Delving into the Latest Updates on Supaglutide with Synapse

Overview

Basic Info

Drug Type

Fusion protein

Synonyms

Efsubaglutide Alfa, 依苏帕格鲁肽α

+ [5]

Target

GLP-1R

Mechanism

GLP-1R agonists(Glucagon-like peptide 1 receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseDigestive System Disorders

Active Indication

Diabetes Mellitus, Type 2ObesityNonalcoholic Steatohepatitis

Inactive Indication-

Originator Organization

Guangzhou Yinnuo Pharmaceutical Group Co., Ltd.

Active Organization

Innogen Pharmaceutical Technology Co Ltd.

Intellective Biologics (Suzhou) Co., Ltd.

Guangzhou Yinnuo Pharmaceutical Group Co., Ltd.

Inactive Organization-

Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationSpecial Review Project (CN)

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Gene Sequence

Sequence Code 1198651119

Source: *****

[Translation] A randomized, double-blind, placebo-controlled phase IIa clinical study on the safety, tolerability, pharmacokinetics and pharmacodynamics of multiple subcutaneous injections of esupagglutide α in overweight and obese subjects with poor weight control after diet and exercise intervention

评价依苏帕格鲁肽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的安全性、耐受性、药代动力学和药效学特征。

[Translation]

To evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of esupagglutide alfa injection in overweight and obese subjects whose weight is poorly controlled after diet and exercise intervention.

Start Date21 Apr 2024

Sponsor / Collaborator

Guangzhou Yinnuo Pharmaceutical Group Co., Ltd.

CTR20230127 / CompletedPhase 1

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

[Translation] A single-center, open-label, fixed-sequence clinical study to evaluate the effect of supaglutide injection on the pharmacokinetics of digoxin tablets or metformin hydrochloride tablets in healthy subjects

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。主要目的 1.在健康受试者中，评价多次皮下注射苏帕鲁肽注射液对单次口服地高辛片药代动力学的影响。 2.在健康受试者中，评价多次皮下注射苏帕鲁肽注射液对多次口服盐酸二甲双胍片药代动力学的影响。次要目的 1.在健康受试者中，评价多次皮下注射苏帕鲁肽注射液后单次口服地高辛片的安全性。 2.在健康受试者中，评价多次皮下注射苏帕鲁肽注射液后多次口服盐酸二甲双胍片的安全性。

[Translation]

A single-center, open-label, fixed-sequence clinical study to evaluate the effect of supaglutide injection on the pharmacokinetics of digoxin tablets or metformin hydrochloride tablets in healthy subjects. Primary objective 1. To evaluate the effect of multiple subcutaneous injections of supaglutide injection on the pharmacokinetics of a single oral digoxin tablet in healthy subjects. 2. To evaluate the effect of multiple subcutaneous injections of supaglutide injection on the pharmacokinetics of multiple oral metformin hydrochloride tablets in healthy subjects. Secondary objective 1. To evaluate the safety of a single oral digoxin tablet after multiple subcutaneous injections of supaglutide injection in healthy subjects. 2. To evaluate the safety of multiple oral metformin hydrochloride tablets after multiple subcutaneous injections of supaglutide injection in healthy subjects.

Start Date20 Mar 2023

Sponsor / Collaborator

Guangzhou Yinnuo Pharmaceutical Group Co., Ltd.

[+1]

NCT05694221 / CompletedPhase 1

A Single-centre, Open Labeled, Fixed-sequence Study to Evaluate the Effect of Supaglutide on Digoxin or Metformin Pharmacokinetics

This is a study of a drug drug interaction between Supaglutide and Digoxin or Metformin.

Start Date20 Mar 2023

Sponsor / Collaborator

Innogen Pharmaceutical Technology Co Ltd.

[+1]

100 Clinical Results associated with Supaglutide

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100 Translational Medicine associated with Supaglutide

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100 Patents (Medical) associated with Supaglutide

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4

Literatures (Medical) associated with Supaglutide

01 Aug 2022·European Journal of Pharmaceutical Sciences

Pharmacokinetic and pharmacodynamic studies of supaglutide in rats and monkeys

Article

Author: Wang, Zhihong ; Zhang, Li ; Ma, Anran ; Prud'homme, Gerald J ; Liao, Yijing ; Wang, Qinghua ; Liu, Lin ; 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.

01 Feb 2021·Journal of EndocrinologyQ3 · MEDICINE

Novel GLP-1 analog supaglutide improves glucose homeostasis in diabetic monkeys

Q3 · MEDICINE

Article

Author: Ma, Anran ; Zhao, Ying ; Li, Jia ; Cui, Qiaoli ; Zhou, Quanquan ; Zhang, Li ; Wang, Qinghua ; Liang, Yinan ; Wang, Zhihong ; Jiang, Yaojing ; Shao, Anna ; Tao, Weihong ; Yang, Zunyuan ; Liao, Yijing ; Zeng, Wen ; Yang, Zhenyan ; Huang, Xiaohang ; Wu, Minglin

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 PhysiologyQ2 · MEDICINE

Novel GLP-1 Analog Supaglutide Stimulates Insulin Secretion in Mouse and Human Islet Beta-Cells and Improves Glucose Homeostasis in Diabetic Mice

Q2 · MEDICINE

ArticleOA

Author: Zhang, Zhaoyun ; Zhang, Lina ; Wang, Liqian ; Feng, Ying ; Liu, Wenjuan ; Jin, Tianru ; Ren, Liwei ; Wang, Qinghua ; Leng, Ying ; Liao, Yijing ; Cui, Qiaoli ; Li, Yiming ; Yang, Yehong ; Sun, Wanwan ; Prud'homme, Gerald J

Glucagon-like peptide-1 (GLP-1), an incretin hormone plays an important role in regulating glucose homeostasis. The therapeutic use of native GLP-1 is inadequate due to its short in vivo half-life. We recently developed a novel GLP-1 mimetics supaglutide, and demonstrated that this formulation retained native GLP-1 biological activities and possessed long-lasting GLP-1 actions. In this study, we further examined its abilities in regulating blood glucose in diabetic mice. We found that supaglutide stimulated insulin secretion in both mouse and human islets in a dose-dependent fashion. Oral glucose tolerance test conducted in normal ICR mice showed that supaglutide significantly decreased postprandial glucose excursions in a dose-dependent fashion. In type 2 diabetic db/db mice, a single-dose injection of supaglutide significantly decreased blood glucose levels, and this efficacy was lasted for at least 72 h in a dose-dependent fashion. During a 4-weeks intervention course supaglutide (twice injections per week) dose-dependently and significantly decreased fasting and random blood glucose levels in hyperglycemic db/db mice. Supaglutide, at a dose of 1.2 mg/kg, significantly reduced serum fructosamine levels. This was associated with significant enlargement of beta-cell mass, increased pancreatic insulin content, and increased plasma insulin level. Notably, during the intervention course supaglutide significantly reduced body-weight gain in these obese diabetic mice, associated with reduced fat mass (but not the lean mass), improved lipid profile, i.e., declined serum triglyceride, and free fatty acid levels compared to the placebo control. These finding reveals that supaglutide exerts beneficial effects in regulating blood glucose and lipid homeostasis in diabetic db/db mice.

100 Deals associated with Supaglutide

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	NDA/BLA	CN	Intellective Biologics (Suzhou) Co., Ltd.	27 Sep 2023
Diabetes Mellitus, Type 2	NDA/BLA	CN	Innogen Pharmaceutical Technology Co Ltd.	27 Sep 2023
Obesity	Phase 2	CN	Guangzhou Yinnuo Pharmaceutical Group Co., Ltd.	21 Apr 2024
Nonalcoholic Steatohepatitis	Phase 2	US	Innogen Pharmaceutical Technology Co Ltd.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05694221 (ADA2024) Manual	Phase 1	-	32	Supaglutide+digoxin	(lulpncvrnx) = 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. jnknllbavk (xwrellycug )	Positive	14 Jun 2024
				Supaglutide+metformin hydrochloride
NCT04998032 (EASD2023)	Phase 3	Diabetes Mellitus, Type 2 Add-on HbA1c	344	Supaglutide 3 mg	(msatfzgusk) = ljzdhdqcyi cuethvtznr (kghmfweodk )	Positive	03 Oct 2023
NCT04994288 (phase 3, EASD2023)	Phase 3	Diabetes Mellitus, Type 2	297	Supaglutide 1 mg	(eodscbmhse) = uymvcytrby ucnivnedcd (ikjhznzsys, -1.92 to -1.54)	Positive	03 Oct 2023
				Supaglutide 3 mg	(eodscbmhse) = iyiynegncm ucnivnedcd (ikjhznzsys, -2.35 to -1.95)
NCT04994288 (ADA2023)	Phase 2/3	Diabetes Mellitus, Type 2	297	Supaglutide 1 mg	(jnovyiukmw) = tncrrzsymw udqpokunzn (sjletlaqas )	Positive	20 Jun 2023
				Supaglutide 3 mg	(jnovyiukmw) = hrkxhrwxqw udqpokunzn (sjletlaqas )
NCT04998032 (ADA2023)	Phase 2/3	Diabetes Mellitus, Type 2 Add-on	340	Supaglutide 3 mg	qwhyxsfade(hcoxepvazw) = The most common TEAEs with supa were GI symptoms, such as nausea, vomiting, diarrhea and decreased appetite mostly in mild or moderate severity isguxxzbyy (azgnrmzuyc ) View more	Positive	20 Jun 2023
ADA2022	Not Applicable	-	48	Supaglutide	(okgedhrqlj) = ctbhmjbbap ozhajyfjua (hhrmihpmhg ) View more	-	01 Jun 2022