☆ 4.7 Review

Effect of dual glucose-dependent insulinotropic peptide/glucagon-like peptide-1 receptor agonist on weight loss in subjects with obesity

FRONTIERS IN ENDOCRINOLOGY (2023)

相关参考文献

注意：仅列出部分参考文献，下载原文获取全部文献信息。

Editorial Material Cell Biology

GLP-1/GIP/glucagon receptor triagonism gets its try in humans

Brian Finan et al.

Summary: The study by Bossart et al. discusses the in vivo receptor occupancy, body weight lowering effects, and first-in-human results of SAR441255, a triagonist targeting GLP-1R/GIPR/GcgR. The results show positive acute glucoregulatory effects and acceptable safety profile in terms of gastrointestinal tolerability and cardiovascular hemodynamics.

CELL METABOLISM (2022)

添加到收藏夹

Article Cell Biology

Effects on weight loss and glycemic control with SAR441255, a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist

Martin Bossart et al.

Summary: Unimolecular triple incretins have shown efficacy in reducing body weight and improving glucose control. SAR441255, a synthetic peptide agonist, activates GLP-1, GCG, and GIP receptors with balanced potency, demonstrating superior metabolic outcomes compared to dual agonists in animal models.

CELL METABOLISM (2022)

添加到收藏夹

Article Medicine, General & Internal

Effect of Subcutaneous Tirzepatide vs Placebo Added to Titrated Insulin Glargine on Glycemic Control in Patients With Type 2 Diabetes The SURPASS-5 Randomized Clinical Trial

Dominik Dahl et al.

Summary: The addition of tirzepatide to insulin glargine treatment in patients with type 2 diabetes resulted in significant improvements in glycemic control after 40 weeks.

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Effects of Tirzepatide, a Dual GIP and GLP-1 RA, on Lipid and Metabolite Profiles in Subjects With Type 2 Diabetes

Valentina Pirro et al.

Summary: Tirzepatide significantly reduced HbA1c and body weight in subjects with type 2 diabetes compared to dulaglutide, modulating metabolites associated with insulin resistance, obesity, and future T2D risk. These metabolic changes were proportional to improvements in glycemic control and beta-cell function, indicating a unique effect of tirzepatide on metabolic health.

JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM (2022)

添加到收藏夹

Article Endocrinology & Metabolism

The incretin/glucagon system as a target for pharmacotherapy of obesity

Stefano Del Prato et al.

Summary: Obesity is a chronic disease with complex pathophysiology that requires comprehensive interventions targeting multiple pathways. Receptor agonists that target both glucagon and incretin hormone receptors show promise in promoting weight loss, lowering glucose levels, and regulating food intake. Further research is needed to fully understand the molecular mechanisms and metabolic effects of these dual and triple receptor agonists.

OBESITY REVIEWS (2022)

添加到收藏夹

Article Biology

Role of a Dual Glucose-Dependent Insulinotropic Peptide (GIP)/Glucagon-like Peptide-1 Receptor Agonist (Twincretin) in Glycemic Control: From Pathophysiology to Treatment

Maria Chiara Pelle et al.

Summary: Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are two gut hormones that play different roles in insulin secretion and food intake. GLP-1 has been successful in diabetes treatment, while the application of GIP for T2DM is still being discussed. The combination of GIP and GLP-1 has shown a synergistic effect in increasing insulin response and inhibiting glucagon secretion.

LIFE-BASEL (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

Tirzepatide cardiovascular event risk assessment: a pre-specified meta-analysis

Naveed Sattar et al.

Summary: This meta-analysis study on Tirzepatide included 7 randomized controlled trials, and the findings suggest that using Tirzepatide in patients with T2D does not increase the risk of major cardiovascular events.

NATURE MEDICINE (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Effects of subcutaneous tirzepatide versus placebo or semaglutide on pancreatic islet function and insulin sensitivity in adults with type 2 diabetes: a multicentre, randomised, double-blind, parallel-arm, phase 1 clinical trial

Tim Heise et al.

Summary: Tirzepatide demonstrates remarkable glucose-lowering ability in patients with type 2 diabetes by improving insulin secretion and sensitivity. Compared to other GLP-1 receptor agonists, Tirzepatide shows more significant improvements in glucose metabolism.

LANCET DIABETES & ENDOCRINOLOGY (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Effect of tirzepatide versus insulin degludec on liver fat content and abdominal adipose tissue in people with type 2 diabetes (SURPASS-3 MRI): a substudy of the randomised, open-label, parallel-group, phase 3 SURPASS-3 trial

Amalia Gastaldelli et al.

Summary: Tirzepatide demonstrated significant reductions in liver fat content, visceral adipose tissue, and abdominal subcutaneous adipose tissue in patients with type 2 diabetes in the SURPASS-3 study.

LANCET DIABETES & ENDOCRINOLOGY (2022)

添加到收藏夹

Review Pharmacology & Pharmacy

Efficacy and safety of tirzepatide in patients with type 2 diabetes: A systematic review and meta-analysis

Yan Tang et al.

Summary: This systematic review and meta-analysis evaluated the clinical efficacy and safety of tirzepatide in patients with type 2 diabetes. The results showed that tirzepatide significantly reduced HbA1c, fasting serum glucose, and body weight, and improved blood pressure and fasting lipid profiles without increasing the risk of hypoglycemia.

FRONTIERS IN PHARMACOLOGY (2022)

添加到收藏夹

Review Biochemistry & Molecular Biology

Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review

Vivek P. Chavda et al.

Summary: Tirzepatide is a novel anti-diabetic drug that significantly improves weight, glycemic levels, and lipid metabolism in patients with diabetes. It offers a once-weekly dosing option through injection, providing an important therapeutic choice for diabetes and obesity.

MOLECULES (2022)

添加到收藏夹

Editorial Material Endocrinology & Metabolism

What's preventing us from curbing the obesity crisis?

[Anonymous]

LANCET DIABETES & ENDOCRINOLOGY (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Efficacy and safety of tirzepatide monotherapy compared with dulaglutide in Japanese patients with type 2 diabetes (SURPASS J-mono): a double-blind, multicentre, randomised, phase 3 trial

Nobuya Inagaki et al.

Summary: Tirzepatide showed superior efficacy in glycemic control and reduction in body weight compared to dulaglutide, suggesting a potential therapeutic use in Japanese patients with type 2 diabetes.

LANCET DIABETES & ENDOCRINOLOGY (2022)

添加到收藏夹

Article Cell Biology

LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept

Tamer Coskun et al.

Summary: With the increasing prevalence of obesity, there is a need for new therapies to improve body weight management and metabolic health. The novel triple agonist peptide LY3437943 shows promising results in reducing body weight and improving glycemic control in obese mice, making it a potential treatment for obesity.

CELL METABOLISM (2022)

添加到收藏夹

Article Medicine, General & Internal

LY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in people with type 2 diabetes: a phase 1b, multicentre, double-blind, placebo-controlled, randomised, multiple-ascending dose trial

Shweta Urva et al.

Summary: LY3437943, a multi-receptor agonist for the treatment of type 2 diabetes and obesity, demonstrated acceptable safety, suitable pharmacokinetics for once-weekly dosing, and significant improvements in glucose and bodyweight outcomes in this study.

LANCET (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Effects of tirzepatide versus insulin glargine on kidney outcomes in type 2 diabetes in the SURPASS-4 trial: post-hoc analysis of an open-label, randomised, phase 3 trial

Hiddo J L Heerspink et al.

Lancet Diabetes & Endocrinology (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Next generation GLP-1/GIP/glucagon triple agonists normalize body weight in obese mice

Patrick J. Knerr et al.

Summary: This study aims to design unimolecular peptide triagonists that activate multiple receptors to improve metabolic diseases. The optimized triagonists show promising results in controlling body weight and enhancing energy expenditure in animal models, providing a potential new approach for obesity treatment.

MOLECULAR METABOLISM (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Tirzepatide induces a thermogenic-like amino acid signature in brown adipose tissue

Ricardo J. Samms et al.

Summary: Tirzepatide improves insulin sensitivity in T2D patients and obese mice by promoting the catabolism of BCAAs in BAT, resulting in reduced systemic levels of BCAAs and changes in the thermogenic amino acid profile in BAT.

MOLECULAR METABOLISM (2022)

添加到收藏夹

Review Endocrinology & Metabolism

WEIGHT LOSS EFFECT OF SODIUM-GLUCOSE COTRANSPORTER-2 (SGLT2) INHIBITORS IN PATIENTS WITH OBESITY WITHOUT DIABETES: A SYSTEMATIC REVIEW

K. G. Pratama et al.

Summary: SGLT2 inhibitors are effective weight loss therapy for obese individuals without diabetes.

ACTA ENDOCRINOLOGICA-BUCHAREST (2022)

添加到收藏夹

Article Medicine, General & Internal

Tirzepatide Once Weekly for the Treatment of Obesity

Ania M. Jastreboff et al.

Summary: In this 72-week trial in participants with obesity, once-weekly doses of 5 mg, 10 mg, or 15 mg of tirzepatide provided substantial and sustained reductions in body weight, and improvements in cardiometabolic measures were also observed.

NEW ENGLAND JOURNAL OF MEDICINE (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Next generation GLP-1/GIP/glucagon triple agonists normalize body weight in obese mice

Patrick J. Knerr et al.

Summary: This study introduces empirically optimized unimolecular peptide triagonists, which effectively reduce body weight and enhance energy expenditure in DIO mice, outperforming GLP-1R mono-agonists and GLP-1R/GIPR co-agonists. The data suggest that unimolecular poly-pharmacology is an effective means to target obesity and implicate GcgR activation as a differentiating factor in incretin receptor agonists.

MOLECULAR METABOLISM (2022)

添加到收藏夹

Article Endocrinology & Metabolism

HbA(1c) Change and Diabetic Retinopathy During GLP-1 Receptor Agonist Cardiovascular Outcome Trials: A Meta-analysis and Meta-regression

M. Angelyn Bethel et al.

Summary: The study found that HbA(1c) reduction was significantly associated with increased retinopathy risk in GLP-1RA CVOTs. However, no relationship was found for SBP or weight. The magnitude of HbA(1c) reduction was correlated with retinopathy risk in people with diabetes.

DIABETES CARE (2021)

添加到收藏夹

Article Cell Biology

The glucose-dependent insulinotropic polypeptide (GIP) regulates body weight and food intake via CNS-GIPR signaling

Qian Zhang et al.

Summary: The activation or inhibition of the glucose-dependent insulinotropic polypeptide receptor (GIPR) for the treatment of obesity remains uncertain. Studies show that CNS Gipr plays a key role in controlling energy metabolism, with activation or inhibition having significant effects on body weight and glucose metabolism.

CELL METABOLISM (2021)

添加到收藏夹

Article Medicine, General & Internal

Tirzepatide versus insulin glargine in type 2 diabetes and increased cardiovascular risk (SURPASS-4): a randomised, open-label, parallel-group, multicentre, phase 3 trial

Stefano Del Prato et al.

Summary: In this study comparing Tirzepatide and glargine in patients with type 2 diabetes inadequately controlled on oral glucose-lowering medications, Tirzepatide demonstrated greater reduction in HbA(1c) and lower incidence of hypoglycemia at week 52, with no excess cardiovascular risk observed compared to glargine.

LANCET (2021)

添加到收藏夹

Article Endocrinology & Metabolism

The Role of GIP Receptor in the CNS for the Pathogenesis of Obesity

Makoto Fukuda

Summary: GIP, a hormone produced in the upper gut in response to food ingestion, plays a physiological and pharmacological role in obesity. Inhibiting GIP can lead to decreased energy intake, increased energy expenditure, and ultimately weight loss. The widespread distribution of the GIP receptor in the brain suggests its important role in obesity-related pathogenesis.

DIABETES (2021)

添加到收藏夹

Article Medicine, General & Internal

Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial

Julio Rosenstock et al.

Summary: Tirzepatide demonstrated significant improvements in glycemic control and body weight without increasing the risk of hypoglycemia. The safety profile was consistent with GLP-1 receptor agonists, suggesting a potential monotherapy use for the treatment of type 2 diabetes.

LANCET (2021)

添加到收藏夹

Article Medicine, General & Internal

Once-weekly tirzepatide versus once-daily insulin degludec as add-on to metformin with or without SGLT2 inhibitors in patients with type 2 diabetes (SURPASS-3): a randomised, open-label, parallel-group, phase 3 trial

Bernhard Ludvik et al.

Summary: The study aimed to compare the efficacy and safety of tirzepatide versus titrated insulin degludec in the treatment of type 2 diabetes. The results showed that tirzepatide had significant advantages in reducing HbA(1c) and bodyweight, and decreased the risk of hypoglycemia.

LANCET (2021)

添加到收藏夹

Article Medicine, General & Internal

Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes

Juan P. Frias et al.

Summary: The study showed that Tirzepatide was both noninferior and superior to Semaglutide in terms of the mean change in glycated hemoglobin levels for patients with type 2 diabetes over 40 weeks. Additionally, reductions in body weight were greater with Tirzepatide compared to Semaglutide, with similar rates of gastrointestinal adverse events reported in both groups.

NEW ENGLAND JOURNAL OF MEDICINE (2021)

添加到收藏夹

Article Medicine, Research & Experimental

GIPR agonism mediates weight-independent insulin sensitization by tirzepatide in obese mice

Ricardo J. Samms et al.

Summary: Tirzepatide, a dual GIP and GLP-1 receptor agonist, improves insulin sensitivity in obese mice to a greater extent than GLP-1R agonism. This effect is associated with enhanced glucose disposal in white adipose tissue and reduction of branched-chain amino acids in the circulation. The upregulation of genes related to the catabolism of glucose, lipid, and BCAAs in brown adipose tissue contributes to the improved insulin sensitivity by tirzepatide.

JOURNAL OF CLINICAL INVESTIGATION (2021)

添加到收藏夹

Review Endocrinology & Metabolism

Glucose-Dependent Insulinotropic Polypeptide Receptor Therapies for the Treatment of Obesity, Do Agonists = Antagonists?

Elizabeth A. Killion et al.

ENDOCRINE REVIEWS (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

The early history of GIP 1969-2000: From enterogastrone to major metabolic hormone

Vincent Marks

PEPTIDES (2020)

添加到收藏夹

Article Medicine, Research & Experimental

Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

Francis S. Willard et al.

JCI INSIGHT (2020)

添加到收藏夹

Article Pharmacology & Pharmacy

Evaluation of biased agonism mediated by dual agonists of the GLP-1 and glucagon receptors

Sanaz Darbalaei et al.

BIOCHEMICAL PHARMACOLOGY (2020)

添加到收藏夹

Review Endocrinology & Metabolism

How May GIP Enhance the Therapeutic Efficacy of GLP-1?

Ricardo J. Samms et al.

TRENDS IN ENDOCRINOLOGY AND METABOLISM (2020)

添加到收藏夹

Review Pharmacology & Pharmacy

Safety and tolerability of once-weekly GLP-1 receptor agonists in type 2 diabetes

Jennifer Trujillo

JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS (2020)

添加到收藏夹

Article Endocrinology & Metabolism

Liraglutide treatment improves postprandial lipid metabolism and cardiometabolic risk factors in humans with adequately controlled type 2 diabetes: A single-centre randomized controlled study

Niina Matikainen et al.

DIABETES OBESITY & METABOLISM (2019)

添加到收藏夹

Article Medicine, General & Internal

Dulaglutide and cardiovascular outcomes in type 2 diabetes (REWIND): a double-blind, randomised placebo-controlled trial

Hertzel C. Gerstein et al.

LANCET (2019)

添加到收藏夹

Article Cell Biology

Glucose-Dependent Insulinotropic Polypeptide Receptor-Expressing Cells in the Hypothalamus Regulate Food Intake

Alice E. Adriaenssens et al.

CELL METABOLISM (2019)

添加到收藏夹

Article Urology & Nephrology

Blood Pressure Variability, Mortality, and Cardiovascular Outcomes in CKD Patients

Francesca Mallamaci et al.

CLINICAL JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY (2019)

添加到收藏夹

Article Endocrinology & Metabolism

Separate and Combined Glucometabolic Effects of Endogenous Glucose-Dependent Insulinotropic Polypeptide and Glucagon-like Peptide 1 in Healthy Individuals

Laerke S. Gasbjerg et al.

DIABETES (2019)

添加到收藏夹

Article Peripheral Vascular Disease

Short-termblood pressure variability in nondialysis chronic kidney disease patients: correlates and prognostic role on the progression of renal disease

Silvio Borrelli et al.

JOURNAL OF HYPERTENSION (2018)

添加到收藏夹

Article Medicine, General & Internal

Efficacy and safety of LY3298176, a novel dual GIP and GLP-1 receptor agonist, in patients with type 2 diabetes: a randomised, placebo-controlled and active comparator-controlled phase 2 trial

Juan Pablo Frias et al.

LANCET (2018)

添加到收藏夹

Article Endocrinology & Metabolism

LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept

Tamer Coskun et al.

MOLECULAR METABOLISM (2018)

添加到收藏夹

Article Neurosciences

A rapidly acting glutamatergic ARC→PVH satiety circuit postsynaptically regulated by α-MSH

Henning Fenselau et al.

NATURE NEUROSCIENCE (2017)

添加到收藏夹

Article Neurosciences

Novel GLP-1R/GIPR co-agonist twincretin is neuroprotective in cell and rodent models of mild traumatic brain injury

Ian A. Tamargo et al.

EXPERIMENTAL NEUROLOGY (2017)

添加到收藏夹

Letter Medicine, General & Internal

Mechanisms, Pathophysiology, and Management of Obesity

Nai-Wei Sheu et al.

NEW ENGLAND JOURNAL OF MEDICINE (2017)

添加到收藏夹

Article Medicine, General & Internal

Health Effects of Overweight and Obesity in 195 Countries over 25 Years

Ashkan Afshin et al.

NEW ENGLAND JOURNAL OF MEDICINE (2017)

添加到收藏夹

Article Biochemistry & Molecular Biology

Central administration of GLP-1 and GIP decreases feeding in mice

Cherl NamKoong et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2017)

添加到收藏夹

Review Oncology

Obesity and Cancer Mechanisms: Tumor Microenvironment and Inflammation

Neil M. Iyengar et al.

JOURNAL OF CLINICAL ONCOLOGY (2016)

添加到收藏夹

Article Cardiac & Cardiovascular Systems

Prognostic role of LDL cholesterol in non-dialysis chronic kidney disease: Multicenter prospective study in Italy

Luca De Nicola et al.

NUTRITION METABOLISM AND CARDIOVASCULAR DISEASES (2015)

添加到收藏夹

Article Endocrinology & Metabolism

European Guidelines for Obesity Management in Adults

Volkan Yumuk et al.

OBESITY FACTS (2015)

添加到收藏夹

Article Medicine, Research & Experimental

The arcuate nucleus mediates GLP-1 receptor agonist liraglutide-dependent weight loss

Anna Secher et al.

JOURNAL OF CLINICAL INVESTIGATION (2014)

添加到收藏夹

Article Cardiac & Cardiovascular Systems

2013 AHA/ACC/TOS Guideline for the Management of Overweight and Obesity in Adults A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines and The Obesity Society

Michael D. Jensen et al.

JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY (2014)

添加到收藏夹

Article Cell Biology

Unimolecular Dual Incretins Maximize Metabolic Benefits in Rodents, Monkeys, and Humans

Brian Finan et al.

SCIENCE TRANSLATIONAL MEDICINE (2013)

添加到收藏夹

Article Multidisciplinary Sciences

GIP-Overexpressing Mice Demonstrate Reduced Diet-Induced Obesity and Steatosis, and Improved Glucose Homeostasis

Su-Jin Kim et al.

PLOS ONE (2012)

添加到收藏夹

Article Medicine, Research & Experimental

Administration of an acylated GLP-I and GIP preparation provides added beneficial glucose-lowering and insulinotropic actions over single incretins in mice with Type 2 diabetes and obesity

Victor A. Gault et al.

CLINICAL SCIENCE (2011)

添加到收藏夹

Article Physiology

GIP-Dependent Expression of Hypothalamic Genes

S. Ambati et al.

PHYSIOLOGICAL RESEARCH (2011)

添加到收藏夹

Article Biochemistry & Molecular Biology

GIP increases human adipocyte LPL expression through CREB and TORC2-mediated trans-activation of the LPL gene

Su-Jin Kim et al.

JOURNAL OF LIPID RESEARCH (2010)

添加到收藏夹

Article Endocrinology & Metabolism

The direct effects of GLP-1 and GIP, alone or in combination, on human pancreatic islets

R. Lupi et al.

REGULATORY PEPTIDES (2010)

添加到收藏夹

Article Neurosciences

Immunohistochemical distribution of glucose-dependent insulinotropic polypeptide in the adult rat brain

Jenny Nyberg et al.

JOURNAL OF NEUROSCIENCE RESEARCH (2007)

添加到收藏夹

Article Biochemistry & Molecular Biology

Comparison of the subchronic antidiabetic effects of DPP IV-resistant GIP and GLP-1 analogues in obese diabetic (ob/ob) mice

Nigel Irwin et al.

JOURNAL OF PEPTIDE SCIENCE (2007)

添加到收藏夹

Review Gastroenterology & Hepatology

Biology of incretins: GLP-1 and GIP

Laurie L. Baggio et al.

GASTROENTEROLOGY (2007)

添加到收藏夹

Review Medicine, General & Internal

The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes

Daniel J. Drucker et al.

LANCET (2006)

添加到收藏夹

Article Pharmacology & Pharmacy

Prior in vitro exposure to GLP-1 with or without GIP can influence the subsequent beta cell responsiveness

D Delmeire et al.

BIOCHEMICAL PHARMACOLOGY (2004)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.