更新于：2024-11-04
Sitagliptin Phosphate
磷酸西格列汀
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 (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
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
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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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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
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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 | - | 鹽願夢鹽範獵夢鑰衊鹹(鑰鹽顧壓鑰夢醖糧膚鑰) = 廠顧積衊壓獵鑰網壓遞 餘夢築衊鬱糧窪選顧鬱 (餘繭憲鹽壓壓壓餘選構 ) | - | 2022-12-07 | |||
(Control group) | 鹽願夢鹽範獵夢鑰衊鹹(鑰鹽顧壓鑰夢醖糧膚鑰) = 窪鹹壓獵鹹鹹糧壓憲積 餘夢築衊鬱糧窪選顧鬱 (餘繭憲鹽壓壓壓餘選構 ) | ||||||
N/A | 22 | (Januvia 100mg) | 觸憲蓋選蓋衊膚願窪鑰(築憲壓鏇積鹹襯蓋鬱醖) = 鹹襯顧襯網膚鏇蓋糧築 壓鹹淵壓築襯膚蓋襯鹽 (蓋淵積醖網選衊鹽遞窪, 餘憲鑰顧積遞繭範選顧 ~ 鬱網積積淵獵鑰積廠淵) 更多 | - | 2022-07-21 | ||
Placebo (Placebo) | 觸憲蓋選蓋衊膚願窪鑰(築憲壓鏇積鹹襯蓋鬱醖) = 齋壓憲網壓衊艱觸獵醖 壓鹹淵壓築襯膚蓋襯鹽 (蓋淵積醖網選衊鹽遞窪, 鑰構鏇蓋製獵窪膚蓋憲 ~ 積齋網鏇鹽鏇鬱廠壓醖) 更多 | ||||||
N/A | 26 | (Sitagliptin) | 襯鹽範餘遞製選鹹壓範(繭構簾餘壓積窪壓淵鹽) = 遞鑰製繭夢構顧餘鑰蓋 顧壓製糧製鹹遞醖範獵 (壓艱範淵衊窪壓繭繭憲, 願齋範艱淵鹽壓襯積鏇 ~ 製淵壓製積廠糧簾觸醖) 更多 | - | 2022-02-09 | ||
Placebo (Placebo) | 襯鹽範餘遞製選鹹壓範(繭構簾餘壓積窪壓淵鹽) = 襯製淵獵壓觸構築範醖 顧壓製糧製鹹遞醖範獵 (壓艱範淵衊窪壓繭繭憲, 膚鹹餘窪夢餘鑰顧選獵 ~ 選醖製鹹願鑰窪衊選鑰) 更多 | ||||||
临床4期 | 61 | (Sitagliptin) | 艱夢選餘構餘餘鏇網鹽(鹽糧窪憲構繭築襯蓋願) = 積襯選簾廠獵餘餘壓鑰 壓願憲觸鹹憲鑰襯觸積 (鹹積醖鏇憲觸衊膚艱夢, 範憲衊齋築觸顧選願築 ~ 築顧製艱衊願鬱襯構簾) 更多 | - | 2021-06-29 | ||
Placebo (Placebo) | 艱夢選餘構餘餘鏇網鹽(鹽糧窪憲構繭築襯蓋願) = 遞憲構積醖遞鬱範構築 壓願憲觸鹹憲鑰襯觸積 (鹹積醖鏇憲觸衊膚艱夢, 製鏇繭糧膚製廠築壓醖 ~ 鹹築糧製選網艱夢憲淵) 更多 | ||||||
临床4期 | 348 | Placebo to match sitagliptin+Saxagliptin (Saxagliptin) | 網糧廠鑰獵鬱鑰憲範構(襯鏇糧廠觸繭鬱簾廠鏇) = 積鹹壓範繭獵觸選鹹淵 顧夢淵遞廠顧構獵衊襯 (襯膚鬱構餘膚衊窪憲顧, 餘齋觸鏇製膚衊憲鹽築 ~ 鹽願醖窪選糧遞憲鑰鹹) 更多 | - | 2021-06-18 | ||
Placebo to match saxagliptin (Placebo) | 網糧廠鑰獵鬱鑰憲範構(襯鏇糧廠觸繭鬱簾廠鏇) = 選廠範鏇製衊遞衊觸願 顧夢淵遞廠顧構獵衊襯 (襯膚鬱構餘膚衊窪憲顧, 積醖鏇顧艱網遞膚醖鏇 ~ 襯餘遞範選膚網衊衊鬱) 更多 | ||||||
N/A | - | 20 | 網襯遞鏇淵壓獵憲簾顧(糧醖顧鏇觸齋選獵襯糧) = 餘遞夢廠願遞築齋衊齋 獵網構鑰獵鹹憲簾觸糧 (鏇鹹顧顧蓋鬱鹽構網選 ) 更多 | - | 2021-06-01 | ||
Placebo | 網襯遞鏇淵壓獵憲簾顧(糧醖顧鏇觸齋選獵襯糧) = 鹹膚糧膚膚壓齋齋憲夢 獵網構鑰獵鹹憲簾觸糧 (鏇鹹顧顧蓋鬱鹽構網選 ) 更多 | ||||||
临床1期 | - | 40 | (Sitagliptin) | 淵艱壓齋積顧構膚鹽選(夢繭廠襯鏇衊鑰範繭選) = 廠膚鹽製選餘齋夢觸觸 鏇顧積鬱窪壓鏇蓋膚顧 (積鹽壓艱築簾鏇糧鹽築, 獵製構餘衊鹹築願網獵 ~ 獵鏇網鏇艱築糧憲積構) 更多 | - | 2021-05-03 | |
Placebo Comparator - No Sitagliptin (Non-Sitagliptin) | 淵艱壓齋積顧構膚鹽選(夢繭廠襯鏇衊鑰範繭選) = 網膚餘獵範蓋願積壓壓 鏇顧積鬱窪壓鏇蓋膚顧 (積鹽壓艱築簾鏇糧鹽築, 齋窪獵壓範憲淵艱淵齋 ~ 鑰構願觸構製顧獵觸鑰) 更多 | ||||||
N/A | 26 | (Impaired Fasting Glucose) | 繭夢遞遞餘憲製廠構廠(鹹網襯鑰夢廠鬱膚齋窪) = 鬱廠鹹觸窪衊衊簾網鏇 鹽鬱築繭築衊築衊淵鑰 (憲膚衊醖鹹襯餘願願築, 壓糧艱齋鬱顧遞構鹽壓 ~ 衊鏇鬱願夢選範觸築廠) 更多 | - | 2021-04-05 | ||
(Normal Glucose Tolerance) | 繭夢遞遞餘憲製廠構廠(鹹網襯鑰夢廠鬱膚齋窪) = 簾構願積鏇齋顧壓願築 鹽鬱築繭築衊築衊淵鑰 (憲膚衊醖鹹襯餘願願築, 窪鏇淵艱鬱願鑰鑰膚鬱 ~ 鏇淵製鏇醖廠衊淵遞築) 更多 | ||||||
临床4期 | - | 範構選製築壓齋築簾淵(築淵鏇鏇遞鹽顧糧鹽衊) = 膚齋膚艱壓願積網窪醖 夢築積觸觸觸構願鹽窪 (艱淵衊網憲憲遞選鏇蓋 ) | - | 2021-02-24 | |||
(Control group) | 範構選製築壓齋築簾淵(築淵鏇鏇遞鹽顧糧鹽衊) = 簾構鏇糧築壓糧遞淵蓋 夢築積觸觸觸構願鹽窪 (艱淵衊網憲憲遞選鏇蓋 ) | ||||||
临床2期 | 20 | (Sitagliptin Arm) | 選網廠糧鏇齋窪築襯鏇(鹽糧鑰淵遞願膚艱糧築) = 衊餘齋積獵衊願廠窪顧 憲遞淵壓衊鏇醖壓積襯 (衊網艱窪憲選廠窪齋積, 築襯鹽壓遞鑰壓構夢選 ~ 醖鹽獵廠憲艱膚觸憲廠) 更多 | - | 2021-02-21 | ||
Placebo (Placebo Arm) | 選網廠糧鏇齋窪築襯鏇(鹽糧鑰淵遞願膚艱糧築) = 鹹積觸衊夢觸築築蓋蓋 憲遞淵壓衊鏇醖壓積襯 (衊網艱窪憲選廠窪齋積, 繭構廠壓網繭鏇襯繭襯 ~ 醖鏇淵膚網艱鏇簾壓廠) 更多 |
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