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Semaglutide
From Wikipedia, the free encyclopedia
Semaglutide, sold under the brand name Ozempic among others, is an antidiabetic medication used for the treatment of type 2 diabetes and long-term weight management.[15][16][17]
Semaglutide acts like human glucagon-like peptide-1 (GLP-1) in that it increases insulin secretion, thereby increasing sugar metabolism. It is distributed as a metered subcutaneous injection in a prefilled pen, or as an oral form. One of its advantages over other antidiabetic drugs is that it has a long duration of action, so a once-a-week injection is sufficient.[18]
An injectable version (Ozempic) was approved for medical use in the United States in December 2017,[19] and in the European Union,[12] Canada,[20] and Japan in 2018. A version which is taken by mouth (Rybelsus) was approved for medical use in the United States in September 2019,[21] and in the European Union in April 2020.[13] It is the first glucagon-like peptide receptor protein treatment approved for use in the United States that does not need to be injected.[22] It was developed by Novo Nordisk. Side effects include nausea, vomiting, diarrhea, abdominal pain, and constipation.[9]
In June 2021, the US Food and Drug Administration (FDA) approved semaglutide injection sold under the brand name Wegovy for long-term weight management in adults.[11][17]
Contents
Medical uses
Semaglutide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.[9][10]
Semaglutide (Wegovy) is also indicated as an adjunct to diet and exercise for long-term weight management in adults with obesity (initial body mass index (BMI) ≥ 30 kg/m2) or overweight (initial BMI ≥ 27 kg/m2) with at least one weight-related comorbidity.[11][14][17]
Adverse effects
Side effects include nausea, vomiting, diarrhea, abdominal pain, and constipation.[9] In people with heart problems, it can cause damage to the retina of the eye (retinopathy).[23] Other, less common side effects include kidney problems, allergic reactions, low blood sugar, and pancreatitis.[22]
Contraindications
It is contraindicated in patients with a personal or family history of medullary thyroid carcinoma and in patients with multiple endocrine neoplasia syndrome type 2.[10][9]
Mechanism of action
Semaglutide is a glucagon-like peptide-1 receptor agonist. It increases the production of insulin, a hormone that lowers the blood sugar level.[24] It also appears to enhance growth of β cells in the pancreas, which are the sites of insulin production.[25] It also inhibits glucagon, which is a hormone that increases blood sugar. It additionally reduces food intake by lowering appetite and slows down digestion in the stomach.[23] In this way it reduces body fat.[26]
Structure
Semaglutide is chemically similar to human glucagon-like peptide-1 (GLP-1), with 94% similarity. The only differences are two amino-acid substitutions at positions 8 and 34, where alanine and lysine are replaced by 2-aminoisobutyric acid and arginine, respectively.[27] Amino-acid substitution at position 8 prevents chemical breakdown by dipeptidyl peptidase-4. In addition, lysine at position 26 is in its derivative form (acylated with stearic diacid). Acylation with a spacer and C-18 fatty diacid chain increases the drug binding to blood protein (albumin), which enables longer presence in the blood circulation.[28] Its half-life in the blood is about 7 days (165–184 hours); therefore, once-weekly injection is enough.[18][25]
History
Semaglutide was developed in 2012,[29] by a team of researchers at Novo Nordisk as a longer-acting alternative to liraglutide.[30] It was given the brand name Ozempic. Clinical trials were started in 2015, and phase III was completed in 2016.[31][full citation needed]
Researchers at the University of Leeds and Novo Nordisk reported in 2017, that it can also be used for the treatment of obesity.[32] It reduces hunger, food craving and body fat.[33] A Phase 3 Randomized Controlled Trial found that once-weekly injection of 2.4 mg of the drug resulted in an average change of −14.9% body weight at 68 weeks compared to −2.4% for the placebo.[34]
The US FDA New Drug Application (NDA) was filed in December 2016, and in October 2017, the FDA Advisory Committee voted 16–0 in favor.[35] Approval was announced in December 2017.[19] It can be used as both injection-type or oral-type drug.[36] The marketing authorization in the European Union was granted in February 2018.[12][37] The Japanese Ministry of Health, Labour and Welfare announced approval on 23 March 2018.[38] Health Canada issued approval on 4 January 2018.[20]
Semaglutide was approved for medical use in Australia in August 2019 for "the treatment of adults with insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise; and as monotherapy when metformin is not tolerated or contraindicated."[1][3]
From Wikipedia, the free encyclopedia
Semaglutide, sold under the brand name Ozempic among others, is an antidiabetic medication used for the treatment of type 2 diabetes and long-term weight management.[15][16][17]
Semaglutide acts like human glucagon-like peptide-1 (GLP-1) in that it increases insulin secretion, thereby increasing sugar metabolism. It is distributed as a metered subcutaneous injection in a prefilled pen, or as an oral form. One of its advantages over other antidiabetic drugs is that it has a long duration of action, so a once-a-week injection is sufficient.[18]
An injectable version (Ozempic) was approved for medical use in the United States in December 2017,[19] and in the European Union,[12] Canada,[20] and Japan in 2018. A version which is taken by mouth (Rybelsus) was approved for medical use in the United States in September 2019,[21] and in the European Union in April 2020.[13] It is the first glucagon-like peptide receptor protein treatment approved for use in the United States that does not need to be injected.[22] It was developed by Novo Nordisk. Side effects include nausea, vomiting, diarrhea, abdominal pain, and constipation.[9]
In June 2021, the US Food and Drug Administration (FDA) approved semaglutide injection sold under the brand name Wegovy for long-term weight management in adults.[11][17]
Contents
Medical uses
Semaglutide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.[9][10]
Semaglutide (Wegovy) is also indicated as an adjunct to diet and exercise for long-term weight management in adults with obesity (initial body mass index (BMI) ≥ 30 kg/m2) or overweight (initial BMI ≥ 27 kg/m2) with at least one weight-related comorbidity.[11][14][17]
Adverse effects
Side effects include nausea, vomiting, diarrhea, abdominal pain, and constipation.[9] In people with heart problems, it can cause damage to the retina of the eye (retinopathy).[23] Other, less common side effects include kidney problems, allergic reactions, low blood sugar, and pancreatitis.[22]
Contraindications
It is contraindicated in patients with a personal or family history of medullary thyroid carcinoma and in patients with multiple endocrine neoplasia syndrome type 2.[10][9]
Mechanism of action
Semaglutide is a glucagon-like peptide-1 receptor agonist. It increases the production of insulin, a hormone that lowers the blood sugar level.[24] It also appears to enhance growth of β cells in the pancreas, which are the sites of insulin production.[25] It also inhibits glucagon, which is a hormone that increases blood sugar. It additionally reduces food intake by lowering appetite and slows down digestion in the stomach.[23] In this way it reduces body fat.[26]
Structure
Semaglutide is chemically similar to human glucagon-like peptide-1 (GLP-1), with 94% similarity. The only differences are two amino-acid substitutions at positions 8 and 34, where alanine and lysine are replaced by 2-aminoisobutyric acid and arginine, respectively.[27] Amino-acid substitution at position 8 prevents chemical breakdown by dipeptidyl peptidase-4. In addition, lysine at position 26 is in its derivative form (acylated with stearic diacid). Acylation with a spacer and C-18 fatty diacid chain increases the drug binding to blood protein (albumin), which enables longer presence in the blood circulation.[28] Its half-life in the blood is about 7 days (165–184 hours); therefore, once-weekly injection is enough.[18][25]
History
Semaglutide was developed in 2012,[29] by a team of researchers at Novo Nordisk as a longer-acting alternative to liraglutide.[30] It was given the brand name Ozempic. Clinical trials were started in 2015, and phase III was completed in 2016.[31][full citation needed]
Researchers at the University of Leeds and Novo Nordisk reported in 2017, that it can also be used for the treatment of obesity.[32] It reduces hunger, food craving and body fat.[33] A Phase 3 Randomized Controlled Trial found that once-weekly injection of 2.4 mg of the drug resulted in an average change of −14.9% body weight at 68 weeks compared to −2.4% for the placebo.[34]
The US FDA New Drug Application (NDA) was filed in December 2016, and in October 2017, the FDA Advisory Committee voted 16–0 in favor.[35] Approval was announced in December 2017.[19] It can be used as both injection-type or oral-type drug.[36] The marketing authorization in the European Union was granted in February 2018.[12][37] The Japanese Ministry of Health, Labour and Welfare announced approval on 23 March 2018.[38] Health Canada issued approval on 4 January 2018.[20]
Semaglutide was approved for medical use in Australia in August 2019 for "the treatment of adults with insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise; and as monotherapy when metformin is not tolerated or contraindicated."[1][3]
