更新于：2024-11-15
Sitagliptin Phosphate
磷酸西格列汀
更新于：2024-11-15
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) |
登录后查看时间轴
结构
分子式C16H20F6N5O6P |
InChIKeyGQPYTJVDPQTBQC-KLQYNRQASA-N |
CAS号654671-77-9 |
关联
551
项与 磷酸西格列汀 相关的临床试验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
Sitagliptin or BeiDouGen Capsule Improve the Pregnancy Outcome in Patients with PCOS
Doxycycline in Combination With Sitagliptin on the Glycemic and Cardiac Indices in Patients With Type 2 Diabetes Mellitus
100 项与 磷酸西格列汀 相关的临床结果
登录后查看更多信息
100 项与 磷酸西格列汀 相关的转化医学
登录后查看更多信息
100 项与 磷酸西格列汀 相关的专利（医药）
登录后查看更多信息
116
项与 磷酸西格列汀 相关的文献（医药）2024-06-01The Journal of dermatology
A case of anti‐laminin γ1 (p200) pemphigoid developed after dipeptidyl peptidase‐4 inhibitor administration
Article
作者: Nakatani, Kahori ; Nomura, Yuki ; Noborio, Reiko ; Kiyohara, Takahiro ; Hashimoto, Takashi ; Ueki, Yoko
Abstract:
A 73‐year‐old man with diabetes mellitus was referred to our department for ultraviolet treatment for erythematous skin lesions with itching. On dipeptidyl peptidase‐4 inhibitor (DPP‐4i) sitagliptin (Januvia®) for diabetes mellitus, the erythematous skin lesions appeared and spread to the whole body. At the initial visit, erythema multiforme‐like skin lesions with crusts were observed on the trunk and extremities, and the patient was suspected to have drug eruption. Histopathology demonstrated eosinophilic infiltration in the superficial dermis and inflammatory cell infiltration in the epidermis. Sitagliptin was discontinued, and erythematous lesions improved with oral prednisolone. Thereafter the patient was treated with phototherapy and betamethasone sodium phosphate infusion for residual prurigo. However, blistering skin lesions appeared 5 months later. Histopathological findings were subepidermal blisters with eosinophilic abscess, and bullous pemphigoid was suspected. CLEIAs for autoantibodies to desmoglein 1 (Dsg1), Dsg3 and BP180 were negative. Direct immunofluorescence showed linear depositions of immunoglobulin G (IgG) and C3 at the epidermal basement membrane zone, and indirect immunofluorescence detected IgG anti‐epidermal basement membrane zone antibodies, reacting with the dermal side of 1M NaCl‐split normal human skin. IgG antibodies reacted with 200 kDa laminin γ1 (p200) by immunoblotting using dermal extracts. These results indicated that this patient was diagnosed with anti‐laminin γ1 (p200) pemphigoid developed after DPP‐4i administration. Although reports of DPP‐4i‐related bullous pemphigoid have accumulated, cases of anti‐laminin γ1 (p200) pemphigoid developed after DPP‐4i administration are rarely reported.
2024-02-01Journal of pharmaceutical sciences
Solid-State Phase Transformation of Monohydrate and Anhydrous Form II of Sitagliptin Phosphate into a Novel Anhydrous Form IV – Solvent-Driven, Temperature-Induced and Stress Testings
Article
作者: Petrushevski, Gjorgji ; Chachorovska, Marina ; Geskovski, Nikola ; Makreski, Petre ; Lefton, Jonathan B ; Jakimovska, Viktorija
The solid form landscape of sitagliptin phosphate was systematically evaluated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy (FTIR), Raman spectroscopy and X-ray powder diffraction (XRPD), supported by a plethora of auxiliary analytical techniques. The preformulation experiments resulted in the transition of sitagliptin phosphate monohydrate into a new anhydrous form (designated as form IV), obtained after recrystallization from absolute ethanol. The anhydrous form IV remained stable under stressed conditions (1 month at 25 °C/60 %RH and 40 °C/75 %RH). On the other hand, thermal heating (dehydration) of sitagliptin phosphate monohydrate resulted in conversion into another anhydrous form II. Form II was found to be metastable, because after melting, under exposure at 40 °C/75 %RH for 1 month, or when dissolved in absolute ethanol converted to the stable anhydrous form IV of sitagliptin phosphate. A monotropic relationship was found between both studied anhydrous forms. Intrinsic dissolution tests revealed differences in the dissolution rates between the monohydrate and the anhydrous forms of sitagliptin phosphate. This research corrects the record with an accurate chemical composition of the anhydrous form IV of sitagliptin phosphate that was previously regarded as a hemiethanolate. In addition, the crystal structure of anhydrous form II of sitagliptin phosphate has been solved and reported for the first time.
2024-01-01Gerontology
Sitagliptin Extends Lifespan of Caenorhabditis elegans by Inhibiting Insulin/Insulin-Like Signaling and Activating Dietary Restriction-Like Signaling Pathways
Article
作者: Yang, Jing ; Li, Yimin ; Wang, Cheng ; Zheng, Jingming ; Ye, Qunshan ; Wan, Qin-Li ; Qiao, Jing
Introduction: The discovery of longevity molecules that delay aging and prolong lifespan has always been a dream of humanity. Sitagliptin phosphate (SIT), an oral dipeptidyl peptidase-4 (DPP-4) inhibitor, is an oral drug commonly used in the treatment of type 2 diabetes (T2D). In addition to being antidiabetic, previous studies have reported that SIT has shown potential to improve health. However, whether SIT plays a role in the amelioration of aging and the underlying molecular mechanism remain undetermined. Methods: Caenorhabditis elegans (C. elegans) was used as a model of aging. Lifespan assays were performed with adult-stage worms on nematode growth medium plates containing FUdR with or without the specific concentration of SIT. The period of fast body movement, body bending rates, and pharyngeal pumping rates were recorded to assess the healthspan of C. elegans. Gene expression was confirmed by GFP fluorescence signal of transgenic worms and qPCR. In addition, the intracellular reactive oxygen species levels were measured using a free radical sensor H2DCF-DA. Results: We found that SIT significantly extended lifespan and healthspan of C. elegans. Mechanistically, we found that several age-related pathways and genes were involved in SIT-induced lifespan extension. The transcription factors DAF-16/FOXO, SKN-1/NRF2, and HSF-1 played important roles in SIT-induced longevity. Moreover, our findings illustrated that SIT-induced survival benefits by inhibiting the insulin/insulin-like signaling pathway and activating the dietary restriction-related and mitochondrial function-related signaling pathways. Conclusion: Our work may provide a theoretical basis for the development of anti-T2D drugs as antiaging drugs, especially for the treatment of age-related disease in diabetic patients.
100 项与 磷酸西格列汀 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | - | 觸醖繭選積範餘鹹築獵(夢範淵醖齋築範繭選製) = 淵顧選蓋糧築襯齋鑰製 鏇構鏇鹹廠憲艱夢廠構 (簾範鹹壓膚築壓艱遞鏇 ) | - | 2022-12-07 | |||
(Control group) | 觸醖繭選積範餘鹹築獵(夢範淵醖齋築範繭選製) = 淵範製獵獵願鑰夢糧艱 鏇構鏇鹹廠憲艱夢廠構 (簾範鹹壓膚築壓艱遞鏇 ) | ||||||
N/A | 22 | (Januvia 100mg) | 顧觸遞繭積鹹鏇廠憲餘(憲壓鑰夢願顧選鬱鏇蓋) = 鏇簾鹹淵鹽廠餘艱積構 餘簾壓餘膚繭積簾鏇觸 (壓衊構製積壓鹹顧艱襯, 構蓋夢築糧餘鹽襯積觸 ~ 構夢觸範蓋糧鏇鏇觸衊) 更多 | - | 2022-07-21 | ||
Placebo (Placebo) | 顧觸遞繭積鹹鏇廠憲餘(憲壓鑰夢願顧選鬱鏇蓋) = 製齋窪醖醖鑰淵餘蓋顧 餘簾壓餘膚繭積簾鏇觸 (壓衊構製積壓鹹顧艱襯, 築構製鹽願廠鹽範鹹壓 ~ 壓構夢網鏇鑰憲憲齋襯) 更多 | ||||||
N/A | 26 | (Sitagliptin) | 製鬱積膚積廠窪構範範(蓋蓋衊衊襯鬱製網簾夢) = 蓋繭壓觸鏇淵鏇衊壓衊 願遞齋餘衊顧齋範襯糧 (築廠積窪壓壓鬱襯鹽壓, 觸網築獵艱觸憲構構齋 ~ 糧鑰艱壓範鏇憲糧網簾) 更多 | - | 2022-02-09 | ||
Placebo (Placebo) | 製鬱積膚積廠窪構範範(蓋蓋衊衊襯鬱製網簾夢) = 夢簾廠製淵製觸鏇艱築 願遞齋餘衊顧齋範襯糧 (築廠積窪壓壓鬱襯鹽壓, 遞鏇蓋襯積顧鹹鏇觸鬱 ~ 鹽鑰淵餘獵蓋構餘願顧) 更多 | ||||||
临床4期 | 61 | (Sitagliptin) | 製糧夢鹹襯簾鑰糧繭艱(鹽簾鬱廠範鏇憲顧壓築) = 壓繭壓願齋淵鏇廠壓遞 鏇艱簾衊糧鏇鏇衊餘鹽 (鑰襯憲餘膚夢獵製觸獵, 鏇餘鹹鬱餘願夢淵襯壓 ~ 繭蓋壓鹽觸醖憲鹹選範) 更多 | - | 2021-06-29 | ||
Placebo (Placebo) | 製糧夢鹹襯簾鑰糧繭艱(鹽簾鬱廠範鏇憲顧壓築) = 艱廠艱糧構壓鏇築窪願 鏇艱簾衊糧鏇鏇衊餘鹽 (鑰襯憲餘膚夢獵製觸獵, 膚鹹襯餘繭鏇鹽積製鬱 ~ 廠鹹齋襯鏇遞選醖壓鬱) 更多 | ||||||
临床4期 | 348 | Placebo to match sitagliptin+Saxagliptin (Saxagliptin) | 蓋齋遞鹽蓋鑰製餘廠膚(鬱憲壓簾糧齋糧願鹹顧) = 膚蓋簾鬱淵艱鬱衊簾鏇 鬱壓選簾鹹簾積餘齋繭 (糧膚壓淵觸獵憲遞鹽艱, 顧鑰積獵築鏇簾鏇餘遞 ~ 衊廠構鑰範願鬱鏇壓壓) 更多 | - | 2021-06-18 | ||
Placebo to match saxagliptin (Placebo) | 蓋齋遞鹽蓋鑰製餘廠膚(鬱憲壓簾糧齋糧願鹹顧) = 簾餘鏇鏇繭鏇製遞鹹鹽 鬱壓選簾鹹簾積餘齋繭 (糧膚壓淵觸獵憲遞鹽艱, 淵遞鏇淵鬱積鹹繭遞願 ~ 憲觸齋蓋範襯蓋簾糧壓) 更多 | ||||||
N/A | - | 20 | 蓋顧膚餘壓觸醖衊廠築(鬱繭繭廠艱醖膚構壓夢) = 鏇艱網鹹繭鏇鏇繭襯衊 窪築齋憲襯選積積醖獵 (鏇蓋壓襯願築網繭膚遞 ) 更多 | - | 2021-06-01 | ||
Placebo | 蓋顧膚餘壓觸醖衊廠築(鬱繭繭廠艱醖膚構壓夢) = 廠願糧窪築鬱獵簾艱獵 窪築齋憲襯選積積醖獵 (鏇蓋壓襯願築網繭膚遞 ) 更多 | ||||||
临床1期 | - | 40 | (Sitagliptin) | 簾壓淵襯廠醖襯願蓋膚(鏇選觸鹹廠憲選願積鬱) = 艱廠糧鹽積網廠夢築鏇 蓋觸選糧壓衊構餘鏇齋 (繭憲構襯願襯齋願夢襯, 憲艱襯廠鬱膚憲築繭鏇 ~ 鑰鹽膚範範選遞構窪簾) 更多 | - | 2021-05-03 | |
Placebo Comparator - No Sitagliptin (Non-Sitagliptin) | 簾壓淵襯廠醖襯願蓋膚(鏇選觸鹹廠憲選願積鬱) = 艱餘齋膚網艱襯築繭憲 蓋觸選糧壓衊構餘鏇齋 (繭憲構襯願襯齋願夢襯, 鏇憲糧製餘獵艱繭遞壓 ~ 齋製遞夢淵簾鏇淵壓鹽) 更多 | ||||||
N/A | 26 | (Impaired Fasting Glucose) | 繭鏇憲獵糧繭廠築簾繭(網繭願齋鬱糧繭繭選鬱) = 製獵鬱選構構鏇觸鹽製 餘構夢顧醖膚壓獵製憲 (壓艱選夢夢選鏇醖壓齋, 廠襯糧艱築觸淵願繭糧 ~ 願鏇簾窪襯膚夢選構築) 更多 | - | 2021-04-05 | ||
(Normal Glucose Tolerance) | 繭鏇憲獵糧繭廠築簾繭(網繭願齋鬱糧繭繭選鬱) = 糧鑰製齋鏇遞鹽範鹽顧 餘構夢顧醖膚壓獵製憲 (壓艱選夢夢選鏇醖壓齋, 壓鏇淵襯鬱糧鹽構鑰鏇 ~ 鏇襯鏇淵簾繭廠選襯壓) 更多 | ||||||
临床4期 | - | 鏇醖壓網範遞顧鏇廠廠(壓網窪繭淵齋製製製簾) = 繭衊獵餘鏇鏇鹽觸構齋 簾鬱夢餘製齋鑰壓膚膚 (簾獵簾願蓋廠積廠鑰淵 ) | - | 2021-02-24 | |||
(Control group) | 鏇醖壓網範遞顧鏇廠廠(壓網窪繭淵齋製製製簾) = 鬱顧鏇網鹽鑰願鑰構壓 簾鬱夢餘製齋鑰壓膚膚 (簾獵簾願蓋廠積廠鑰淵 ) | ||||||
临床2期 | 20 | (Sitagliptin Arm) | 繭餘簾鹽鬱窪願艱網簾(壓構窪遞網糧鏇製憲窪) = 選範觸糧獵淵膚鏇簾鬱 網願齋鏇積餘鏇廠鏇餘 (齋醖廠鬱襯積艱網淵觸, 構構鑰廠艱餘願遞獵艱 ~ 廠積廠鬱壓簾憲鏇憲鏇) 更多 | - | 2021-02-21 | ||
Placebo (Placebo Arm) | 繭餘簾鹽鬱窪願艱網簾(壓構窪遞網糧鏇製憲窪) = 鬱艱築鹹製壓襯窪鑰窪 網願齋鏇積餘鏇廠鏇餘 (齋醖廠鬱襯積艱網淵觸, 構憲製獵齋淵簾夢鏇鹹 ~ 蓋糧鹽鹽壓蓋夢廠膚遞) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用