Emerging hormonal-based combination pharmacotherapies for the treatment of metabolic diseases

Inactivation of the Glucose-Dependent Insulinotropic Polypeptide Receptor Improves Outcomes following Experimental Myocardial Infarction

(2018) John R. Ussher et al.   Cell Metabolism

Effect of a glucagon receptor antibody (REMD-477) in type 1 diabetes: A randomized controlled trial

(2018) Jeremy Pettus et al.   DIABETES OBESITY & METABOLISM

Toward Precision Approaches for the Prevention and Treatment of Obesity

(2018) Susan Z. Yanovski et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Estrogen receptor α protects pancreatic β-cells from apoptosis by preserving mitochondrial function and suppressing endoplasmic reticulum stress

(2018) Zhenqi Zhou et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multidose Formulations

(2018) Andreas Evers et al.   JOURNAL OF MEDICINAL CHEMISTRY

NGM282 for treatment of non-alcoholic steatohepatitis: a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

(2018) Stephen A Harrison et al.   LANCET

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

Direct effects of thyroid hormones on hepatic lipid metabolism

(2018) Rohit A. Sinha et al.   Nature Reviews Endocrinology

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

Glucagon-like Peptide-1 Receptor Agonists and Cardiovascular Events: Class Effects versus Individual Patterns

(2018) Soo Lim et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Glucagon Receptor Antagonism Improves Glucose Metabolism and Cardiac Function by Promoting AMP-Mediated Protein Kinase in Diabetic Mice

(2018) Ankit X. Sharma et al.   Cell Reports

Dulaglutide as add-on therapy to SGLT2 inhibitors in patients with inadequately controlled type 2 diabetes (AWARD-10): a 24-week, randomised, double-blind, placebo-controlled trial

(2018) Bernhard Ludvik et al.   Lancet Diabetes & Endocrinology

FGF21, a liver hormone that inhibits alcohol intake in mice, increases in human circulation after acute alcohol ingestion and sustained binge drinking at Oktoberfest

(2018) Susanna Søberg et al.   Molecular Metabolism

The incretin hormone GIP is upregulated in patients with atherosclerosis and stabilizes plaques in ApoE −/− mice by blocking monocyte/macrophage activation

(2018) Florian Kahles et al.   Molecular Metabolism

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

Structures of β-klotho reveal a ‘zip code’-like mechanism for endocrine FGF signalling

(2018) Sangwon Lee et al.   NATURE

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

Albiglutide and cardiovascular outcomes in patients with type 2 diabetes and cardiovascular disease (Harmony Outcomes): a double-blind, randomised placebo-controlled trial

(2018) Adrian F Hernandez et al.   LANCET

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

Safety and Efficacy of Teduglutide (Gattex) in Patients With Crohn’s Disease and Need for Parenteral Support Due to Short Bowel Syndrome–associated Intestinal Failure

(2017) Bharati Kochar et al.   JOURNAL OF CLINICAL GASTROENTEROLOGY

Mouse species-specific control of hepatocarcinogenesis and metabolism by FGF19/FGF15

(2017) Mei Zhou et al.   JOURNAL OF HEPATOLOGY

Design of Novel Exendin-Based Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists

(2017) Andreas Evers et al.   JOURNAL OF MEDICINAL CHEMISTRY

GUB06-046, a novel secretin/glucagon-like peptide 1 co-agonist, decreases food intake, improves glycemic control, and preserves beta cell mass in diabetic mice

(2017) Søren B. van Witteloostuijn et al.   JOURNAL OF PEPTIDE SCIENCE

The Dual Amylin- and Calcitonin-Receptor Agonist KBP-042 Works as Adjunct to Metformin on Fasting Hyperglycemia and HbA1c in a Rat Model of Type 2 Diabetes

(2017) Sara T. Hjuler et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

3 years of liraglutide versus placebo for type 2 diabetes risk reduction and weight management in individuals with prediabetes: a randomised, double-blind trial

(2017) Carel W le Roux et al.   LANCET

Drug development in the era of precision medicine

(2017) Sarah A. Dugger et al.   NATURE REVIEWS DRUG DISCOVERY

Mechanisms, Pathophysiology, and Management of Obesity

(2017) Steven B. Heymsfield et al.   NEW ENGLAND JOURNAL OF MEDICINE

Effects of Once-Weekly Exenatide on Cardiovascular Outcomes in Type 2 Diabetes

(2017) Rury R. Holman et al.   NEW ENGLAND JOURNAL OF MEDICINE

The New Biology and Pharmacology of Glucagon

(2017) T. D. Müller et al.   PHYSIOLOGICAL REVIEWS

Effect of Sodium‐Glucose Cotransport‐2 Inhibitors on Blood Pressure in People With Type 2 Diabetes Mellitus: A Systematic Review and Meta‐Analysis of 43 Randomized Control Trials With 22 528 Patients

(2017) Mohsen Mazidi et al.   Journal of the American Heart Association

Fibroblast growth factor 21 (FGF21) is robustly induced by ethanol and has a protective role in ethanol associated liver injury

(2017) Bhavna N. Desai et al.   Molecular Metabolism

Circulating FGF21 in humans is potently induced by short term overfeeding of carbohydrates

(2017) Anne-Marie Lundsgaard et al.   Molecular Metabolism

Monomeric GLP-1/GIP/glucagon triagonism corrects obesity, hepatosteatosis, and dyslipidemia in female mice

(2017) Sigrid Jall et al.   Molecular Metabolism

KBP-088, a novel DACRA with prolonged receptor activation, is superior to davalintide in terms of efficacy on body weight

(2016) Sofie Gydesen et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

FGF21 Regulates Sweet and Alcohol Preference

(2016) Saswata Talukdar et al.   Cell Metabolism

iNKT Cells Induce FGF21 for Thermogenesis and Are Required for Maximal Weight Loss in GLP1 Therapy

(2016) Lydia Lynch et al.   Cell Metabolism

A Long-Acting FGF21 Molecule, PF-05231023, Decreases Body Weight and Improves Lipid Profile in Non-human Primates and Type 2 Diabetic Subjects

(2016) Saswata Talukdar et al.   Cell Metabolism

Unimolecular Polypharmacy for Treatment of Diabetes and Obesity

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

The Intestinal Immune System in Obesity and Insulin Resistance

(2016) Daniel A. Winer et al.   Cell Metabolism

FGF21 Mediates Endocrine Control of Simple Sugar Intake and Sweet Taste Preference by the Liver

(2016) Stephanie von Holstein-Rathlou et al.   Cell Metabolism

Robust anti-obesity and metabolic effects of a dual GLP-1/glucagon receptor peptide agonist in rodents and non-human primates

(2016) S. J. Henderson et al.   DIABETES OBESITY & METABOLISM

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

Renaissance of leptin for obesity therapy

(2016) Carmelo Quarta et al.   DIABETOLOGIA

Neurotensin Is Coexpressed, Coreleased, and Acts Together With GLP-1 and PYY in Enteroendocrine Control of Metabolism

(2016) Kaare V. Grunddal et al.   ENDOCRINOLOGY

Glucose-Dependent Insulinotropic Polypeptide Is Associated With Lower Low-Density Lipoprotein But Unhealthy Fat Distribution, Independent of Insulin: The ADDITION-PRO Study

(2016) Cathrine Laustrup Møller et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Insulin Plays a Permissive Role for the Vasoactive Effect of GIP Regulating Adipose Tissue Metabolism in Humans

(2016) Meena Asmar et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Central injection of fibroblast growth factor 1 induces sustained remission of diabetic hyperglycemia in rodents

(2016) Jarrad M Scarlett et al.   NATURE MEDICINE

Cardiovascular effects of bariatric surgery

(2016) Andrew J. Beamish et al.   Nature Reviews Cardiology

GLP-1 and estrogen conjugate acts in the supramammillary nucleus to reduce food-reward and body weight

(2016) Heike Vogel et al.   NEUROPHARMACOLOGY

Semaglutide and Cardiovascular Outcomes in Patients with Type 2 Diabetes

(2016) Steven P. Marso et al.   NEW ENGLAND JOURNAL OF MEDICINE

Liraglutide and Cardiovascular Outcomes in Type 2 Diabetes

(2016) Steven P. Marso et al.   NEW ENGLAND JOURNAL OF MEDICINE

The dual amylin- and calcitonin-receptor agonist KBP-042 increases insulin sensitivity and induces weight loss in rats with obesity

(2016) Sara Toftegaard Hjuler et al.   Obesity

Skeletal muscle action of estrogen receptor α is critical for the maintenance of mitochondrial function and metabolic homeostasis in females

(2016) Vicent Ribas et al.   Science Translational Medicine

Reappraisal of GIP Pharmacology for Metabolic Diseases

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

Exenatide once weekly plus dapagliflozin once daily versus exenatide or dapagliflozin alone in patients with type 2 diabetes inadequately controlled with metformin monotherapy (DURATION-8): a 28 week, multicentre, double-blind, phase 3, randomised controlled trial

(2016) Juan P Frías et al.   Lancet Diabetes & Endocrinology

Cooperative interaction between leptin and amylin signaling in the ventral tegmental area for the control of food intake

(2015) Elizabeth G. Mietlicki-Baase et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Species-specific action of (Pro3)GIP - a full agonist at human GIP receptors, but a partial agonist and competitive antagonist at rat and mouse GIP receptors

(2015) A H Sparre-Ulrich et al.   BRITISH JOURNAL OF PHARMACOLOGY

Neural Control of Energy Balance: Translating Circuits to Therapies

(2015) Laurent Gautron et al.   CELL

The Role of Gut Adaptation in the Potent Effects of Multiple Bariatric Surgeries on Obesity and Diabetes

(2015) Randy J. Seeley et al.   Cell Metabolism

Weight Management in Type 2 Diabetes: Current and Emerging Approaches to Treatment

(2015) Luc Van Gaal et al.   DIABETES CARE

Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies

(2015) Christof M. Kazda et al.   DIABETES CARE

Dual melanocortin-4 receptor and GLP-1 receptor agonism amplifies metabolic benefits in diet-induced obese mice

(2015) C. Clemmensen et al.   EMBO Molecular Medicine

KBP-042 improves bodyweight and glucose homeostasis with indices of increased insulin sensitivity irrespective of route of administration

(2015) Sara T. Hjuler et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Evidence against hypothalamic-pituitary-adrenal axis suppression in the antidiabetic action of leptin

(2015) Gregory J. Morton et al.   JOURNAL OF CLINICAL INVESTIGATION

TCF1 links GIPR signaling to the control of beta cell function and survival

(2015) Jonathan E Campbell et al.   NATURE MEDICINE

Therapeutic potential of the endocrine fibroblast growth factors FGF19, FGF21 and FGF23

(2015) Chiara Degirolamo et al.   NATURE REVIEWS DRUG DISCOVERY

Empagliflozin, Cardiovascular Outcomes, and Mortality in Type 2 Diabetes

(2015) Bernard Zinman et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Randomized, Controlled Trial of 3.0 mg of Liraglutide in Weight Management

(2015) Xavier Pi-Sunyer et al.   NEW ENGLAND JOURNAL OF MEDICINE

Lixisenatide in Patients with Type 2 Diabetes and Acute Coronary Syndrome

(2015) Marc A. Pfeffer et al.   NEW ENGLAND JOURNAL OF MEDICINE

The anti-diabetic effects of GLP-1-gastrin dual agonist ZP3022 in ZDF rats

(2015) Jolanta Skarbaliene et al.   PEPTIDES

FGF21 Revolutions: Recent Advances Illuminating FGF21 Biology and Medicinal Properties

(2015) Alexei Kharitonenkov et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Effect of targeted estrogen delivery using glucagon-like peptide-1 on insulin secretion, insulin sensitivity and glucose homeostasis

(2015) Joseph P. Tiano et al.   Scientific Reports

FGF21-Mediated Improvements in Glucose Clearance Require Uncoupling Protein 1

(2015) Michelle M. Kwon et al.   Cell Reports

Pharmacological Activation of Thyroid Hormone Receptors Elicits a Functional Conversion of White to Brown Fat

(2015) Jean Z. Lin et al.   Cell Reports

A novel oral dual amylin and calcitonin receptor agonist (KBP-042) exerts antiobesity and antidiabetic effects in rats

(2014) Kim V. Andreassen et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Estradiol Regulates Brown Adipose Tissue Thermogenesis via Hypothalamic AMPK

(2014) Pablo B. Martínez de Morentin et al.   Cell Metabolism

A Missing Link in Body Weight Homeostasis: The Catabolic Signal of the Overfed State

(2014) Yann Ravussin et al.   Cell Metabolism

Identification and Saturable Nature of Signaling Pathways Induced by Metreleptin in Humans: Comparative Evaluation of In Vivo, Ex Vivo, and In Vitro Administration

(2014) Hyun-Seuk Moon et al.   DIABETES

GLP-1–oestrogen attenuates hyperphagia and protects from beta cell failure in diabetes-prone New Zealand obese (NZO) mice

(2014) Robert W. Schwenk et al.   DIABETOLOGIA

Estrogens stimulate serotonin neurons to inhibit binge-like eating in mice

(2014) Xuehong Cao et al.   JOURNAL OF CLINICAL INVESTIGATION

Endocrinization of FGF1 produces a neomorphic and potent insulin sensitizer

(2014) Jae Myoung Suh et al.   NATURE

Leptin reverses diabetes by suppression of the hypothalamic-pituitary-adrenal axis

(2014) Rachel J Perry et al.   NATURE MEDICINE

A rationally designed monomeric peptide triagonist corrects obesity and diabetes in rodents

(2014) Brian Finan et al.   NATURE MEDICINE

Targeting inflammation in the treatment of type 2 diabetes: time to start

(2014) Marc Y. Donath   NATURE REVIEWS DRUG DISCOVERY

Mechanisms of changes in glucose metabolism and bodyweight after bariatric surgery

(2014) Sten Madsbad et al.   Lancet Diabetes & Endocrinology

The Effects of LY2405319, an FGF21 Analog, in Obese Human Subjects with Type 2 Diabetes

(2013) Gregory Gaich et al.   Cell Metabolism

GLP-1/Glucagon Coagonism Restores Leptin Responsiveness in Obese Mice Chronically Maintained on an Obesogenic Diet

(2013) C. Clemmensen et al.   DIABETES

Vertical Sleeve Gastrectomy Is Effective in Two Genetic Mouse Models of Glucagon-Like Peptide 1 Receptor Deficiency

(2013) H. E. Wilson-Perez et al.   DIABETES

FGF19 action in the brain induces insulin-independent glucose lowering

(2013) Gregory J. Morton et al.   JOURNAL OF CLINICAL INVESTIGATION

FGF21 contributes to neuroendocrine control of female reproduction

(2013) Bryn M Owen et al.   NATURE MEDICINE

Improved Glucose Control and Reduced Body Weight in Rodents with Dual Mechanism of Action Peptide Hybrids

(2013) James L. Trevaskis et al.   PLoS One

Acute effects of continuous infusions of glucagon-like peptide (GLP)-1, GLP-2 and the combination (GLP-1+GLP-2) on intestinal absorption in short bowel syndrome (SBS) patients. A placebo-controlled study

(2013) K.B. Madsen et al.   REGULATORY PEPTIDES

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

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

Leptin reverses declines in satiation in weight-reduced obese humans

(2012) Harry R Kissileff et al.   AMERICAN JOURNAL OF CLINICAL NUTRITION

Central Nervous System Mechanisms Linking the Consumption of Palatable High-Fat Diets to the Defense of Greater Adiposity

(2012) Karen K. Ryan et al.   Cell Metabolism

Coadministration of Glucagon-Like Peptide-1 During Glucagon Infusion in Humans Results in Increased Energy Expenditure and Amelioration of Hyperglycemia

(2012) T. M. Tan et al.   DIABETES

The novel GLP-1-gastrin dual agonist, ZP3022, increases β-cell mass and prevents diabetes in db/db mice

(2012) K. Fosgerau et al.   DIABETES OBESITY & METABOLISM

Combination therapy with GLP-1 receptor agonists and basal insulin: a systematic review of the literature

(2012) R. Balena et al.   DIABETES OBESITY & METABOLISM

Fibroblast Growth Factor-19 Action in the Brain Reduces Food Intake and Body Weight and Improves Glucose Tolerance in Male Rats

(2012) Karen K. Ryan et al.   ENDOCRINOLOGY

Restoration of leptin responsiveness in diet-induced obese mice using an optimized leptin analog in combination with exendin-4 or FGF21

(2012) Timo D. Müller et al.   JOURNAL OF PEPTIDE SCIENCE

Targeted estrogen delivery reverses the metabolic syndrome

(2012) Brian Finan et al.   NATURE MEDICINE

Fibroblast growth factor 21 promotes bone loss by potentiating the effects of peroxisome proliferator-activated receptor  

(2012) W. Wei et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Efficacy of Metreleptin in Obese Patients With Type 2 Diabetes: Cellular and Molecular Pathways Underlying Leptin Tolerance

(2011) H.-S. Moon et al.   DIABETES

Subcutaneous administration of leptin normalizes fasting plasma glucose in obese type 2 diabetic UCD-T2DM rats

(2011) B. P. Cummings et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Leptin Deficiency Causes Insulin Resistance Induced by Uncontrolled Diabetes

(2010) J. P. German et al.   DIABETES

Leptin Activates a Novel CNS Mechanism for Insulin-Independent Normalization of Severe Diabetic Hyperglycemia

(2010) Jonathan P. German et al.   ENDOCRINOLOGY

The anorexigenic effects of metformin involve increases in hypothalamic leptin receptor expression

(2010) Grégory Aubert et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Central and Peripheral Administration of Secretin Inhibits Food Intake in Mice through the Activation of the Melanocortin System

(2010) Carrie Yuen Yee Cheng et al.   NEUROPSYCHOPHARMACOLOGY

Direct medical cost of overweight and obesity in the USA: a quantitative systematic review

(2010) A. G. Tsai et al.   Obesity Reviews

Leptin therapy in insulin-deficient type I diabetes

(2010) M.-y. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Leptin therapy improves insulin-deficient type 1 diabetes by CNS-dependent mechanisms in mice

(2010) T. Fujikawa et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2009) A. Pocai et al.   DIABETES

Mechanisms of Amylin/Leptin Synergy in Rodent Models

(2009) Victoria F. Turek et al.   ENDOCRINOLOGY

Changes in gut microbiota control inflammation in obese mice through a mechanism involving GLP-2-driven improvement of gut permeability

(2009) P. D. Cani et al.   GUT

A new glucagon and GLP-1 co-agonist eliminates obesity in rodents

(2009) Jonathan W Day et al.   Nature Chemical Biology

Enhanced Weight Loss With Pramlintide/Metreleptin: An Integrated Neurohormonal Approach to Obesity Pharmacotherapy

(2009) Eric Ravussin et al.   Obesity

Combination Therapy With Glucagon-Like Peptide-1 and Gastrin Restores Normoglycemia in Diabetic NOD Mice

(2008) W. L. Suarez-Pinzon et al.   DIABETES

Four weeks of near-normalisation of blood glucose improves the insulin response to glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide in patients with type 2 diabetes

(2008) P. V. Højberg et al.   DIABETOLOGIA

Making insulin-deficient type 1 diabetic rodents thrive without insulin

(2008) X. Yu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Leptin responsiveness restored by amylin agonism in diet-induced obesity: Evidence from nonclinical and clinical studies

(2008) J. D. Roth et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA