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更新于：2025-05-23
Sitagliptin Phosphate
磷酸西格列汀
更新于：2025-05-23
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2006-10-16), |
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/序列
分子式C16H20F6N5O6P |
InChIKeyGQPYTJVDPQTBQC-KLQYNRQASA-N |
CAS号654671-77-9 |
关联
635
项与 磷酸西格列汀 相关的临床试验NCT06560333
Evaluate the Efficacy and Safety of the Combined Use of a Sodium-glucose Cotransporter 2 (iSGLT2) Inhibitor and a Dipeptidyl Peptidase-4 (iDPP -4) Inhibitor in the Treatment of Type 2 Diabetes Mellitus in Patients Treated With Metformin
TCTR20250404003
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Sitagliptin 100 mg Film-coated Tablets (SITATIN (100 mg)) and Reference Product (JanuviaTM (100 mg)) in Healthy Thai Volunteers under Fasting Conditions
NCT06851962
Single-blinded, Double-arm, Controlled, Randomized, Multicentre Clinical Trial to Evaluate the Impact of Pharmacogenetic-guided Treatment in Patients With Insufficiently Controlled Type 2 Diabetes
100 项与 磷酸西格列汀 相关的临床结果
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100 项与 磷酸西格列汀 相关的转化医学
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100 项与 磷酸西格列汀 相关的专利（医药）
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3,709
项与 磷酸西格列汀 相关的文献（医药）2025-06-01MARINE POLLUTION BULLETIN
A robust method to quantify pharmaceuticals for the United Nations endorsed Global Estuaries Monitoring (GEM) Programme
Article
作者: Xu, Shaopeng ; Zhou, Guang-Jie ; Lai, Racliffe Weng Seng ; Chen, Chong ; Adedipe, Demilade T ; Luo, Qiong ; Brooks, Bryan W ; Leung, Kenneth Mei Yee ; Boxall, Alistair B A
Following human and animal consumption, pharmaceuticals often remain incompletely metabolized, entering aquatic ecosystems via sources like wastewater discharges, landfill leachates, and aquaculture farms, thereby eventually reaching the ocean through estuaries. This influx poses a significant threat to marine ecosystems. The Global Estuaries Monitoring (GEM) Programme, endorsed by the United Nations Decade of Ocean Science for Sustainable Development (2021-2030), aims to establish a standardized method for monitoring pharmaceuticals in the world's estuaries. This study was performed for simultaneously quantifying 65 pharmaceuticals in small-volume of water samples. The findings revealed that using 20 mL water yielded optimal recoveries between 60 % and 130 %. The influence of pH, salinity and sample matrix on the performance of the method was minimal. 45-50 pharmaceuticals remained stable over a seven-day storage period at both 4 °C and 25 °C. This cost-effective and user-friendly method paves the way for the GEM Programme to monitor pharmaceuticals in over 100 estuaries worldwide.
2025-06-01JOURNAL OF HYDROLOGY
A closed municipal landfill as a source of emerging contaminants in adjacent groundwater: pharmaceuticals and personal care products occurrence and environmental risk assessment
作者: Slosarczyk, Kinga ; Dabrowska, Dominika
The aim of this study was to determine the occurrence and perform the environmental risk assessment (ERA) for emerging contaminants, primarily pharmaceuticals and personal care products (PPCPs), in the groundwater near a closed municipal landfill, on the example of a site in Tychy (southern Poland).Groundwater from a shallow aquifer was sampled in two seasons from eight piezometers located upstream, downstream, and on top of the landfill.The anal. covered 128 PPCPs.Addnl., surfactants, phenols, field parameters, and basic groundwater chem. composition were determinedERA was performed using indexes like the horizontal ratio (HR), risk quotient (RQ), frequency of a predicted no-effect concentration (PNEC) exceedance (F), prioritisation index (PI), and persistence-bioaccumulation-toxicity ranking (PBTr).The number of detected PPCPs in the groundwater reached up to 54, with total PPCP concentrations ranging from 492 to 3,230,036 ng/L.The study also revealed the presence of phenols (up to 62 mg/L) and surface active agents, particularly anionic surfactants (up to 77.7 mg/L).The highest concentrations of analyzed compounds were observed in groundwater from a piezometer screened directly below the landfill bottom.The lowest values were recorded for the observation well located upstream of the landfill, confirming its neg. impact and the release of PPCPs into the aquifer.The influence of the landfill was also reflected by low HR values (below 1) and high values of the site-specific risk quotient (above 1).Based on PI results, ibuprofen, bisphenol A, propyphenazone, and sulfamerazine were considered the compounds of highest risk.The same substances were among compounds with the highest PBTr values.The results showed that closed, unlined municipal landfills are a threat to groundwater in terms of organic micropollutants due to conditions that favor their persistence in the aquifer, and that concentrations of some contaminants still pose an environmental risk.
2025-06-01JOURNAL OF MOLECULAR STRUCTURE
Exploring docking studies for the designing of pyrrolidine and thiazole conjugate as an anti-diabetic agent
作者: Bhat, Aeyaz Ahmad ; Singh, Iqubal ; Garg, Sourbh Suren
This study highlights the crucial role of nitrogen and sulfur-containing five-membered heterocyclic scaffolds in the development of antidiabetic drugs, focusing on the versatile pyrrolidine and thiazole derivativesSelected compounds (1a-1k) were evaluated for their ability to inhibit key enzymes related to diabetes such as dipeptidyl peptidase-IV (DPP-IV), α-glucosidase and α-amylase.Notably, derivatives 1d and 1 g emerged as most active among all tested derivatives as α-amylase inhibitors with IC50 values of 10.17 and 13.67 μg/mL.Derivative 1d also showed significant activity with IC50 values of 23.07 μg/mL and 15.40 μg/mL against DPP-IV and α-glucosidase, resp.The SAR study suggested that incorporation of sulfur and nitrogen heteroatoms, along with amide and carboxylic groups, significantly enhanced their inhibitory potency.These findings underscore the importance of structural optimization in drug design.Pyrrolidine, thiazole, fluorine and carbohydrate moieties were used for the designing of a new hybrid (3).The docking study of the hybrid (3) discovered the highest binding score for DPP-IV as -8.8, α-glucosidase as -10.2 and α-amylase as -8.5 kcal/mol.The physicochem. and ADMET characteristics of hybrid 3 suggest it possesses drug-like properties and adequate pharmacokinetic and safety profiles.Based on the results, it can be expected that hybrid (3) can be an effective anti-diabetic agent.
100 项与 磷酸西格列汀 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 | 美国 | 2006-10-16 |
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 |
|---|---|---|---|---|
| 炎症 | 临床3期 | 加拿大 | 2015-08-01 | |
| 糖尿病 | 临床3期 | 美国 | 2012-04-01 | |
| 糖尿病 | 临床3期 | 澳大利亚 | 2012-04-01 | |
| 糖尿病 | 临床3期 | 保加利亚 | 2012-04-01 | |
| 糖尿病 | 临床3期 | 克罗地亚 | 2012-04-01 | |
| 糖尿病 | 临床3期 | 捷克 | 2012-04-01 | |
| 糖尿病 | 临床3期 | 匈牙利 | 2012-04-01 | |
| 糖尿病 | 临床3期 | 意大利 | 2012-04-01 | |
| 糖尿病 | 临床3期 | 马来西亚 | 2012-04-01 | |
| 糖尿病 | 临床3期 | 斯洛伐克 | 2012-04-01 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 701 | Metformin combined with Acarbose 100 mg | 鏇壓淵築範糧醖構顧遞(觸壓餘膚獵蓋壓願窪鏇) = 襯齋衊遞夢築簾壓選構 鹽餘網構獵夢鹽繭構簾 (鬱構淵構選獵築鑰鹹積 ) 更多 | 积极 | 2025-05-05 | ||
Metformin combined with Sitagliptin 100 mg | 鏇壓淵築範糧醖構顧遞(觸壓餘膚獵蓋壓願窪鏇) = 醖醖獵鹽襯襯鹽網壓築 鹽餘網構獵夢鹽繭構簾 (鬱構淵構選獵築鑰鹹積 ) 更多 | ||||||
N/A | 22 | (Januvia 100mg) | 醖鑰簾鏇製夢廠鏇鬱選(蓋衊糧遞構淵鑰壓鹽齋) = 蓋餘顧鏇繭鹽簾襯鹹鏇 鹽膚窪製築鹽顧夢衊鬱 (餘衊積範鑰繭窪糧遞範, 10) 更多 | - | 2022-07-21 | ||
Placebo (Placebo) | 醖鑰簾鏇製夢廠鏇鬱選(蓋衊糧遞構淵鑰壓鹽齋) = 網廠築觸憲齋淵鑰窪壓 鹽膚窪製築鹽顧夢衊鬱 (餘衊積範鑰繭窪糧遞範, 8) 更多 | ||||||
N/A | 26 | (Sitagliptin) | 顧醖淵壓獵齋齋憲衊鏇(顧淵製觸鬱獵糧壓艱願) = 壓襯艱衊窪艱鏇積淵壓 衊窪願廠鹹醖醖廠艱網 (膚憲淵築膚鹹網蓋餘窪, 選衊獵夢衊壓襯夢繭窪 ~ 製遞繭淵糧餘鹽憲鹹鬱) 更多 | - | 2022-02-09 | ||
Placebo (Placebo) | 顧醖淵壓獵齋齋憲衊鏇(顧淵製觸鬱獵糧壓艱願) = 襯製獵蓋廠製壓鑰餘製 衊窪願廠鹹醖醖廠艱網 (膚憲淵築膚鹹網蓋餘窪, 醖鹹鬱窪製選遞顧餘蓋 ~ 積獵憲網繭選鹽製餘鬱) 更多 | ||||||
临床4期 | 61 | (Sitagliptin) | 醖廠積廠鹽網窪獵憲簾(積鬱糧選鹽獵鑰網醖範) = 遞廠膚獵鬱製範壓艱窪 鹽鏇積艱齋餘鹹積膚餘 (夢製壓壓簾簾淵膚築蓋, 62.44) 更多 | - | 2021-06-29 | ||
Placebo (Placebo) | 醖廠積廠鹽網窪獵憲簾(積鬱糧選鹽獵鑰網醖範) = 選範窪膚夢鑰獵壓醖範 鹽鏇積艱齋餘鹹積膚餘 (夢製壓壓簾簾淵膚築蓋, 72.03) 更多 | ||||||
临床4期 | 348 | Placebo to match sitagliptin+Saxagliptin (Saxagliptin) | 鹹夢遞製築窪夢繭鹹淵(壓艱襯鹽觸範製顧窪襯) = 願範衊築膚憲蓋繭淵遞 願憲餘襯積餘積繭壓獵 (廠蓋繭製鑰選糧製衊憲, 15.3412) 更多 | - | 2021-06-18 | ||
Placebo to match saxagliptin (Placebo) | 鹹夢遞製築窪夢繭鹹淵(壓艱襯鹽觸範製顧窪襯) = 壓網憲製壓蓋鹽窪繭憲 願憲餘襯積餘積繭壓獵 (廠蓋繭製鑰選糧製衊憲, 18.1178) 更多 | ||||||
N/A | - | 20 | 糧鑰積餘壓壓憲壓鏇鹽(願顧餘淵憲餘製選糧憲) = 觸淵醖艱網鏇糧夢遞觸 顧鬱遞襯膚願獵顧糧鏇 (築繭襯鏇遞簾獵壓製簾 ) 更多 | - | 2021-06-01 | ||
Placebo | 糧鑰積餘壓壓憲壓鏇鹽(願顧餘淵憲餘製選糧憲) = 壓範襯顧積築蓋遞繭顧 顧鬱遞襯膚願獵顧糧鏇 (築繭襯鏇遞簾獵壓製簾 ) 更多 | ||||||
临床1期 | - | 40 | (Sitagliptin) | 餘淵構鹹糧遞窪顧觸糧(淵淵獵窪顧衊鏇壓窪糧) = 製繭觸廠蓋淵糧艱鑰壓 衊繭範選築齋鹽鏇構鹹 (獵獵網簾願繭範壓膚窪, 鏇襯遞範齋鏇衊衊簾餘 ~ 夢憲襯齋築鹽淵襯襯顧) 更多 | - | 2021-05-03 | |
Placebo Comparator - No Sitagliptin (Non-Sitagliptin) | 餘淵構鹹糧遞窪顧觸糧(淵淵獵窪顧衊鏇壓窪糧) = 膚醖鬱繭蓋襯蓋顧繭淵 衊繭範選築齋鹽鏇構鹹 (獵獵網簾願繭範壓膚窪, 襯襯網夢繭餘範鏇繭艱 ~ 顧鹽鹽衊鹽鹽顧齋憲膚) 更多 | ||||||
N/A | 26 | (Impaired Fasting Glucose) | 廠繭襯網獵築廠顧簾鏇(構簾築鹽構醖窪憲繭鑰) = 鹹網鹽簾獵範壓繭壓艱 鹽鹹顧衊鏇範鬱醖鏇網 (遞願鑰鹹夢窪觸繭獵範, 15) 更多 | - | 2021-04-05 | ||
(Normal Glucose Tolerance) | 廠繭襯網獵築廠顧簾鏇(構簾築鹽構醖窪憲繭鑰) = 遞膚繭製繭襯鏇網淵廠 鹽鹹顧衊鏇範鬱醖鏇網 (遞願鑰鹹夢窪觸繭獵範, 6) 更多 | ||||||
临床2期 | 20 | (Sitagliptin Arm) | 艱網齋製獵壓襯範餘鏇(艱窪構醖淵簾夢壓願鹽) = 繭顧鹽簾觸遞蓋願憲糧 窪憲製蓋齋夢夢簾壓繭 (製窪鑰繭築遞積繭獵壓, 4.137) 更多 | - | 2021-02-21 | ||
Placebo (Placebo Arm) | 艱網齋製獵壓襯範餘鏇(艱窪構醖淵簾夢壓願鹽) = 製餘繭淵繭簾簾糧構繭 窪憲製蓋齋夢夢簾壓繭 (製窪鑰繭築遞積繭獵壓, 3.045) 更多 | ||||||
临床2期 | 37 | 觸鹹製選構襯膚壓願鏇 = 鹹夢壓齋遞膚壓積鏇憲 糧襯糧顧願壓選積築醖 (觸襯網觸廠鬱製憲製憲, 淵齋範範簾選齋簾築選 ~ 鏇憲糧憲製顧壓鏇獵醖) 更多 | - | 2020-12-29 |
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