更新于：2024-06-29
Supaglutide
苏帕鲁肽
更新于：2024-06-29
概要
基本信息
原研机构 |
非在研机构- |
最高研发阶段申请上市 |
首次获批日期- |
最高研发阶段(中国)申请上市 |
特殊审评- |
关联
11
项与 苏帕鲁肽 相关的临床试验依苏帕格鲁肽α注射液在饮食和运动干预后体重控制不佳的超重及肥胖受试者中多次皮下注射给药的安全性、耐受性、药代动力学和药效学特征的随机、双盲、安慰剂对照IIa期临床研究
一项在健康受试者中评价苏帕鲁肽注射液对地高辛片或盐酸二甲双胍片药代动力学影响的单中心、开放、固定序列临床研究
A Single-centre, Open Labeled, Fixed-sequence Study to Evaluate the Effect of Supaglutide on Digoxin or Metformin Pharmacokinetics
100 项与 苏帕鲁肽 相关的临床结果
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100 项与 苏帕鲁肽 相关的转化医学
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100 项与 苏帕鲁肽 相关的专利（医药）
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4
项与 苏帕鲁肽 相关的文献（医药）2022-08-01European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
Pharmacokinetic and pharmacodynamic studies of supaglutide in rats and monkeys
Article
作者: Liu, Lin ; Liao, Yijing ; Prud'homme, Gerald J ; Ma, Anran ; Zhang, Li ; Wang, Qinghua ; Wang, Zhihong ; Zhang, Na ; Zhou, Yue
We demonstrated recently that supaglutide, a novel GLP-1 mimetic generated by recombinant fusion protein techniques, exerted hypoglycemic effects in type 2 diabetes db/db mice and spontaneous diabetic monkeys. In this study, we investigated the pharmacokinetics and pharmacodynamics of supaglutide by single subcutaneous and intravenous injection(s) in rats and rhesus monkeys, as well as fourconsecutive subcutaneous injections in monkeys.We found the half-life (t1/2) of supaglutide was 39.7 h and 35.8 h at dosing 0.1 mg/kg upon subcutaneous or intravenous administration respectively, in rhesus monkeys. The plasma supaglutide peaked at 8-10 h, while the plasma drug exposure levels increased with the increase of dose, showing approximately a linear pharmacokinetic characteristic. The elimination kinetics (Ke) were found to be similar between subcutaneous (∼0.025 in rats and ∼0.018 in monkeys) and intravenous administration (0.021 in rats and 0.020 in monkeys), whereas the bioavailability was found to be 31.1% in rats and 63.9% in monkeys. In monkeys, a single dose injection of supaglutide markedly decreased the random blood glucose levels that reaching the maxima effects in 14-16 h, gradually recovered and returned to the baseline level approximately after 72 h. 125I-supaglutide was found mainly distributed in the serum and organs rich in blood supply. Urine was found to be the primary excretion route of supaglutide, following by feces, but mostly not in bile.Our results show that supaglutide possess linear pharmacokinetic characteristics associated with prolonged hypoglycemic effects inanimals,suggestinga potential weekly dosing therapeutic reagent for the treatment of type 2 diabetes and metabolic diseases.
2021-02-01The Journal of endocrinology3区 · 医学
Novel GLP-1 analog supaglutide improves glucose homeostasis in diabetic monkeys
3区 · 医学
Article
作者: Yang, Zhenyan ; Shao, Anna ; Liao, Yijing ; Jiang, Yaojing ; Zeng, Wen ; Zhou, Quanquan ; Tao, Weihong ; Huang, Xiaohang ; Li, Jia ; Zhao, Ying ; Ma, Anran ; Liang, Yinan ; Wang, Qinghua ; Zhang, Li ; Wu, Minglin ; Wang, Zhihong ; Yang, Zunyuan ; Cui, Qiaoli
Glucagon-like peptide 1 (GLP-1) is an insulinotropic hormone and plays an important role in regulating glucose homeostasis. GLP-1 has a short half-life (t1/2 < 2 min) due to degrading enzyme dipeptidyl peptidase-IV and rapid kidney clearance, which limits its clinical application as a therapeutic reagent. We demonstrated recently that supaglutide, a novel GLP-1 mimetic generated by recombinant fusion protein techniques, exerted hypoglycemic and β-cell trophic effects in type 2 diabetes db/db mice. In the present study, we examined supaglutide’s therapeutic efficacy and pharmacokinetics in diabetic rhesus monkeys. We found that a single subcutaneous injection of supaglutide of tested doses transiently and significantly reduced blood glucose levels in a dose-dependent fashion in the diabetic monkeys. During a 4-week intervention period, treatment of supaglutide of weekly dosing dose-dependently decreased fasting and random blood glucose levels. This was associated with significantly declined plasma fructosamine levels. The repeated administration of supaglutide remarkably also decreased body weight in a dose-dependent fashion accompanied by decreased food intake. Intravenous glucose tolerance test results showed that supaglutide improved glucose tolerance. The intervention also showed enhanced glucose-stimulated insulin secretion and improved lipid profile in diabetic rhesus monkeys. These results reveal that supaglutide exerts beneficial effects in regulating blood glucose and lipid homeostasis in diabetic rhesus monkeys.
Frontiers in physiology2区 · 医学
Novel GLP-1 Analog Supaglutide Reduces HFD-Induced Obesity Associated with Increased Ucp-1 in White Adipose Tissue in Mice
2区 · 医学
ArticleOA
作者: Bao, Xi ; Wang, Zhihong ; Wan, Yun ; Cui, Qiaoli ; Wang, Qinghua ; Jiang, Dongdong ; Liu, Wenjuan ; Liu, Rui ; Zhang, Xiangyu ; Huang, Jiabao
GLP-1, an important incretin hormone plays an important role in the regulation of glucose homeostasis. However, the therapeutic use of native GLP-1 is limited due to its short half-life. We recently developed a novel GLP-1 mimetics (supaglutide) by genetically engineering recombinant fusion protein production techniques. We demonstrated that this formulation possessed long-lasting GLP-1 actions and was effective in glycemic control in both type 1 and type 2 diabetes rodent models. Here, we investigated the effects of supaglutide in regulating energy homeostasis in obese mice. Mice were fed with high-fat diet (HFD) for 6 months to induce obesity and then subjected to supaglutide treatment (300 μg/kg, bi-weekly for 4 weeks), and placebo as control. Metabolic conditions were monitored and energy expenditure was assessed by indirect calorimetry (CLAMS). Cold tolerance test was performed to evaluate brown-adipose tissue (BAT) activities in response to cold challenge. Glucose tolerance and insulin resistance were evaluated by intraperitoneal glucose tolerance test and insulin tolerance tests. Liver and adipose tissues were collected for histology analysis. Expression of uncoupling protein 1(Ucp1) in adipose tissues was evaluated by Western blotting. We found that supaglutide treatment reduced body weight, which was associated with reduced food intake. Compared to the placebo control, supaglutide treatment improved lipid profile, i.e., significantly decreased circulating total cholesterol levels, declined serum triglyceride, and free fatty acid levels. Importantly, the intervention significantly reduced fatty liver, decreased liver triglyceride content, and concomitantly ameliorated liver injury exemplified by declined hepatic alanine aminotransferase (ALT) and aspartic transaminase (AST) content. Remarkably, supaglutide reduced hepatic lipid accumulation and altered morphometry in favor of small adipocytes in fat. This is consistent with the observation that supaglutide increased tolerance of the mice to cold environment associated with up-regulation of Ucp1 in the inguinal fat. Furthermore, supaglutide improved glucose tolerance, and insulin sensitivity in the obese mice suggesting improved glucose and energy homeostasis. Our findings suggest that supaglutide exerts beneficial effect on established obesity through reducing energy intake and is associated with brown remodeling of white adipose tissue.
研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 2型糖尿病 | 申请上市 | 中国 | 2023-09-27 | |
| 2型糖尿病 | 申请上市 | 中国 | 2023-09-27 | |
| 肥胖 | 临床2期 | 中国 | 2024-04-21 | |
| 非酒精性脂肪性肝炎 | 临床2期 | 美国 | - |
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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1期 | - | 32 | 憲憲壓衊蓋鹹繭範繭窪(顧積廠範願衊鹽獵觸壓) = the coadministration of supa injection had no effect on the AUC0-last of digoxin, a reduction in Cmax by about 24%, and an increase in the AUC0-inf by about 15% compared with that of the digoxin administration alone. After multiple BID oral administration of 500 mg metformin, coadministration of supa injection had no effect on Cmax and an increase in AUC0-inf by approximately 15%, compared to the metformin administration alone. 鹽網淵鹹製顧餘鏇壓鏇 (觸觸範選衊醖網壓餘衊 ) | 积极 | 2024-06-14 | ||
临床3期 | 297 | 齋淵繭餘襯簾廠遞齋觸(製淵網襯淵觸繭鑰醖醖) = 遞願範簾壓憲遞鏇壓淵 鹽窪窪築憲構糧艱淵繭 (製齋餘觸餘積醖夢膚齋, -1.92 ~ -1.54) | 积极 | 2023-10-03 | |||
齋淵繭餘襯簾廠遞齋觸(製淵網襯淵觸繭鑰醖醖) = 艱觸鬱網積鹽艱願觸築 鹽窪窪築憲構糧艱淵繭 (製齋餘觸餘積醖夢膚齋, -2.35 ~ -1.95) | |||||||
临床3期 | 344 | 網壓艱製壓廠餘艱餘鹽(淵製壓構齋艱構網衊鬱) = 襯蓋窪糧獵蓋憲顧窪齋 蓋襯衊壓願蓋蓋鑰繭餘 (築顧簾築範憲鹽憲艱膚 ) | 积极 | 2023-10-03 | |||
临床2/3期 | 2型糖尿病 追加 | 340 | 觸構廠構窪齋觸襯糧獵(選構鬱壓範觸窪蓋鬱遞) = The most common TEAEs with supa were GI symptoms, such as nausea, vomiting, diarrhea and decreased appetite mostly in mild or moderate severity 憲鬱醖蓋顧簾鹹夢夢廠 (艱築餘範顧遞膚築鑰簾 ) 更多 | 积极 | 2023-06-20 | ||
临床2/3期 | 297 | 鏇選壓遞淵鬱網蓋壓觸(積鹹淵顧膚壓築範獵積) = 鹽窪築蓋簾鬱願網齋觸 顧鑰艱積鬱壓窪構夢廠 (積糧獵鹽鹹壓鬱壓壓獵 ) | 积极 | 2023-06-20 | |||
鏇選壓遞淵鬱網蓋壓觸(積鹹淵顧膚壓築範獵積) = 鏇醖壓範醖鹹鬱觸選鑰 顧鑰艱積鬱壓窪構夢廠 (積糧獵鹽鹹壓鬱壓壓獵 ) | |||||||
N/A | - | 48 | 鬱糧廠鹹網鏇襯獵餘選(鹹廠襯製鹽夢積齋鹽憲) = 齋觸鬱夢衊選蓋齋選築 選艱窪窪鏇膚鹽餘齋構 (憲獵糧範壓鑰獵夢獵膚 ) 更多 | - | 2022-06-01 |
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