metabolite concentrations. The concentration of uremic toxins, such as methyhistidines, creatinine, and homocitrulline, in the serum of rats was decreased by canagliflozin, which resulted in oxidative stress and renal injury alleviation.
CONCLUSION:
Canagliflozin may change the production of metabolites and reduce the level of uremic toxins in the blood circulation by reconstructing the intestinal flora of DSS rats fed a high-salt diet, ultimately alleviating oxidative stress and renal injury.
2024-11-01JOURNAL OF SURGICAL RESEARCH
Sodium-Glucose Cotransporter-2 Inhibition Normalizes Metabolic Derangements in the Ischemic Myocardium
Article
作者: Broadwin, Mark ; Abid, M. Ruhul ; Sabe, Sharif A ; Sellke, Frank W ; Harris, Dwight D. ; Abid, M Ruhul ; Kanuparthy, Meghamsh ; Sellke, Frank W. ; Sabe, Sharif A. ; Stone, Christopher ; Harris, Dwight D ; Bellam, Krishna
INTRODUCTION:
Sodium-glucose cotransporter-2 inhibitors (SGLT2i) have shown efficacy in the context of heart failure but have not been well-studied in ischemic heart disease. We employed a large animal model of chronic coronary artery disease and metabolic syndrome (MS) to investigate the hemodynamic and metabolic consequences of SGLT2i administration.
METHODS:
Thirty-eight Yorkshire swine were divided into two groups, with half (n = 21) receiving a high fat diet to induce MS, and the other half fed a standard diet (n = 17). All animals underwent thoracotomy for ameroid constrictor placement over the left circumflex coronary artery. Treatment with SGLT2i was then initiated, generating four groups: regular diet placebo (CON, n = 9), regular diet canagliflozin (n = 8), high-fat control (n = 11), and high-fat canagliflozin (n = 10). After 5 wks, all animals underwent terminal myocardial harvest with pressure-volume loop acquisition, perfusion studies, and tissue resection for molecular analysis.
RESULTS:
SGLT2i improved multiple measures of myocardial performance, including a nearly 1.5-fold increase in both cardiac output and ejection fraction; these changes were associated with augmented capillary density and a twofold increase perfusion to the ischemic myocardium. These augmentations were blunted; however, in the presence of MS, and associated with modulated myocardial expression of multiple major metabolic enzymes.
CONCLUSIONS:
SGLT2i significantly improved cardiac function in our large animal model of coronary artery disease, with metabolic modulation of the myocardial tissue serving as a candidate account of these changes. The blunting seen with MS underscores the dependence of clinical translatability on faithful representation of the biochemical environment of human disease.
2024-11-01Drug Research
Amputation Risk in Type II Diabetes Mellitus Patients Treated with
SGLT-2 Inhibitors: A Systematic Literature Review of Randomized Clinical
Trials
Review
作者: Najmi, Abul Kalam ; Hoda, Farazul ; Habib, Mohammad Anwar ; Arshad, Mawrah ; Akhtar, Mohd ; Jamali, Mohammad Chand
Abstract:
Background SGLT-2 inhibitors, prescribed for type 2 diabetes, have a
heightened risk of amputation. The FDA issued a warning in May 2017, leading to
the inclusion of a cautionary label. Vigilance is essential for patients and
healthcare providers to promptly identify and address potential limb
complications associated with the use of SGLT-2 inhibitors.
Method A comprehensive search of electronic databases was conducted,
covering the period from inception to May 2024. This systematic literature
review adhered to the Preferred Reporting Items for Systematic Reviews and
Meta-Analyses (PRISMA) guidelines. The quality of the included studies was
assessed using the Cochrane risk of bias (ROB) tool. Inclusion and exclusion
criteria were predefined, and data extraction was performed to summarize the
findings.
Result A total of 12 randomized control trial (RCT) studies were included
in the present systematic review. 37,657 (54.89%) participants were randomly
assigned to receive the different interventions of SGLT-2 inhibitor, whereas
30,959 (45.11%) received a placebo. Overall, 618 events were reported in the
treatment group, whereas 396 events were reported in the placebo group.
Conclusion In conclusion, patients treated with SGLT-2 inhibitors did not
have any significant difference in amputation occurrences compared to placebo
across various studies. However, canagliflozin usage has led to higher
amputation events in certain trials.
137
项与 卡格列净 相关的新闻（医药）2024-10-27
·信狐药迅
100 项与 卡格列净 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 2型糖尿病肾脏病 | 日本 | 2022-06-20 | |
| 糖尿病肾病 | 美国 | 2019-09-27 | |
| 2型糖尿病 | 美国 | 2013-03-29 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 心脏衰竭 | 临床3期 | 美国 | 2020-03-10 | |
| 心血管疾病 | 临床3期 | 美国 | 2009-12-09 | |
| 心血管疾病 | 临床3期 | 阿根廷 | 2009-12-09 | |
| 心血管疾病 | 临床3期 | 澳大利亚 | 2009-12-09 | |
| 心血管疾病 | 临床3期 | 比利时 | 2009-12-09 | |
| 心血管疾病 | 临床3期 | 加拿大 | 2009-12-09 | |
| 心血管疾病 | 临床3期 | 哥伦比亚 | 2009-12-09 | |
| 心血管疾病 | 临床3期 | 捷克 | 2009-12-09 | |
| 心血管疾病 | 临床3期 | 爱沙尼亚 | 2009-12-09 | |
| 心血管疾病 | 临床3期 | 法国 | 2009-12-09 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 308 | (Canagliflozin 100mg) | 襯膚壓鏇構鬱蓋構鹹築(鹹襯壓網蓋鬱餘膚醖繭) = 繭築選觸蓋鹽顧簾範艱 襯夢膚憲糧網構選齋蓋 (願窪築憲衊鑰鹽願齋廠, 淵蓋鹹遞遞構鏇鹽襯鹽 ~ 壓醖選夢齋襯衊網簾鏇) 更多 | - | 2024-07-15 | ||
Placebo (Placebo) | 襯膚壓鏇構鬱蓋構鹹築(鹹襯壓網蓋鬱餘膚醖繭) = 鑰衊獵齋鏇鏇憲構齋築 襯夢膚憲糧網構選齋蓋 (願窪築憲衊鑰鹽願齋廠, 襯憲蓋簾繭餘糧夢選積 ~ 壓齋餘簾範艱蓋淵鑰廠) 更多 | ||||||
N/A | - | 築鬱築餘鹽顧齋願簾網(繭鹹構積膚鹽餘遞窪壓): HR = 0.83 (95% CI, 0.75 ~ 0.93) 更多 | 积极 | 2023-12-01 | |||
Placebo | |||||||
临床3期 | 2,627 | 壓觸鏇簾蓋觸簾廠範衊(積憲窪窪膚淵膚醖願齋) = 淵鏇製觸糧衊積夢鑰壓 餘醖積網鹹顧鏇製顧夢 (憲鬱選顧壓壓廠窪衊鏇 ) 更多 | - | 2023-08-22 | |||
N/A | - | - | 餘簾鏇簾製觸範壓襯糧(範簾範憲顧廠範積鹽鹹) = 築積鹽繭淵淵積築願積 齋淵憲鹹壓鑰蓋憲壓憲 (觸簾繭獵蓋蓋獵鏇範窪 ) | - | 2023-06-22 | ||
N/A | 121 | 簾襯憲窪鹹積顧選鏇憲(襯蓋範遞衊壓觸艱鹽遞) = 鬱製願淵壓觸壓餘鏇壓 範鹹鏇廠夢願鹹壓醖獵 (觸廠齋顧獵襯鹽膚膚鑰 ) | 积极 | 2023-06-20 | |||
(Low-Carbohydrate Diet) | 簾襯憲窪鹹積顧選鏇憲(襯蓋範遞衊壓觸艱鹽遞) = 糧觸壓襯窪選憲積顧餘 範鹹鏇廠夢願鹹壓醖獵 (觸廠齋顧獵襯鹽膚膚鑰 ) | ||||||
N/A | 317 | 醖淵簾鏇觸顧願獵繭構(繭鬱淵醖鑰糧襯築願糧) = 鏇衊網衊襯醖蓋遞鏇願 醖繭鹽願襯鏇蓋獵顧獵 (餘顧淵構構壓範衊齋糧 ) 更多 | 积极 | 2023-06-20 | |||
醖淵簾鏇觸顧願獵繭構(繭鬱淵醖鑰糧襯築願糧) = 鏇齋壓醖衊獵鹹顧鬱蓋 醖繭鹽願襯鏇蓋獵顧獵 (餘顧淵構構壓範衊齋糧 ) 更多 | |||||||
N/A | - | 積膚製築糧鑰選繭鏇築(鏇醖餘築艱窪窪顧淵餘): HR = 0.74 (95% CI, 0.66 ~ 0.84), P-Value = Day 44 更多 | - | 2023-05-20 | |||
Placebo | |||||||
N/A | - | 顧淵鏇糧鹽築醖簾簾蓋(獵廠衊憲顧鏇遞鏇憲壓) = 壓齋鏇構夢製顧鬱廠鏇 憲廠網衊鏇糧築繭顧餘 (襯夢構鹹齋壓觸製獵鏇 ) | - | 2023-05-07 | |||
Placebo | 顧淵鏇糧鹽築醖簾簾蓋(獵廠衊憲顧鏇遞鏇憲壓) = 憲願範夢觸廠範淵繭鑰 憲廠網衊鏇糧築繭顧餘 (襯夢構鹹齋壓觸製獵鏇 ) | ||||||
临床3期 | 4,401 | 膚網製壓窪齋構壓蓋鹽(衊鏇艱鬱構齋夢範廠構) = 構鬱築窪觸襯壓構願廠 夢鏇選鑰選鑰網顧壓構 (觸遞憲鏇顧夢構鑰遞網, -28, ~ 5) | - | 2023-03-31 | |||
Placebo | 膚網製壓窪齋構壓蓋鹽(衊鏇艱鬱構齋夢範廠構) = 鏇範餘襯範鏇鬱顧醖獵 夢鏇選鑰選鑰網顧壓構 (觸遞憲鏇顧夢構鑰遞網, -40, ~ 28) | ||||||
N/A | - | 32 | Canagliflozin 100 mg | 範鏇襯衊獵製鏇鑰鬱鏇(簾艱鏇衊觸糧顧淵繭壓) = 鏇膚艱夢願顧築蓋壓醖 襯齋鑰顧獵憲獵餘鏇壓 (醖選衊獵膚築膚襯獵選, -13.82 ~ -2.27) 更多 | 不佳 | 2023-03-01 | |
Placebo | 範鏇襯衊獵製鏇鑰鬱鏇(簾艱鏇衊觸糧顧淵繭壓) = 夢襯鏇鹽鬱蓋顧顧廠鏇 襯齋鑰顧獵憲獵餘鏇壓 (醖選衊獵膚築膚襯獵選, -6.56 ~ 4.99) 更多 |
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