Glucagon‐like peptide‐1 in diabetes care: Can glycaemic control be achieved without nausea and vomiting?

Design and Evaluation of Peptide Dual-Agonists of GLP-1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis

(2021) Brandon T. Milliken et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2021) Qian Zhang et al.   Cell Metabolism

Synthesis, Optimization, and Biological Evaluation of Corrinated Conjugates of the GLP-1R Agonist Exendin-4

(2021) Ian C. Tinsley et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy and tolerability of tirzepatide, a dual glucose‐dependent insulinotropic peptide and glucagon‐like peptide‐1 receptor agonist in patients with type 2 diabetes: A 12‐week, randomized, double‐blind, placebo‐controlled study to evaluate different dose‐escalation regimens

(2020) Juan Pablo Frias et al.   DIABETES OBESITY & METABOLISM

Effects of Novel Dual GIP and GLP-1 Receptor Agonist Tirzepatide on Biomarkers of Nonalcoholic Steatohepatitis in Patients With Type 2 Diabetes

(2020) Mark L. Hartman et al.   DIABETES CARE

A second generation GLP ‐1 receptor agonist mitigates vomiting and anorexia while retaining glucoregulatory potency in lean diabetic and emetic mammalian models

(2020) Tito Borner et al.   DIABETES OBESITY & METABOLISM

Drug Therapy in Obesity: A Review of Current and Emerging Treatments

(2020) David M. Williams et al.   Diabetes Therapy

A Role for GLP-1 in Treating Hyperphagia and Obesity

(2020) Harvey J Grill   ENDOCRINOLOGY

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

(2020) Ricardo J. Samms et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Corrination of a GLP-1 Receptor Agonist for Glycemic Control without Emesis

(2020) Tito Borner et al.   Cell Reports

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

(2020) Francis S. Willard et al.   JCI Insight

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

(2020) Jennifer Trujillo   JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS

Glucagon-like peptide-1 receptor co-agonists for treating metabolic disease

(2020) Laurie L. Baggio et al.   Molecular Metabolism

The Role of Tirzepatide, Dual GIP and GLP-1 Receptor Agonist, in the Management of Type 2 Diabetes: The SURPASS Clinical Trials

(2020) Thinzar Min et al.   Diabetes Therapy

From the Incretin Concept and the Discovery of GLP-1 to Today's Diabetes Therapy

(2019) Jens Juul Holst   Frontiers in Endocrinology

Efficacy and safety of once-weekly semaglutide 1.0 mg vs once-daily liraglutide 1.2 mg as add-on to 1–3 oral antidiabetic drugs in subjects with type 2 diabetes (SUSTAIN 10)

(2019) M.S. Capehorn et al.   DIABETES & METABOLISM

WITHDRAWN: Global and regional diabetes prevalence estimates for 2019 and projections for 2030 and 2045: results from the International Diabetes Federation Diabetes Atlas, 9th edition

(2019) Pouya Saeedi et al.   DIABETES RESEARCH AND CLINICAL PRACTICE

Gut-derived GIP activates central Rap1 to impair neural leptin sensitivity during overnutrition

(2019) Kentaro Kaneko et al.   JOURNAL OF CLINICAL INVESTIGATION

Glucagon-like peptide 1 (GLP-1)

(2019) T.D. Müller et al.   Molecular Metabolism

Dual GIP–GLP1-Receptor Agonists In The Treatment Of Type 2 Diabetes: A Short Review On Emerging Data And Therapeutic Potential

(2019) Marie Bastin et al.   Diabetes Metabolic Syndrome and Obesity-Targets and Therapy

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Transporters

(2019) Stephen P H Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Enzymes

(2019) Stephen P H Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

Oral semaglutide for type 2 diabetes: A systematic review and meta‐analysis

(2019) Ioannis Avgerinos et al.   DIABETES OBESITY & METABOLISM

Effects on pancreatic Beta and other Islet cells of the glucose-dependent insulinotropic polypeptide

(2019) Rabeet Khan et al.   PEPTIDES

2019 Update to: Management of Hyperglycemia in Type 2 Diabetes, 2018. A Consensus Report by the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD)

(2019) John B. Buse et al.   DIABETES CARE

9. Pharmacologic Approaches to Glycemic Treatment: Standards of Medical Care in Diabetes—2020

(2019)   DIABETES CARE

MANAGEMENT OF ENDOCRINE DISEASE: Are all GLP-1 agonists equal in the treatment of type 2 diabetes?

(2019) Michael A Nauck et al.   EUROPEAN JOURNAL OF ENDOCRINOLOGY

Mechanisms of Action and Therapeutic Application of Glucagon-like Peptide-1

(2018) Daniel J. Drucker   Cell Metabolism

A vitamin B12 conjugate of exendin-4 improves glucose tolerance without associated nausea or hypophagia in rodents

(2018) Elizabeth G. Mietlicki-Baase et al.   DIABETES OBESITY & METABOLISM

Semaglutide induces weight loss in subjects with type 2 diabetes regardless of baseline BMI or gastrointestinal adverse events in the SUSTAIN 1 to 5 trials

(2018) Bo Ahrén et al.   DIABETES OBESITY & METABOLISM

MEDI0382, a GLP-1 and glucagon receptor dual agonist, in obese or overweight patients with type 2 diabetes: a randomised, controlled, double-blind, ascending dose and phase 2a study

(2018) Philip Ambery et al.   LANCET

Novel GLP-1/GLP-2 co-agonists display marked effects on gut volume and improves glycemic control in mice

(2018) Pernille Wismann et al.   PHYSIOLOGY & BEHAVIOR

CINV: still troubling patients after all these years

(2018) Matti Aapro   SUPPORTIVE CARE IN CANCER

Targeting GLP-1 receptor trafficking to improve agonist efficacy

(2018) Ben Jones et al.   Nature Communications

Chimeric peptide EP45 as a dual agonist at GLP-1 and NPY2R receptors

(2018) Oleg G. Chepurny et al.   Scientific Reports

Semaglutide versus dulaglutide once weekly in patients with type 2 diabetes (SUSTAIN 7): a randomised, open-label, phase 3b trial

(2018) Richard E Pratley et al.   Lancet Diabetes & Endocrinology

Recent updates on GLP-1 agonists: Current advancements & challenges

(2018) Dilip Sharma et al.   BIOMEDICINE & PHARMACOTHERAPY

Efficacy and safety of semaglutide compared with liraglutide and placebo for weight loss in patients with obesity: a randomised, double-blind, placebo and active controlled, dose-ranging, phase 2 trial

(2018) Patrick M O'Neil et al.   LANCET

Integrated Brain Atlas for Unbiased Mapping of Nervous System Effects Following Liraglutide Treatment

(2018) Casper Bo Gravesen Salinas et al.   Scientific Reports

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

(2018) Juan Pablo Frias et al.   LANCET

Anti-obesity effects of GIPR antagonists alone and in combination with GLP-1R agonists in preclinical models

(2018) Elizabeth A. Killion et al.   Science Translational Medicine

Optimized GIP analogs promote body weight lowering in mice through GIPR agonism not antagonism

(2018) Piotr A. Mroz et al.   Molecular 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

(2018) Tamer Coskun et al.   Molecular Metabolism

Pleiotropic Effects of GLP-1 and Analogs on Cell Signaling, Metabolism, and Function

(2018) Jordan Rowlands et al.   Frontiers in Endocrinology

Discovery, characterization, and clinical development of the glucagon-like peptides

(2017) Daniel J. Drucker et al.   JOURNAL OF CLINICAL INVESTIGATION

Obesity and Type 2 Diabetes: Two Diseases with a Need for Combined Treatment Strategies - EASO Can Lead the Way

(2017) Deborah R. Leitner et al.   Obesity Facts

Vitamin B12 deficiency

(2017) Ralph Green et al.   Nature Reviews Disease Primers

Reasons for discontinuation of GLP1 receptor agonists: data from a real-world cross-sectional survey of physicians and their patients with type 2 diabetes

(2017) Mirko Sikirica et al.   Diabetes Metabolic Syndrome and Obesity-Targets and Therapy

Unimolecular Polypharmacy for Treatment of Diabetes and Obesity

(2016) Matthias H. Tschöp et al.   Cell Metabolism

Once-Daily Liraglutide Versus Lixisenatide as Add-on to Metformin in Type 2 Diabetes: A 26-Week Randomized Controlled Clinical Trial

(2016) Michael Nauck et al.   DIABETES CARE

Occurrence of nausea, vomiting and diarrhoea reported as adverse events in clinical trials studying glucagon-like peptide-1 receptor agonists: A systematic analysis of published clinical trials

(2016) Karolin Bettge et al.   DIABETES OBESITY & METABOLISM

Efficacy and safety of dulaglutide in the treatment of type 2 diabetes: a comprehensive review of the dulaglutide clinical data focusing on the AWARD phase 3 clinical trial program

(2016) Johan Jendle et al.   DIABETES-METABOLISM RESEARCH AND REVIEWS

Excitatory Hindbrain–Forebrain Communication Is Required for Cisplatin-Induced Anorexia and Weight Loss

(2016) Amber L. Alhadeff et al.   JOURNAL OF NEUROSCIENCE

Endogenous Glucagon-like Peptide-1 Receptor Signaling in the Nucleus Tractus Solitarius is Required for Food Intake Control

(2016) Amber L Alhadeff et al.   NEUROPSYCHOPHARMACOLOGY

Reappraisal of GIP Pharmacology for Metabolic Diseases

(2016) Brian Finan et al.   TRENDS IN MOLECULAR MEDICINE

The incretin effect in healthy individuals and those with type 2 diabetes: physiology, pathophysiology, and response to therapeutic interventions

(2016) Michael A Nauck et al.   Lancet Diabetes & Endocrinology

Gastric inhibitory polypeptide immunoneutralization attenuates development of obesity in mice

(2015) Michael O. Boylan et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Review of head-to-head comparisons of glucagon-like peptide-1 receptor agonists

(2015) Sten Madsbad   DIABETES OBESITY & METABOLISM

Vitamin B12Conjugation of Peptide-YY3–36Decreases Food Intake Compared to Native Peptide-YY3–36Upon Subcutaneous Administration in Male Rats

(2015) Kelly E. Henry et al.   ENDOCRINOLOGY

Enhanced Peptide Stability Against Protease Digestion Induced by Intrinsic Factor Binding of a Vitamin B12 Conjugate of Exendin-4

(2015) Ron L. Bonaccorso et al.   MOLECULAR PHARMACEUTICS

Investigation of a Vitamin B12Conjugate as a PET Imaging Probe

(2014) Oluwatayo F. Ikotun et al.   ChemMedChem

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

(2014) Anna Secher et al.   JOURNAL OF CLINICAL INVESTIGATION

Neuronal GLP1R mediates liraglutide’s anorectic but not glucose-lowering effect

(2014) Stephanie Sisley et al.   JOURNAL OF CLINICAL INVESTIGATION

Measuring the nausea-to-emesis continuum in non-human animals: refocusing on gastrointestinal vagal signaling

(2014) Charles C. Horn   EXPERIMENTAL BRAIN RESEARCH

Vitamin B12: chemical modifications

(2013) Keith ó Proinsias et al.   CHEMICAL SOCIETY REVIEWS

The role of vagal neurocircuits in the regulation of nausea and vomiting

(2013) Tanja Babic et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Tolerability of nausea and vomiting and associations with weight loss in a randomized trial of liraglutide in obese, non-diabetic adults

(2013) M E J Lean et al.   INTERNATIONAL JOURNAL OF OBESITY

Tumor Imaging in Patients with Advanced Tumors Using a New 99mTc-Radiolabeled Vitamin B12 Derivative

(2013) B.-R. Sah et al.   JOURNAL OF NUCLEAR MEDICINE

Separation of emetic and anorexic responses of exendin-4, a GLP-1 receptor agonist in Suncus murinus (house musk shrew)

(2013) Sze Wa Chan et al.   NEUROPHARMACOLOGY

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

(2013) B. Finan et al.   Science Translational Medicine

Hindbrain Neurons as an Essential Hub in the Neuroanatomically Distributed Control of Energy Balance

(2012) Harvey J. Grill et al.   Cell Metabolism

Synthesis, Characterization and Pharmacodynamics of Vitamin-B12-Conjugated Glucagon-Like Peptide-1

(2012) Susan Clardy-James et al.   ChemMedChem

Vitamin B12 transport from food to the body's cells—a sophisticated, multistep pathway

(2012) Marianne J. Nielsen et al.   Nature Reviews Gastroenterology & Hepatology

Comparison of Recombinant Human Haptocorrin Expressed in Human Embryonic Kidney Cells and Native Haptocorrin

(2012) Evelyne Furger et al.   PLoS One

Brain activation following peripheral administration of the GLP-1 receptor agonist exendin-4

(2011) Elena-Dana Baraboi et al.   AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY

Peripheral and Central GLP-1 Receptor Populations Mediate the Anorectic Effects of Peripherally Administered GLP-1 Receptor Agonists, Liraglutide and Exendin-4

(2011) Scott E. Kanoski et al.   ENDOCRINOLOGY

A physiological role of glucagon-like peptide-1 receptors in the central nervous system of Suncus murinus (house musk shrew)

(2011) Sze Wa Chan et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Oral Delivery of the Appetite Suppressing Peptide hPYY(3–36) through the Vitamin B12Uptake Pathway

(2011) Christopher H. Fazen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hyperphagia and Increased Fat Accumulation in Two Models of Chronic CNS Glucagon-Like Peptide-1 Loss of Function

(2011) J. G. Barrera et al.   JOURNAL OF NEUROSCIENCE

The role of nausea in food intake and body weight suppression by peripheral GLP-1 receptor agonists, exendin-4 and liraglutide

(2011) Scott E. Kanoski et al.   NEUROPHARMACOLOGY

Preproglucagon neurons project widely to autonomic control areas in the mouse brain

(2011) I.J. Llewellyn-Smith et al.   NEUROSCIENCE

Exendin-4 increases blood glucose levels acutely in rats by activation of the sympathetic nervous system

(2010) Diego Pérez-Tilve et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Dose-dependent effects of the once-daily GLP-1 receptor agonist lixisenatide in patients with Type 2 diabetes inadequately controlled with metformin: a randomized, double-blind, placebo-controlled trial

(2010) R. E. Ratner et al.   DIABETIC MEDICINE

Pharmacokinetic and Pharmacodynamic Modeling of Exendin-4 in Type 2 Diabetic Goto-Kakizaki Rats

(2010) W. Gao et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Efficacy and safety of exenatide once weekly versus sitagliptin or pioglitazone as an adjunct to metformin for treatment of type 2 diabetes (DURATION-2): a randomised trial

(2010) Richard M Bergenstal et al.   LANCET

Role of the glucagon-like-peptide-1 receptor in the control of energy balance

(2010) Matthew R. Hayes et al.   PHYSIOLOGY & BEHAVIOR

Chemotherapy agent cisplatin induces 48-h Fos expression in the brain of a vomiting species, the house musk shrew (Suncus murinus)

(2009) Bart C. De Jonghe et al.   AMERICAN JOURNAL OF PHYSIOLOGY-REGULATORY INTEGRATIVE AND COMPARATIVE PHYSIOLOGY

A New Principle for Measurement of Cobalamin and Corrinoids, Used for Studies of Cobalamin Analogs on Serum Haptocorrin

(2009) T. F. Hardlei et al.   CLINICAL CHEMISTRY

Glucagon-Like Peptide 1/Glucagon Receptor Dual Agonism Reverses Obesity in Mice

(2009) A. Pocai et al.   DIABETES

Incretin-based therapies for type 2 diabetes mellitus

(2009) Julie A. Lovshin et al.   Nature Reviews Endocrinology

Amnionless (AMN) mutations in Imerslund–Gräsbeck syndrome may be associated with disturbed vitamin B12 transport into the CNS

(2008) A. S. Luder et al.   JOURNAL OF INHERITED METABOLIC DISEASE

Chemotherapy-Induced Nausea and Vomiting

(2008) Paul J. Hesketh   NEW ENGLAND JOURNAL OF MEDICINE

The Role of Incretins in Glucose Homeostasis and Diabetes Treatment

(2008) W. Kim et al.   PHARMACOLOGICAL REVIEWS