Efinopegdutide
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Efinopegdutide
Efinopegdutide (MK-6024) is a dual agonist of the glucagon and GLP-1 receptors. It is being developed by Merck for non-alcoholic fatty liver disease An alcohol-free or non-alcoholic drink, also known as a temperance drink, is a version of an alcoholic drink made without alcohol, or with the alcohol removed or reduced to almost zero. These may take the form of a non-alcoholic mixed drink or n .... It was also developed for type 2 diabetes and obesity but these indications were discontinued. References Glucagon receptor agonists GLP-1 receptor agonists Peptide therapeutics Drugs developed by Merck & Co. {{pharma-stub ...
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Glucagon Receptor Agonist
Glucagon receptor agonists are a class of drugs under development for the treatment of obesity, non-alcoholic fatty liver disease, and congenital hyperinsulinism. Background Glucagon is a hormone that generally opposes the action of insulin. It increases blood glucose by stimulating the production of glucose in the liver via glycogenolysis (breakdown of glycogen) and gluconeogenesis (production of glucose from non-carbohydrate sources). Glucagon also increases the breakdown of lipids and amino acids and the production of ketones. In healthy people, a low dose of exogenous glucagon increases energy expenditure and reduces energy intake without causing hyperglycemia. Glucagon is often elevated in type 2 diabetes; glucagon receptor antagonists were developed for the treatment of this disease but most were abandoned due to safety and adverse effects. Therapeutic uses Rescue glucagon has been a preferred treatment for hypoglycemic shocks in insulin-dependent diabetes since the 1960s ...
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GLP-1 Receptor Agonist
Glucagon-like peptide-1 (GLP-1) receptor agonists, also known as GLP-1 analogs, GLP-1RAs, or incretin mimetics, are a class of anorectic drugs that reduce blood sugar and energy intake by activating the GLP-1 receptor. They mimic the actions of the endogenous incretin hormone GLP-1, which is released by the gut after eating. GLP-1 agonists were initially developed for type 2 diabetes. The 2022 American Diabetes Association standards of medical care recommend GLP-1 agonists as a first-line therapy for type 2 diabetes, specifically in patients with atherosclerotic cardiovascular disease or obesity. The drugs were also noted to reduce food intake and body weight significantly, and some have been approved to treat obesity and other components of the metabolic syndrome in the absence of diabetes. They are also in development for other indications, such as non-alcoholic fatty liver disease, polycystic ovary syndrome, and diseases of the reward system such as addictions. Mechanism of ...
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Merck & Co
Merck & Co., Inc. is an American Multinational corporation, multinational pharmaceutical company headquartered in Rahway, New Jersey. The company does business as Merck Sharp & Dohme or MSD outside the United States and Canada. It is one of the largest pharmaceutical companies in the world, generally ranking in the global top five by revenue. Merck & Co. was originally established as the American affiliate of Merck Group in 1891. Merck develops and produces medicines, vaccines, biologic therapies and animal health products. It has several blockbuster products, including cancer immunotherapy, anti-diabetic medications, and vaccines for HPV and chickenpox, each generating significant revenue as of 2020. The company is ranked 71st on the 2022 Fortune 500, ''Fortune'' 500 and 87th on the 2022 Forbes Global 2000, ''Forbes'' Global 2000, both based on 2021 revenues. In 2023, the company’s seat in the ''Forbes'' Global 2000 was 73. Products The company develops medicines, vaccines, ...
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Non-alcoholic Fatty Liver Disease
An alcohol-free or non-alcoholic drink, also known as a temperance drink, is a version of an alcoholic drink made without alcohol, or with the alcohol removed or reduced to almost zero. These may take the form of a non-alcoholic mixed drink or non-alcoholic beer, and are widely available where alcoholic drinks are sold. Scientific definition Low-alcoholic drink Sparkling apple cider, soft drinks, and juice naturally contain trace amounts or no alcohol. Some fresh orange juices are above the UK 'alcohol free' limit of 0.05% ABV, as are some yogurts and rye bread. Ethanol distillation is used to separate alcoholic drinks into what are advertised as non-alcoholic drinks and spirits. Distilled wine produces low alcohol wine and brandy (from brandywine, derived from Dutch ''brandewijn'', "burning wine"). Distilled beer may be used to produce low-alcohol beer and whisky. However, alcoholic drinks cannot be further purified to 0.00% alcohol by volume by distillation, although sev ...
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Glucagon Receptor Agonists
Glucagon is a peptide hormone, produced by alpha cells of the pancreas. It raises the concentration of glucose and fatty acids in the bloodstream and is considered to be the main catabolic hormone of the body. It is also used as a medication to treat a number of health conditions. Its effect is opposite to that of insulin, which lowers extracellular glucose. It is produced from proglucagon, encoded by the ''GCG'' gene. The pancreas releases glucagon when the amount of glucose in the bloodstream is too low. Glucagon causes the liver to engage in glycogenolysis: converting stored glycogen into glucose, which is released into the bloodstream. High blood-glucose levels, on the other hand, stimulate the release of insulin. Insulin allows glucose to be taken up and used by insulin-dependent tissues. Thus, glucagon and insulin are part of a feedback system that keeps blood glucose levels stable. Glucagon increases energy expenditure and is elevated under conditions of stress. Glucagon be ...
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GLP-1 Receptor Agonists
Glucagon-like peptide-1 (GLP-1) receptor agonists, also known as GLP-1 analogs, GLP-1RAs, or incretin mimetics, are a class of anorectic drugs that reduce blood sugar and energy intake by activating the GLP-1 receptor. They mimic the actions of the endogenous incretin hormone GLP-1, which is released by the gut after eating. GLP-1 agonists were initially developed for type 2 diabetes. The 2022 American Diabetes Association standards of medical care recommend GLP-1 agonists as a first-line therapy for type 2 diabetes, specifically in patients with atherosclerotic cardiovascular disease or obesity. The drugs were also noted to reduce food intake and body weight significantly, and some have been approved to treat obesity and other components of the metabolic syndrome in the absence of diabetes. They are also in development for other indications, such as non-alcoholic fatty liver disease, polycystic ovary syndrome, and diseases of the reward system such as addictions. Mechanism of a ...
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Peptide Therapeutics
Peptide therapeutics are peptides or polypeptides (oligomers or short polymers of amino acids) which are used to for the treatment of diseases. Naturally occurring peptides may serve as hormones, growth factors, neurotransmitters, ion channel ligands, and anti-infectives; peptide therapeutics mimic such functions. Peptide Therapeutics are seen as relatively safe and well-tolerated as peptides can be Metabolism, metabolized by the body. Examples The current highest selling marketed diabetic drug Liraglutide, incorporates a lipid chain to extend plasma circulation and prolong bioavailability. Liraglutide is a GLP-1 agonist drug that Self-assembly, self-assembles into an alpha-helical structure, and it requires once a day administration. Lipid conjugation of a palmitoyl chain to a lysine residue at position 26 of Liraglutide results in an extended half-life (around 13–14 hours) in the blood. This is due to the palmitoyl chain allowing non covalent binding to albumin, which delays p ...
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