Delving into the Latest Updates on Taspoglutide with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Taspoglutide (USAN/INN), BIM 51077, BIM-51077

+ [10]

Target

GLP-1R

Action

agonists

Mechanism

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

Therapeutic Areas

Cardiovascular DiseasesEndocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Cardiovascular DiseasesDiabetes MellitusDiabetes Mellitus, Type 2+ [1]

Originator Organization

Ipsen SA

Active Organization-

Inactive Organization

Hoffmann-La Roche, Inc.Ipsen Pharma SAS

Shanghai Roche Pharmaceuticals Ltd.

License Organization

Ipsen SA

Roche Holding AG

Teijin Ltd.

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC152H232N40O45

InChIKeyWRGVLTAWMNZWGT-VQSPYGJZSA-N

CAS Registry275371-94-3

Sequence Code 10258990

Source: *****

A multi-center, single-dose, open-label, randomized, parallel group study to investigate the reduction of initial taspoglutide Cmax after administration of 20 mg taspoglutide 10% Sustained Release Formulation (SRF) using three modified formulations as compared to the current Phase 3 formulation in healthy volunteers. - Taspoglutide BE study in healthy volunteers

Start Date26 Oct 2010

Sponsor / Collaborator-

100 Clinical Results associated with Taspoglutide

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100 Translational Medicine associated with Taspoglutide

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100 Patents (Medical) associated with Taspoglutide

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66

Literatures (Medical) associated with Taspoglutide

01 Apr 2025·DIABETES OBESITY & METABOLISM

Comparison of the efficacy and safety of GLP ‐1 receptor agonists on cardiovascular events and risk factors: A review and network meta‐analysis

Review

Author: Jiang, Linlin ; Zhao, Xuefei ; Sun, WenJie ; Zhang, YueHong ; Lian, Fengmei ; Sun, Yuting ; Gao, Qing ; Kang, Xiaomin ; An, Xuedong ; Wen, Zhige ; Duan, LiYun ; Ji, Hangyu

Abstract:

Objective:

This study aims to systematically evaluate and perform a systematic review and network meta‐analysis comparing the comprehensive cardiovascular protective effects of various glucagon‐like peptide‐1 receptor agonists (GLP‐1RAs), focusing on cardiovascular events and risk factors.

Methods:

We searched PubMed, Embase, Cochrane Library and Web of Science from inception to December 15, 2024. Included studies were published randomized controlled trials (RCTs) comparing GLP‐1RAs to placebo or other GLP‐1RAs. Missing data were standardized, and network meta‐analysis was performed using Stata 17.0. Study heterogeneity, publication bias and evidence quality were assessed using the Cochrane Risk of Bias tool and Confidence in Network Meta‐Analysis (CINeMA).

Results:

As of December 15, 2024, a total of 18 313 articles were retrieved. Based on the inclusion and exclusion criteria, 156 high‐quality studies were included, incorporating 144 782 patients and 14 different GLP‐1RAs. The network meta‐analysis demonstrated low heterogeneity, ensuring the reliability of the results. Comprehensive analysis revealed the following: Efpeglenatide was the most effective in reducing major adverse cardiovascular events. Oral semaglutide shows more significant advantages in reducing all‐cause mortality and cardiovascular mortality. Orforglipron excelled in glycaemic control and weight reduction. SC‐Semaglutide showed the greatest efficacy in lowering both systolic blood pressure and diastolic blood pressure, Liraglutide showed the greatest efficacy in lowering total cholesterol, Noiiglutide in triglycerides and Taspoglutide in low‐density lipoprotein cholesterol, but no GLP‐1RAs in high‐density lipoprotein cholesterol. GLP‐1RAs did not significantly increase the incidence of adverse events, but Orforglipron and Taspoglutide significantly increased the incidence of gastrointestinal adverse events compared with placebo.

Conclusion:

This study compared the cardiovascular benefits of different GLP‐1RAs, including reductions in cardiovascular events and improvements in multiple cardiovascular risk factors. However, due to limitations in the quantity and quality of the included studies, the conclusions should be interpreted with caution. Future large‐scale, high‐quality clinical trials are needed to validate these findings and further optimize comprehensive cardiovascular management strategies for patients.

01 Dec 2022·Artificial intelligence in the life sciences

The commoditization of AI for molecule design

Article

Author: Ekins, Sean ; Urbina, Fabio

Anyone involved in designing or finding molecules in the life sciences over the past few years has witnessed a dramatic change in how we now work due to the COVID-19 pandemic. Computational technologies like artificial intelligence (AI) seemed to become ubiquitous in 2020 and have been increasingly applied as scientists worked from home and were separated from the laboratory and their colleagues. This shift may be more permanent as the future of molecule design across different industries will increasingly require machine learning models for design and optimization of molecules as they become "designed by AI". AI and machine learning has essentially become a commodity within the pharmaceutical industry. This perspective will briefly describe our personal opinions of how machine learning has evolved and is being applied to model different molecule properties that crosses industries in their utility and ultimately suggests the potential for tight integration of AI into equipment and automated experimental pipelines. It will also describe how many groups have implemented generative models covering different architectures, for de novo design of molecules. We also highlight some of the companies at the forefront of using AI to demonstrate how machine learning has impacted and influenced our work. Finally, we will peer into the future and suggest some of the areas that represent the most interesting technologies that may shape the future of molecule design, highlighting how we can help increase the efficiency of the design-make-test cycle which is currently a major focus across industries.

01 May 2022·Biochemical pharmacologyQ2 · MEDICINE

Implications of ligand-receptor binding kinetics on GLP-1R signalling

Q2 · MEDICINE

Article

Author: Zhao, Peishen ; Sexton, Patrick M ; Wootten, Denise ; Merlin, Jon ; Truong, Tin T

G protein-coupled receptors (GPCRs) are the largest class of membrane proteins and in recent years there has been a growing appreciation of the importance in understanding temporal aspects of GPCR behaviour, including the kinetics of ligand binding and downstream receptor mediated signalling. Class B1 GPCRs are activated by peptide agonists and are validated therapeutic targets for numerous diseases. However, the kinetics of ligand binding and how this is linked to downstream activation of signalling cascades is not routinely assessed in development of peptide agonists for this receptor class. The glucagon-like peptide-1 receptor (GLP-1R) is a prototypical class B1 GPCR and a validated target for treatment of global health burdens, including type 2 diabetes and obesity. In this study we examined the kinetics of different steps in GLP-1R activation and subsequent cAMP production mediated by a series of GLP-1R peptide agonists, including the ligand-receptor interaction, ligand-receptor-mediated G protein engagement and conformational change and cAMP production. Our results revealed GLP-1R peptide agonist dissociation kinetics (K_off), but not association kinetics (K_on), were positively correlated with the onset of receptor-G protein coupling/conformational change, onset of cAMP production and duration of cAMP signalling. Thus, this study advances the understanding of molecular events that couple GLP-1R ligand binding to intracellular signaling, with the findings likely to have implications for mechanistic understanding of agonist action at other related class B1 GPCRs.

1

News (Medical) associated with Taspoglutide

17 Jul 2024

·www.echemi.com

Roche's GLP-1/GIP Dual Agonist Shows Impressive Weight Loss Results in Phase 1 Trial

Recently, the Swiss pharmaceutical giant roche said, it is in the study of new type of glp-1 / GIP double agonist CT - 388 performance is satisfactory in phase I clinical trials, the results present a positive trend. According to data released this innovative therapy in subjects puts a significant weight loss potential. Research data show that in patients treated with CT - 388 group, 45% of the individual in the process of 24 weeks of treatment, the body weight decreased more than 20%, the result is encouraging. In addition, all the participants lost more than 5% of their body weight during treatment, and 70% of them lost more than 15%. Even more attractive, weight loss effect brought by the CT - 388 after 24 weeks of treatment did not show signs of slowing, the implication for longer follow-up therapy, patients might be able to obtain more excellent weight loss results. An abstract presented at the upcoming European Association for the Study of Diabetes annual meeting in September 2023 heightens expectations that the previously reported average weight loss of 18.8% May be just the beginning. Roche is not new to the development of GLP-1 receptor agonists. The company previously developed a GLP-1 agonist called Taspoglutide, which entered a phase II clinical trial in 2008, but safety concerns eventually led to the discontinuation of further studies in 2011. However, with the acquisition of Carmot Therapeutics in 2023, CT-388 was incorporated into Roche's R&D pipeline, marking a renewed bet on this promising therapeutic area. Dr Manu Chakravarthy, global head of Cardiovascular, renal and Metabolic Products Development at Roche, revealed that the company plans to initiate a phase II clinical trial of CT-388 in the second half of 2024. The test not only can evaluate the efficacy of CT - 388 in terms of weight loss, will also explore the in improving the potential role of cardiovascular disease and type 2 diabetes. CT - 388 the success of research and development will likely for obesity and type 2 diabetes patients to bring a new and more effective treatments. The results of the phase II clinical trial of this GLP-1/GIP dual agonist are being closely watched by people inside and outside the industry, with high expectations for its future performance.

Phase 2AcquisitionPhase 1Clinical Result

100 Deals associated with Taspoglutide

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External Link

KEGG	Wiki	ATC	Drug Bank
D09723	Taspoglutide	-	DB14027

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus	Phase 3	Italy	Ipsen Pharma SAS	30 Aug 2011
Cardiovascular Diseases	Phase 3	United States	Hoffmann-La Roche, Inc.	01 Jan 2010
Cardiovascular Diseases	Phase 3	Australia	Hoffmann-La Roche, Inc.	01 Jan 2010
Cardiovascular Diseases	Phase 3	Brazil	Hoffmann-La Roche, Inc.	01 Jan 2010
Cardiovascular Diseases	Phase 3	Bulgaria	Hoffmann-La Roche, Inc.	01 Jan 2010
Cardiovascular Diseases	Phase 3	Canada	Hoffmann-La Roche, Inc.	01 Jan 2010
Cardiovascular Diseases	Phase 3	Czechia	Hoffmann-La Roche, Inc.	01 Jan 2010
Cardiovascular Diseases	Phase 3	Denmark	Hoffmann-La Roche, Inc.	01 Jan 2010
Cardiovascular Diseases	Phase 3	Estonia	Hoffmann-La Roche, Inc.	01 Jan 2010
Cardiovascular Diseases	Phase 3	Germany	Hoffmann-La Roche, Inc.	01 Jan 2010

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00717457 (T-emerge 2, Pubmed \| Diabetes Care)	Phase 3	Diabetes Mellitus, Type 2	1,189	Taspoglutide 10 mg	zgsntskaet(xnmiflqvae) = oxlhyzcgck ovqaxnxgzq (lvpladalaa ) View more	-	01 Mar 2013
				Taspoglutide 20 mg	zgsntskaet(xnmiflqvae) = ikrbxnscfr ovqaxnxgzq (lvpladalaa ) View more
NCT00755287 (Pubmed \| Diabet Med)	Phase 3	Diabetes Mellitus, Type 2	1,049	Taspoglutide 10 mg once weekly	eetvehfsfn(cmmruhscvr) = zozwvetvyo nbqvlfkstm (gyfaabsdah )	Positive	01 Jan 2013
				Taspoglutide 20 mg once weekly	eetvehfsfn(cmmruhscvr) = ktwyhheyyz nbqvlfkstm (gyfaabsdah )
NCT00423501 (Pubmed \| Diabetes Care)	Phase 2	Diabetes Mellitus, Type 2	306	Taspoglutide 5 mg once weekly	rhfhmlpakv(tfrdbgmupt) = dsblwsumzt asfvlfoqld (elmnckrovb ) View more	Positive	01 Jul 2009
				Taspoglutide 10 mg once weekly	rhfhmlpakv(tfrdbgmupt) = htkqoxsdpq asfvlfoqld (elmnckrovb ) View more

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Biosimilar

Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

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