更新于：2024-06-20
Saxagliptin Hydrochloride/Metformin Hydrochloride
盐酸沙格列汀/盐酸二甲双胍
更新于：2024-06-20
概要
基本信息
药物类型 小分子化药 |
别名 METFORMIN HYDROCHLORIDE/SAXAGLIPTIN HYDROCHLORIDE、SAXAGLIPTIN/METFORMIN HYDROCHLORIDE、Kombiglyze Xr + [2] |
作用机制 DPP-4抑制剂(二肽基肽酶IV抑制剂)、PRKAB1激活剂(腺苷酸活化蛋白激酶亚基β1激活剂) |
治疗领域 |
在研适应症 |
非在研适应症- |
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2010-11-05), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C22H38Cl2N8O2 |
InChIKeyGTSUONGZHGBCPP-ZEGDOHPJSA-N |
CAS号1431862-06-4 |
关联
23
项与 盐酸沙格列汀/盐酸二甲双胍 相关的临床试验沙格列汀二甲双胍缓释片（I）在中国成年健康受试者中的一项单中心、随机、开放、空腹和餐后单次给药、两制剂、两序列、两周期交叉的生物等效性研究
沙格列汀二甲双胍缓释片（Ⅰ）在健康受试者中的单次给药、随机、开放、两周期、双交叉、空腹及餐后状态下的生物等效性研究
沙格列汀二甲双胍缓释片（Ⅰ）在健康人群中的生物等效性试验
100 项与 盐酸沙格列汀/盐酸二甲双胍 相关的临床结果
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100 项与 盐酸沙格列汀/盐酸二甲双胍 相关的转化医学
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100 项与 盐酸沙格列汀/盐酸二甲双胍 相关的专利（医药）
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4
项与 盐酸沙格列汀/盐酸二甲双胍 相关的文献（医药）2018-10-01JGH open : an open access journal of gastroenterology and hepatology
Kombiglyze (metformin and saxagliptin)‐induced hepatotoxicity in a patient with non‐alcoholic fatty liver disease
作者: Mun, Kein Seong ; Thalha, Abdul Malik ; Boon Tan, Alexander Tong ; Mahadeva, Sanjiv
A 33‐year‐old man was referred with hyperosmotic symptoms of 4 weeks. Clinical examination showed palpable hepatomegaly and no stigmata of liver disease. Findings were random glucose 16.6 mmol/L, HbA1c 12.4%, triglyceride 6.2 mmol/L, normal LFTs and ultrasound liver: increased echogenicity. Management consisted of dietician referral and commencement of metformin 500 mg bd, diamicron MR 60 mg od, and fenofibrate 145 mg od. He was non‐compliant, complaining of “heaviness of head” after consuming oral diabetic agents, without symptoms of hypoglycemia. Treatment was switched to Kombiglyze XR (saxaglipitin 5 mg + metformin 1000 mg) and empagliflozin 25 mg od. He presented 1 week later with generalised pruritus with ALT 307 IU/L and serum GGT 808 IU/L. Following this, a percutaneous liver biopsy was performed, revealing steatohepatitis and marked intra‐hepatic cholestasis. Kombiglyze XR was withheld, with resolution of LFTs to baseline. Phenotypes of liver injury are categorised according to R value, defined as ratio ALT/ULN:ALP/ULN. R value of ≥5:hepatocellular injury, ≤2:cholestatic injury, 2–5:mixed‐type injury. Here, R value points toward mixed type (R = 3.203). Hepatotoxicity in patients with NASH is difficult to diagnose, based on laboratory parameters. Liver histology was useful in indicating additional changes apart from NASH, causing liver derangement. The Rousal Uclaf Causality Assessment Method is a scoring method to determine the probability of drug induced liver injury. RUCAM score for this case was 6 (probable adverse drug reaction). Hepatotoxicity from saxagliptin not been reported prior. Clinicians need to be more vigilant, particularly in patients with NASH.
2016-06-01The Journal of clinical endocrinology and metabolism2区 · 医学
Combination of Saxagliptin and Metformin Is Effective as Initial Therapy in New-Onset Type 2 Diabetes Mellitus With Severe Hyperglycemia
2区 · 医学
Article
作者: Fogelfeld, Leon ; Amblee, Ambika ; Lious, Daniel
CONTEXT:
The efficacy/safety of combination oral agents in those with stable newly diagnosed type 2 diabetes (T2DM) with severe hyperglycemia is unknown.
OBJECTIVE:
The objective of the study was to assess glycemic and β-cell outcomes of two oral regimens.
DESIGN:
This was an open-label, randomized controlled trial with patients enrolled from 2011 through 2014 and followed up for 12 weeks.
SETTING:
The study was conducted at a major public hospital in Chicago.
PATIENTS:
One hundred adults with newly diagnosed T2DM and severe hyperglycemia (300-450 mg/dL) participated in the study.
INTERVENTION:
One hundred patients were randomized to receive Kombiglyze XR (saxagliptin 5 mg/metformin 2000 mg) daily (K group) vs glipizide XL 10 mg daily (G group).
MAIN OUTCOME MEASURES:
The measure was to maintain fasting/premeal glucose of less than 300 mg/dL up to 6 weeks and less than 250 mg/dL after 6 weeks until study end, and to have no return acute care-site visits. Those not meeting criteria were discontinued. Other outcomes included continuous glucose monitoring (CGM) and β-cell function estimates at start and study end.
RESULTS:
Baseline characteristics and primary outcome (K group 94%, G group 98%) were similar in both groups. The enrollment glucose (K group 343 mg/dL, G group 341 mg/dL) and glycated hemoglobin (K group 10.8%, G group 11%) declined by week 12 (K group 137 mg/dL, G group 129 mg/dL, and K group 6.8%, G group 6.9%), respectively. Homeostasis model assessment to assess basal insulin secretion and early insulin response improved severalfold (K group ×5.8, G group ×5.9, and K group ×9.5, G group ×13.1). In follow-up, the incidence of hypoglycemia was lower in the K group (self-monitored blood glucose: K group 8.0%, G group 24%; CGM: K group 20%, G group 46.5%) as were the number of episodes of hypoglycemia (self-monitored blood glucose: K group 4 in 12 weeks, G group 27 in 12 weeks; CGM: K group 0.28 per 24 h, G group 0.31 per 24 h).
CONCLUSIONS:
Kombiglyze XR and glipizide XL are efficacious in improving glycemia and β-cell function in stable newly diagnosed T2DM with severe hyperglycemia. The K group had less hypoglycemia. These results suggest that certain oral medications could be appropriate alternatives in treating severe hyperglycemia.
2012-03-01Expert review of endocrinology & metabolism
Saxagliptin plus metformin combination therapy
Article
作者: Scheen, André J
Metformin is considered to be the first-line drug therapy for the management of Type 2 diabetes. Incretin-based therapies, and especially dipeptidyl peptidase-4 inhibitors, offer new opportunities after failure of metformin. An extensive literature search was performed to analyze all clinical trials combining saxagliptin with metformin. Saxagliptin and metformin may be administered together, either separately or in fixed-dose combination, as saxagliptin added to metformin or as an initial combination. Saxagliptin and metformin are not prone to pharmacokinetic drug-drug interactions and fixed-dose combination allows dosing of one single pill (Kombiglyze® XR) or two pills (Komboglyze®) per day. Both compounds exert pharmacodynamic complementary actions. Their coadministration improves blood glucose control (fasting plasma glucose, postprandial glucose and glycated hemoglobin) more potently than either compound separately. Tolerance is good without hypoglycemia, weight gain and further increase in metformin-related gastrointestinal adverse events. The combination saxagliptin plus metformin may be used as first-line or second-line therapy in the management of Type 2 diabetes.
100 项与 盐酸沙格列汀/盐酸二甲双胍 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
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 | 2010-11-05 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 38 | (Metformin XR) | 窪築網獵憲憲廠襯築襯(繭構蓋餘糧衊鑰簾製蓋) = 鬱願網範齋衊網遞獵衊 選鬱齋淵繭顧築簾齋淵 (憲餘製製衊遞襯襯夢製, 獵醖網餘壓蓋遞網蓋壓 ~ 艱蓋鹹糧鹹鏇餘積築壓) 更多 | - | 2017-06-28 | ||
(Saxagliptin) | 窪築網獵憲憲廠襯築襯(繭構蓋餘糧衊鑰簾製蓋) = 鬱顧衊鹹築憲廠壓鹽積 選鬱齋淵繭顧築簾齋淵 (憲餘製製衊遞襯襯夢製, 壓獵鏇遞襯鹹衊糧淵鏇 ~ 鑰鏇鬱繭鏇鬱鹹鹹蓋窪) 更多 | ||||||
临床1期 | 24 | saxagliptin+metformin (Treatment A) | 構糧膚蓋淵鑰夢餘積壓(鬱鹽網廠憲鏇構築憲鑰) = 製願蓋遞製膚鬱鑰襯蓋 範鹹淵艱衊遞網願構鹹 (鹹構夢窪襯簾窪艱積壓, 鏇齋襯選餘選顧選範艱 ~ 選簾繭鹹鏇築獵製範構) 更多 | - | 2012-02-08 | ||
saxagliptin+metformin (Treatment B) | 構糧膚蓋淵鑰夢餘積壓(鬱鹽網廠憲鏇構築憲鑰) = 淵顧窪遞夢餘製齋淵遞 範鹹淵艱衊遞網願構鹹 (鹹構夢窪襯簾窪艱積壓, 膚積構餘壓夢蓋積齋壓 ~ 遞獵顧遞衊夢憲繭繭願) 更多 |
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