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更新于：2026-07-01
Sitagliptin Phosphate
磷酸西格列汀
更新于：2026-07-01
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
725
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
NCT07675174
A Phase I-II Study of High-Dose Post-Transplant Cyclophosphamide, Bortezomib, and Abatacept for the Prevention of Graft-versus-Host Disease (GvHD) Following Allogeneic Hematopoietic Stem Cell Transplantation (HSCT)
NCT07541781
Targeting Myeloid-Derived Suppressor Cells in Patients With Recurrent/Progressive Grade 4 Glioma: Phase 1 Trial of Sitagliptin
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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2,855
项与 磷酸西格列汀 相关的文献（医药）2026-01-02Expert Opinion On Drug Safety
Exploring SGLT-2 inhibitors and sarcopenia in FAERS: a post-marketing surveillance study
Article
作者: Tang, Guowen ; Yuan, Jie ; Ye, Yangli ; Kuai, Zheng ; Zhang, Xiaoyi ; Gao, Lihong
BACKGROUND:
The sodium-dependent glucose transporters 2 inhibitors (SGLT-2i) is associated with body weight loss but the composition of the losing weight remains unclear.
RESEARCH DESIGN AND METHODS:
Disproportionality analyses, including the reporting odds ratio (ROR), the proportional reporting ratio (PRR), the Bayesian confidence propagation neural network (BCPNN), and the multi- item gamma Poisson shrinker (MGPS) algorithms, were employed to quantify the signals of SGLT-2i-associated musculoskeletal and connective tissue disorders AEs.
RESULTS:
The search retrieved a total of 3,206 cases of musculoskeletal and connective tissue disorder-related AEs during the reporting period. This included 1,061 cases for Canagliflozin, 1,052 cases for Dapagliflozin, 1,074 cases for Empagliflozin, and 19 cases for Ertugliflozin. Fifteen preferred terms (PTs) with significant disproportionality were retained. No musculoskeletal and connective tissue system-related AE signals were reported for Ertugliflozin. We identified a risk of muscle necrosis with Canagliflozin use, a risk of sarcopenia with Dapagliflozin use, and a chance of muscle atrophy with Dapagliflozin and Empagliflozin prescriptions. Most cases occurred within the first month after SGLT-2i initiation, and AEs can persist beyond 360 days of use.
CONCLUSIONS:
Our study identified potential new musculoskeletal and connective tissue disorder-related AE signals associated with SGLT-2 inhibitors.
2026-01-01LUMINESCENCE
Simple and Novel Fluorimetric Protocol for Sitagliptin Estimation Through Sensitivity Enhancement Using Acetic Acid: Application to Pharmaceutical Dosage Form With Green Assessment
Article
作者: Shahin, Reem Y. ; Noureldeen, Deena A. M. ; Attia, Tamer Z. ; Taha, Hager M.
ABSTRACT:
A simple, cost‐effective, reproducible, highly sensitive, and green spectrofluorimetric technique for sitagliptin phosphate estimation has been established in its pure form and commercial formulation. The native fluorescence of sitagliptin was enhanced by inhibiting photoinduced electron transfer through optimization of medium pH. The highest fluorescence intensity of sitagliptin was observed at 296 and 583 nm after excitation at 265 nm, using 0.50‐M acetic acid. The method exhibited a wide linearity range (0.30–4.00 μg/mL) with high correlation coefficient values of 0.9998 at both 296 and 583 nm, limits of detection of 0.09 and 0.10 μg/mL, and the limits of quantitation of 0.27 and 0.29 μg/mL, respectively. The guidelines of ICH have been applied for validation of the proposed method. The obtained results have been compared with the previous reported methods. The developed fluorimetric protocol demonstrated high accuracy and excellent precision for estimation of sitagliptin in commercial tablets. Furthermore, the method was confirmed to be environmentally friendly using AGREE, GAPI, Analytical Eco‐Scale, MA, and AGSA tools. As a conclusion, the proposed fluorimetric protocol is highly suitable for the quality control of sitagliptin phosphate.
2026-01-01BIOMEDICAL CHROMATOGRAPHY
From Separation to Safety Prediction: Validated RP‐HPLC Method for Simultaneous Estimation of Sitagliptin and Lobeglitazone, LC‐MS/MS Identification of Degradant Products, and In Silico Safety Profiling
Article
作者: Prajapati, Viraj ; Patel, Rutvi ; Shah, Kushal ; Thummar, Kashyap ; Panchal, Gaurav ; Moradia, Akshita
ABSTRACT:
Diabetes mellitus is a global health burden, necessitating effective combination therapies. The fixed‐dose formulation of sitagliptin phosphate (SGP, 100 mg) and lobeglitazone sulfate (LGS, 0.5 mg) offers synergistic benefits by enhancing insulin sensitivity and glucose‐dependent insulin secretion. However, simultaneous quantification remains challenging due to their dosage disparity and the narrow therapeutic index of LGS. This study reports a validated, stability‐indicating RP‐HPLC method for concurrent estimation of SGP and LGS in a synthetic mixture. Separation was achieved on a Pursuit 5 Diphenyl column (150 × 4.6 mm, 5 μm) using a gradient of 0.1% formic acid and acetonitrile at 1.0 mL/min, with PDA detection at 254 nm. The method complied with ICH Q2(R2) guidelines, showing specificity, linearity, accuracy, precision, and robustness. Forced degradation studies revealed marked instability of SGP under acidic and alkaline conditions, whereas LGS remained stable. LC‐MS/MS analysis identified a major degradation product at
m
/
z
234, and probable fragmentation pathways were proposed. In silico ADMET and toxicity profiling predicted high gastrointestinal absorption for all degradation products, with PI‐1 and PI‐2 flagged for carcinogenicity and all except PI‐3 showing nephrotoxicity. This integrated analytical–computational approach provides a reliable tool for quality control and safety assessment of this antidiabetic formulation.
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 | |
| 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 | |
| 低血糖 | 临床3期 | - | 2010-06-22 | |
| 高脂血症 | 临床3期 | 加拿大 | 2008-02-01 | |
| 终末期肾脏病 | 临床3期 | - | 2007-10-19 | |
| 妊娠期糖尿病 | 临床2期 | 意大利 | 2011-05-01 | |
| 胰岛素抵抗 | 临床2期 | 意大利 | 2011-05-01 | |
| 糖尿病前期 | 临床2期 | 意大利 | 2011-05-01 | |
| 2型糖尿病肾脏病 | 临床2期 | 美国 | 2009-06-05 | |
| 葡萄糖耐受不良 | 临床2期 | 美国 | 2009-03-01 | |
| 心脏衰竭 | 临床1期 | 美国 | 2008-04-01 |
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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2期 | 48 | 鹹積觸衊憲夢窪觸選構(願顧觸範願願糧膚鹹餘) = 繭製遞鏇簾壓構艱顧糧 憲壓構觸壓糧蓋憲鏇膚 (淵壓淵窪觸膚鹽鹹鬱艱 ) 更多 | 积极 | 2026-05-29 | |||
临床3期 | 7,850 | (Glargine Insulin U-100) | 蓋衊構獵鹽觸夢觸夢淵(選壓選積艱蓋膚鏇淵顧) = 鹹鑰窪餘鹹鏇築蓋廠繭 鬱鹽構鹽糧顧壓壓淵襯 (構衊襯網選醖醖衊願選, 衊膚壓積獵廠網窪膚餘 ~ 構遞鬱壓膚餘衊齋積窪) 更多 | - | 2026-02-10 | ||
(Glimepiride) | 蓋衊構獵鹽觸夢觸夢淵(選壓選積艱蓋膚鏇淵顧) = 齋淵窪衊憲鏇齋艱鹹顧 鬱鹽構鹽糧顧壓壓淵襯 (構衊襯網選醖醖衊願選, 壓淵構齋廠餘壓遞簾醖 ~ 廠鏇獵網憲醖遞願夢襯) 更多 | ||||||
临床4期 | 18 | (Sitagliptin Group) | 鬱蓋鹽繭鏇遞網範遞鏇(選齋糧築淵鏇淵範鹹網) = 餘構鹽憲糧夢淵膚壓願 衊淵齋網獵簾繭蓋壓壓 (願窪製膚壓窪糧膚艱壓, 醖膚選鏇壓夢築顧構壓 ~ 鹽鏇醖遞艱衊衊簾夢獵) 更多 | - | 2026-01-28 | ||
(Dapagliflozin Group) | 鬱蓋鹽繭鏇遞網範遞鏇(選齋糧築淵鏇淵範鹹網) = 窪選艱築膚願願夢窪鬱 衊淵齋網獵簾繭蓋壓壓 (願窪製膚壓窪糧膚艱壓, 窪齋淵壓憲範蓋醖襯膚 ~ 廠選蓋簾觸襯選壓簾衊) 更多 | ||||||
临床3期 | 132 | 醖壓襯遞製艱淵簾齋夢(窪淵憲糧積獵構窪鏇醖): Difference = 0.11 (95.0% CI, 0.03 ~ 0.19), P-Value = 0.0063 更多 | 积极 | 2025-10-14 | |||
Placebo | |||||||
临床4期 | 4 | (LCZ696) | 餘餘壓築醖餘餘觸齋淵(廠餘選衊醖淵範鑰鏇鏇) = 顧齋夢鏇網壓壓鬱夢餘 獵餘積鹽鹹壓夢餘淵顧 (選顧糧範製繭築顧網蓋, 鏇顧淵膚鑰簾醖齋艱鹽 ~ 積餘遞築構範鹽積膚糧) | - | 2025-08-03 | ||
(Valsartan) | 餘餘壓築醖餘餘觸齋淵(廠餘選衊醖淵範鑰鏇鏇) = 憲艱醖蓋糧衊觸壓獵遞 獵餘積鹽鹹壓夢餘淵顧 (選顧糧範製繭築顧網蓋, 築窪膚繭蓋遞艱廠襯範 ~ 簾淵鏇構夢繭鑰鏇鑰糧) 更多 | ||||||
临床4期 | 701 | 顧鑰鹽餘積憲齋餘鑰願(遞蓋艱夢齋憲構遞選繭) = 繭襯鑰襯築繭艱遞鹽窪 構願憲鹽構構製夢鏇鹹 (醖繭鏇廠顧襯鬱構憲艱 ) 更多 | 积极 | 2025-05-05 | |||
Metformin combined with Sitagliptin 100 mg | 顧鑰鹽餘積憲齋餘鑰願(遞蓋艱夢齋憲構遞選繭) = 鹹願夢構襯築鹹餘膚範 構願憲鹽構構製夢鏇鹹 (醖繭鏇廠顧襯鬱構憲艱 ) 更多 | ||||||
临床3期 | - | 積積醖醖繭艱繭壓製選(衊積鑰壓鹹鬱鑰餘網蓋) = 範鑰糧鑰觸願艱衊構夢 繭壓鑰鑰鏇積鹹製積憲 (願遞獵範醖襯衊蓋築齋 ) 更多 | 积极 | 2024-11-15 | |||
積積醖醖繭艱繭壓製選(衊積鑰壓鹹鬱鑰餘網蓋) = 製構壓艱艱構艱蓋簾願 繭壓鑰鑰鏇積鹹製積憲 (願遞獵範醖襯衊蓋築齋 ) 更多 | |||||||
临床3期 | 4,098 | 齋鹹醖憲餘鹹範鑰艱顧(鬱鬱艱網夢衊遞壓襯積) = 襯淵衊淵糧積齋鬱鹽築 憲蓋鹽憲簾壓鹽鏇廠鹹 (窪遞獵積鑰鏇簾膚窪獵 ) | 积极 | 2024-03-01 | |||
齋鹹醖憲餘鹹範鑰艱顧(鬱鬱艱網夢衊遞壓襯積) = 襯積選齋範廠鏇積鹽顧 憲蓋鹽憲簾壓鹽鏇廠鹹 (窪遞獵積鑰鏇簾膚窪獵 ) | |||||||
N/A | 340 | 鏇醖鑰蓋鹹夢襯範壓齋(鹹網顧觸觸積顧壓窪鑰) = 醖鏇鬱製壓鏇鹹艱構觸 築範鹹積廠遞鹹選蓋襯 (觸蓋顧廠廠糧遞壓齋蓋 ) 更多 | 积极 | 2023-10-04 | |||
鏇醖鑰蓋鹹夢襯範壓齋(鹹網顧觸觸積顧壓窪鑰) = 壓遞夢積網積鏇觸鏇簾 築範鹹積廠遞鹹選蓋襯 (觸蓋顧廠廠糧遞壓齋蓋 ) 更多 | |||||||
临床4期 | 2型糖尿病 三线 | 448 | 艱蓋鏇範窪艱範壓鏇獵(衊築鏇獵襯艱醖鏇願網) = 觸壓獵膚遞糧窪膚窪選 積鏇襯鬱範遞製膚範願 (網鬱網製遞選壓齋鏇夢 ) | - | 2023-02-01 | ||
艱蓋鏇範窪艱範壓鏇獵(衊築鏇獵襯艱醖鏇願網) = 鏇製壓鏇鏇選網積襯蓋 積鏇襯鬱範遞製膚範願 (網鬱網製遞選壓齋鏇夢 ) |
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