安奈格列汀(Anagliptin) - 药物靶点：DPP-4_在研适应症：2型糖尿病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Anagliptin (JAN/INN)、Beskoa

+ [3]

靶点

DPP-4

作用机制

DPP-4抑制剂(二肽基肽酶IV抑制剂)

治疗领域

内分泌与代谢疾病

在研适应症

2型糖尿病

非在研适应症

非胰岛素依赖型糖尿病2

原研机构

Sanwa Kagaku Kenkyusho Co., Ltd.

在研机构

Sanwa Kagaku Kenkyusho Co., Ltd.

非在研机构

Kowa Research Institute, Inc.

JW PHARMACEUTICAL Corp.

最高研发阶段批准上市

首次获批日期

日本 (2012-09-28),

2型糖尿病

最高研发阶段(中国)-

特殊审评特殊审批 (中国)

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结构

分子式C19H25N7O2

InChIKeyLDXYBEHACFJIEL-HNNXBMFYSA-N

CAS号739366-20-2

关联

44

项与安奈格列汀相关的临床试验

JPRN-jRCTs031200366 / Not yet recruitingN/AIIT

Safety of Anagliptin and MEtformin combination tablets evaluated by non-inferiority between pre- and post-serum Lactate levels In Japanese patients Of type 2 diabetes and moderate renal impairment - AMELIO STUDY

开始日期2021-05-18

申办/合作机构-

JPRN-UMIN000041979 / Completed

Effects of anagliptin / metformin hydrochloride combination tablets in patients with type 2 diabetes: a retrospective observational study - Effects of anagliptin / metformin hydrochloride combination tablets in patients with type 2 diabetes: a retrospective observational study

开始日期2020-09-01

申办/合作机构-

JPRN-UMIN000040960 / CompletedN/AIIT

Effect of switch from metformin / vildagliptin fixed-dose combination tablet to metformin / anagliptin fixed-dose combination tablet - Effect of switch from metformin / vildagliptin fixed-dose combination tablet to metformin / anagliptin fixed-dose combination tablet

开始日期2020-02-01

申办/合作机构-

100 项与安奈格列汀相关的临床结果

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100 项与安奈格列汀相关的转化医学

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100 项与安奈格列汀相关的专利（医药）

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103

项与安奈格列汀相关的文献（医药）

2024-07-12·Medicine

Role of anagliptin, a dipeptidyl peptidase-4 inhibitor, in managing type 2 diabetes: A systematic review and meta-analysis

Review

作者: Dutta, Deep ; Patra, Shinjan ; Bhattacharya, Saptarshi ; Sharma, Meha ; Kamrul-Hasan, A.B.M. ; Nagendra, Lakshmi

Background:No comprehensive meta-analysis has examined and consolidated the effectiveness and safety of anagliptin in treating type 2 diabetes mellitus (T2D). To bridge this knowledge gap, we undertook this meta-analysis.Methods:Randomized controlled trials involving patients with T2D receiving anagliptin were sought after through electronic databases. The control arm consisted of either an active comparator (active control group [ACG]) or a placebo (passive control group [PCG]). The primary outcome was glycated hemoglobin (HbA1c), with secondary outcomes including fasting plasma glucose (FPG) and lipid profiles and adverse events.Results:From the 226 articles first examined, 10 randomized controlled trials with 970 participants were analyzed. Reductions in HbA1c (mean difference [MD]: −0.03%, 95% confidence interval [CI]: −0.14 to 0.14, P = .51, I2 = 9%) and FPG (MD: 0.03 mmol/L, 95% CI: −0.30 to 0.35, P = .87, I2 = 42%) were similar in the anagliptin group and ACG. Anagliptin reduced FPG better than placebo (MD: −1.25 mmol/L, 95% CI: −1.87 to −0.64, P < .0001, I2 = 0%). Sufficient data were unavailable to analyze the HbA1c lowering with anagliptin versus placebo. Among the lipid parameters, changes in total cholesterol, high-density lipoprotein cholesterol, apolipoprotein B48, and apolipoprotein B100 were identical between the anagliptin and control groups (PCG and ACG). Anagliptin was better than ACG at lowering low-density lipoprotein cholesterol but not as good at lowering triglyceride. Adverse events were infrequent and similar in the anagliptin and control groups (PCG and ACG).Conclusion:Anagliptin positively affects glucose control and is safe for managing T2D. Its low-density lipoprotein cholesterol-lowering effect warrants further investigation.

2024-06-01·Diabetes, Obesity and Metabolism

Dipeptidyl peptidase‐4 inhibitor and sodium‐glucose cotransporter 2 inhibitor additively ameliorate hepatic steatosis through different mechanisms of action in high‐fat diet‐fed mice

Article

作者: Shimoda, Masashi ; Nogami, Yuka ; Kaku, Kohei ; Dan, Kazunori ; Mune, Tomoatsu ; Nakanishi, Shuhei ; Fushimi, Yoshiro ; Kimura, Tomohiko ; Kaneto, Hideaki ; Shirakiya, Yoshiko ; Sanada, Junpei ; Katakura, Yukino ; Iwamoto, Hideyuki ; Iwamoto, Yuichiro

AbstractAimDipeptidyl peptidase‐4 (DPP‐4) inhibitors suppress the inactivation of incretin hormones and lower blood glucose levels by inhibiting DPP‐4 function. Sodium‐glucose cotransporter 2 (SGLT2) inhibitors lower blood glucose levels in an insulin‐independent manner by inhibiting renal reabsorption of glucose. DPP‐4 and SGLT2 inhibitors each have the potential to improve hepatic steatosis; however, their combined effects remain unclear. In this study, we examined the effects of the combination of these drugs on hepatic steatosis using high‐fat diet‐fed mice.MethodC57BL/6J male mice were fed a 60% high‐fat diet for 2 months to induce hepatic steatosis. Mice were divided into four groups (control; DPP‐4 inhibitor anagliptin; SGLT2 inhibitor luseogliflozin; anagliptin and luseogliflozin combination), and the effects of each drug and their combination on hepatic steatosis after a 4‐week intervention were evaluated.ResultsThere were no differences in blood glucose levels among the four groups. Anagliptin suppresses inflammation‐ and chemokine‐related gene expression. It also improved macrophage fractionation in the liver. Luseogliflozin reduced body weight, hepatic gluconeogenesis and blood glucose levels in the oral glucose tolerance test. The combination treatment improved hepatic steatosis without interfering with the effects of anagliptin and luseogliflozin, respectively, and fat content and inflammatory gene expression in the liver were significantly improved in the combination group compared with the other groups.ConclusionThe combination therapy with the DPP‐4 inhibitor anagliptin and the SGLT2 inhibitor luseogliflozin inhibits fat deposition in the liver via anti‐inflammatory effects during the early phase of diet‐induced liver steatosis.

2024-01-19·Biological and Pharmaceutical Bulletin

Effect of Anagliptin on Vascular Injury in the Femoral Artery of Type 2 Diabetic Rats

Article

作者: Matsunaga, Tamihide ; Takeuchi, Masayoshi ; Hori, Eisei ; Nagami, Chie ; Kikuchi, Chigusa ; Iwao, Takahiro ; Noda, Masato

Patients with diabetes mellitus (DM) often experience complications such as peripheral arterial disease (PAD), which is thought to be caused by vascular damage resulting from increased oxidative stress. Dipeptidyl peptidase-4 inhibitors have been reported to reduce oxidative stress, although the exact mechanism remains unclear. This study aimed to investigate the impact of long-term (6 weeks) anagliptin treatment at a dose of 200 mg/kg/d against oxidative stress in the femoral artery of Otsuka Long-Evans Tokushima Fatty (OLETF) rats using a well-established animal model for type 2 DM. Serum toxic advanced glycation end-products concentrations and blood glucose levels after glucose loading were significantly elevated in OLETF rats compared to Long-Evans Tokushima Otsuka (LETO) rats but were significantly suppressed by anagliptin administration. Plasma glucagon-like peptide-1 concentrations after glucose loading were significantly increased in anagliptin-treated rats. Superoxide production and reduced nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activity in femoral arteries were significantly increased in OLETF rats compared to LETO rats but were significantly decreased by anagliptin administration. The expressions of NADPH oxidase components (p22^phox in the intima region and p22^phox and gp91^phox in the media region) in the femoral artery were significantly increased in OLETF rats compared to LETO rats but were significantly suppressed by anagliptin administration. Furthermore, the femoral artery showed increased wall thickness in OLETF rats compared to LETO rats, but anagliptin administration reduced the thickening. This study suggests that long-term anagliptin administration can reduce oxidative stress in femoral arteries and improve vascular injury.

100 项与安奈格列汀相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D09780	安奈格列汀	A10BH	DB12417

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
2型糖尿病	日本	Sanwa Kagaku Kenkyusho Co., Ltd.	2012-09-28

未上市

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适应症	最高研发状态	国家/地区	公司	日期
非胰岛素依赖型糖尿病2	临床前	韩国	JW PHARMACEUTICAL Corp.	2011-05-01
2型糖尿病	临床前	韩国	JW PHARMACEUTICAL Corp.	2009-02-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02330406 (REASON, Pubmed \| Cardiovasc Diabetol)	临床4期	2型糖尿病	353	Anagliptin	襯獵窪範網襯廠繭齋醖(鹹憲淵獵窪獵膚觸願艱) = 壓鹹艱鑰鏇餘築觸壓積窪醖積簾衊築構願鹽衊 (襯廠積蓋範窪鹽選淵艱 )	-	2019-11-16
				Sitagliptin	襯獵窪範網襯廠繭齋醖(鹹憲淵獵窪獵膚觸願艱) = 製鬱鹹選選鏇觸糧觸鬱窪醖積簾衊築構願鹽衊 (襯廠積蓋範窪鹽選淵艱 )
NCT02330406 (REASON, Pubmed)	临床4期	糖尿病	380	Anagliptin	(鏇鹽壓廠窪壓選鹹鏇齋) = 壓餘築網積鹹簾構網鏇製鹹製範壓網襯膚鹽鹹 (憲衊衊鑰積艱餘廠觸範 ) 更多	积极	2019-06-12
				Sitagliptin	(鏇鹽壓廠窪壓選鹹鏇齋) = 艱艱鹹醖夢遞夢廠鏇獵製鹹製範壓網襯膚鹽鹹 (憲衊衊鑰積艱餘廠觸範 ) 更多
NCT01529541 (Pubmed \| Diabetes Obes Metab) 人工标引	临床3期	2型糖尿病	180	Anagliptin	(鏇鏇鬱餘鹽願蓋廠糧壓) = 鬱繭鬱獵衊壓觸選鬱壓膚艱網憲鏇遞遞鬱鬱製 (膚願顧積糧範醖鏇鑰築, 0.70)	非劣	2015-05-01
				sitagliptin	(鏇鏇鬱餘鹽願蓋廠糧壓) = 鹽鏇醖膚積廠網築鏇製膚艱網憲鏇遞遞鬱鬱製 (膚願顧積糧範醖鏇鑰築, 0.61)