Clinical data | |
---|---|
Other names | IBI362; LY3305677 |
Legal status | |
Legal status |
|
Identifiers | |
| |
CAS Number | |
PubChem CID | |
UNII | |
Chemical and physical data | |
Formula | C207H317N45O65 |
Molar mass | 4476.063 g·mol−1 |
3D model (JSmol) | |
| |
|
Mazdutide (also known as IBI362 or LY3305677) is a dual agonist of the GLP-1 receptor and glucagon receptor. It is an analog of oxyntomodulin (OXM). [1] [2] [3] The drug is developed by Eli Lilly and is currently in multiple Phase III studies. [4] [5]
Satiety is a state or condition of fullness gratified beyond the point of satisfaction, the opposite of hunger. Following satiation, satiety is a feeling of fullness lasting until the next meal. When food is present in the GI tract after a meal, satiety signals overrule hunger signals, but satiety slowly fades as hunger increases.
Anti-obesity medication or weight loss medications are pharmacological agents that reduce or control excess body fat. These medications alter one of the fundamental processes of the human body, weight regulation, by: reducing appetite and consequently energy intake, increasing energy expenditure, redirecting nutrients from adipose to lean tissue, or interfering with the absorption of calories.
Glucagon-like peptide-1 (GLP-1) is a 30- or 31-amino-acid-long peptide hormone deriving from the tissue-specific posttranslational processing of the proglucagon peptide. It is produced and secreted by intestinal enteroendocrine L-cells and certain neurons within the nucleus of the solitary tract in the brainstem upon food consumption. The initial product GLP-1 (1–37) is susceptible to amidation and proteolytic cleavage, which gives rise to the two truncated and equipotent biologically active forms, GLP-1 (7–36) amide and GLP-1 (7–37). Active GLP-1 protein secondary structure includes two α-helices from amino acid position 13–20 and 24–35 separated by a linker region.
Romance of the Three Kingdoms is a Chinese television series adapted from the classical 14th century novel of the same title by Luo Guanzhong. The series was produced by China Central Television (CCTV) and was first aired on the network in 1994. It spanned a total of 84 episodes, each approximately 45 minutes long. One of the most expensive television series produced at the time, the project cost 170 million yuan. It was completed over four years and involved over 400,000 cast and crew members, including divisions of the People's Liberation Army from the Beijing, Nanjing and Chengdu military regions. Some of the dialogue spoken by characters was adapted directly from the novel. Extensive battle scenes, such as the battles of Guandu, Red Cliffs and Xiaoting, were also live-acted.
The glucagon-like peptide-1 receptor (GLP1R) is a G protein-coupled receptor (GPCR) found on beta cells of the pancreas and on neurons of the brain. It is involved in the control of blood sugar level by enhancing insulin secretion. In humans it is synthesised by the gene GLP1R, which is present on chromosome 6. It is a member of the glucagon receptor family of GPCRs. GLP1R is composed of two domains, one extracellular (ECD) that binds the C-terminal helix of GLP-1, and one transmembrane (TMD) domain that binds the N-terminal region of GLP-1. In the TMD domain there is a fulcrum of polar residues that regulates the biased signaling of the receptor while the transmembrane helical boundaries and extracellular surface are a trigger for biased agonism.
Cinchonine is an alkaloid found in Cinchona officinalis. It is used in asymmetric synthesis in organic chemistry. It is a stereoisomer and pseudo-enantiomer of cinchonidine.
Glucagon-like peptide-1 (GLP-1) receptor agonists, also known as GLP-1 analogs, GLP-1DAs 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 that is released by the gut after eating.
Amazing Detective Di Renjie 2, also known as Shen Tan Di Renjie 2, is the second installment in a four-season Chinese television series based on gong'an detective stories related to Di Renjie, a Tang dynasty magistrate and statesman. Written and directed by Qian Yanqiu, the series starred Liang Guanhua as the titular protagonist, and was first broadcast on CCTV-8 on 20 November 2006, two years after the first season. It was followed by Amazing Detective Di Renjie 3 in 2008, and Mad Detective Di Renjie in 2010. The series was released in the United States on March 21, 2018 on Toku.
Dulaglutide, sold under the brand name Trulicity among others, is a medication used for the treatment of type 2 diabetes in combination with diet and exercise. It is also approved in the United States for the reduction of major adverse cardiovascular events in adults with type 2 diabetes who have established cardiovascular disease or multiple cardiovascular risk factors.
Cotadutide is an experimental drug for the treatment of type 2 diabetes mellitus. It lowers blood glucose levels by mimicking the human hormones glucagon-like peptide 1 and glucagon, which play a role in blood sugar regulation. The drug is a peptide that is injected under the skin.
Tirzepatide is an antidiabetic medication used for the treatment of type 2 diabetes and for weight loss. Tirzepatide is administered via subcutaneous injections. It is sold under the brand names Mounjaro for diabetes treatment, and Zepbound for weight loss.
Cagrilintide/semaglutide, marketed as CagriSema, is a combination of cagrilintide, a dual amylin and calcitonin receptor agonist, and semaglutide, a GLP-1 agonist. It is injected once weekly and is being tested in type 2 diabetes and obesity. Preliminary trial results found a greater weight loss compared to either medication alone. HbA1c was significantly improved compared to cagrilintide alone and non-significantly better than semaglutide alone. In a Phase II trial, weight loss averaged -15.6 percent after 32 weeks, making CagriSema comparable in efficacy to tirzepatide. A future trial sponsored by Novo Nordisk is comparing tirzepatide and CagriSema head-to-head. As of 2023, CagriSema is in a Phase III trial.
Ecnoglutide (XW003) is a GLP-1 agonist being developed for the treatment of obesity and type 2 diabetes. In preclinical trials, "Ecnoglutide showed a favorable potency, pharmacokinetic, and tolerability profile, as well as a simplified manufacturing process" compared to other GLP-1 agonists.
GLP1 poly-agonist peptides are a class of drugs that activate multiple peptide hormone receptors including the glucagon-like peptide-1 (GLP-1) receptor. These drugs are developed for the same indications as GLP-1 receptor agonists—especially obesity, type 2 diabetes, and non-alcoholic fatty liver disease. They are expected to provide superior efficacy with fewer adverse effects compared to GLP-1 mono-agonists, which are dose-limited by gastrointestinal disturbances. The effectiveness of multi-receptor agonists could possibly equal or exceed that of bariatric surgery. The first such drug to receive approval is tirzepatide, a dual agonist of GLP-1 and GIP receptors.
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. It was also developed for type 2 diabetes and obesity but these indications were discontinued.
Cofrogliptin is a long-acting DPP4 inhibitor dosed once every two weeks.
HRS9531 is an experimental GLP-1 and GIPR dual agonist developed by Jiangsu Hengrui.
HEC96719 is a tricyclic farnesoid X receptor agonist developed for non-alcoholic steatohepatitis.
Pemvidutide (ALT-801) is an experimental dual GLP-1/glucagon receptor agonist developed by Altimmune. The drug reduced LDL-C in a clinical trial and does not require dose titration as with GLP-1 mono agonists.
VK2735 is a dual agonist of the GLP-1 receptor and GIP receptor, with a similar mechanism of action as tirzepatide, which acts on the same receptors. It is injectable and is being developed by Viking Therapeutics.