Orforglipron
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Orforglipron
Orforglipron (LY-3502970) is an oral, non-peptide, small-molecule GLP-1 receptor agonist developed as a weight loss drug by Eli Lilly and Company. It was discovered by Chugai Pharmaceutical Co., then was licensed to Lilly in 2018. Orforglipron is easier to produce than existing peptide GLP-1 agonists and is expected to be cheaper. Mechanism Orforglipron is a small-molecule, partial GLP-1 receptor agonist affecting the activity of cyclic adenosine monophosphate (cAMP); its effects are similar to the actions of glucagon-like peptide-1 (GLP-1) for reducing food intake and lowering blood glucose levels. Clinical trials The results of Phase I safety and Phase II ascending-dose clinical trials enrolling people with obesity or type 2 diabetes were published in 2023. Orforglipron has a half-life of 29 to 49 hours across the doses tested and is taken once per day by mouth without food or water restrictions. Safety and dosing trials showed that the incidence of adverse events in ...
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Danuglipron
Danuglipron is a small-molecule GLP-1 agonist, formerly under development by Pfizer that, in an oral formulation, was under investigation as a therapy for diabetes mellitus. Initial results from a randomized controlled trial indicated that it reduced weight and improved diabetic control. The most commonly reported adverse events were nausea, diarrhea, and vomiting. However, in April 2025, Pfizer announced it would abandon further development of Danuglipron due to unpredictable liver toxicity. See also * Lotiglipron Lotiglipron is a non-peptide glucagon-like peptide-1 receptor agonist which was under development by Pfizer as a weight loss drug. However, it was withdrawn from development in June 2023, after early stage clinical trial Clinical trials are p ... * Orforglipron References GLP-1 receptor agonists Experimental diabetes drugs Nitriles Fluoroarenes Disubstituted pyridines Ethers Piperidines Oxetanes Benzimidazoles Carboxylic acids Abandoned drugs ...
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Lotiglipron
Lotiglipron is a non-peptide glucagon-like peptide-1 receptor agonist which was under development by Pfizer as a weight loss drug. However, it was withdrawn from development in June 2023, after early stage clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...s showed elevated liver enzymes which could indicate potential for liver toxicity. See also * Danuglipron * Orforglipron References {{Oral hypoglycemics and insulin analogs Experimental drugs GLP-1 receptor agonists Chloropyridines Piperidines Benzimidazoles Benzodioxoles Oxetanes Carboxylic acids Disubstituted pyridines ...
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Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ...
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Gastrointestinal Disease
Gastrointestinal diseases (abbrev. GI diseases or GI illnesses) refer to diseases involving the Human gastrointestinal tract, gastrointestinal tract, namely the esophagus, stomach, small intestine, large intestine and rectum; and the accessory organs of digestion, the liver, gallbladder, and pancreas. Oral disease The oral cavity is part of the gastrointestinal system and as such the presence of alterations in this district can be the first sign of both systemic and gastrointestinal diseases. By far the most common oral conditions are dental plaque, plaque-induced diseases (e.g., gingivitis, periodontitis, dental caries). Oral symptoms can be similar to lesions occurring elsewhere in the digestive tract, with a pattern of swelling, inflammation, ulcers, and fissures. If these signs are present, then patients are more likely to also have anal and esophageal lesions and experience other extra-intestinal disease manifestations. Some diseases which involve other parts of the GI ...
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Fluoroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ...
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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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Experimental Anti-obesity Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons (e ...
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American Diabetes Association
The American Diabetes Association (ADA) is a United States-based nonprofit that seeks to educate the public about diabetes and to help those affected by it through funding research to manage, cure and prevent diabetes, including type 1 diabetes, type 2 diabetes, gestational diabetes, and pre-diabetes. It is a network of 565,000 volunteers which includes 20,000 healthcare professionals and administration staff members. History The ADA was formally founded in 1939. It was founded by six physicians − including Dr. Herman O. Mosenthal, Dr. Joseph T. Beardwood Jr., Dr. Joseph H. Barach, and Dr. E. S. Dillion − at their annual meeting of the American College of Physicians. Each year the ADA hosts Scientific Sessions, a meeting for diabetes professionals. The ADA has nearly 20,000 members. In the early 2000s, the ADA struck a three-year, $1.5 million sponsorship deal with Cadbury-Schweppes, the world's largest confectioner products including Diet-Rite sodas, Snapple unsweet ...
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Glycated Hemoglobin
Glycated hemoglobin, also called glycohemoglobin, is a form of hemoglobin (Hb) that is chemically linked to a sugar. Most monosaccharides, including glucose, galactose, and fructose, spontaneously (that is, non-enzymatically) bond with hemoglobin when they are present in the bloodstream. However, glucose is only 21% as likely to do so as galactose and 13% as likely to do so as fructose, which may explain why glucose is used as the primary metabolic fuel in humans. The formation of excess sugar-hemoglobin linkages indicates the presence of excessive sugar in the bloodstream and is an indicator of diabetes or other hormone diseases in high concentration . A1c is of particular interest because it is easy to detect. The process by which sugars attach to hemoglobin is called glycation and the reference system is based on HbA1c, defined as beta-N-1-deoxy fructosyl hemoglobin as component. There are several ways to measure glycated hemoglobin, of which HbA1c (or simply A1c) is a stand ...
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Placebo
A placebo ( ) can be roughly defined as a sham medical treatment. Common placebos include inert tablets (like sugar pills), inert injections (like saline), sham surgery, and other procedures. Placebos are used in randomized clinical trials to test the efficacy of medical treatments. In a placebo-controlled trial, any change in the control group is known as the ''placebo response'', and the difference between this and the result of no treatment is the ''placebo effect''. Placebos in clinical trials should ideally be indistinguishable from so-called verum treatments under investigation, except for the latter's particular hypothesized medicinal effect. This is to shield test participants (with their consent) from knowing who is getting the placebo and who is getting the treatment under test, as patients' and clinicians' expectations of efficacy can influence results. The idea of a placebo effect was discussed in 18th century psychology, but became more prominent in the 20th ...
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Injection (medicine)
An injection (often and usually referred to as a "shot" in US English, a "jab" in UK English, or a "jag" in Scottish English and Scots) is the act of administering a liquid, especially a drug, into a person's body using a needle (usually a hypodermic needle) and a syringe. An injection is considered a form of parenteral drug administration; it does not involve absorption in the digestive tract. This allows the medication to be absorbed more rapidly and avoid the first pass effect. There are many types of injection, which are generally named after the body tissue the injection is administered into. This includes common injections such as subcutaneous, intramuscular, and intravenous injections, as well as less common injections such as epidural, intraperitoneal, intraosseous, intracardiac, intraarticular, and intracavernous injections. Injections are among the most common health care procedures, with at least 16 billion administered in developing and transitional ...
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Dulaglutide
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. The most common side effects are nausea, diarrhea, vomiting, abdominal pain, and decreased appetite. It is a glucagon-like peptide-1 receptor agonist (GLP-1 agonist) consisting of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4. GLP-1 is a hormone that is involved in normalizing the level of glucose in blood (glycemia). The Food and Drug Administration (FDA) approved dulaglutide for use in the United States in September 2014. It was approved for use in the European Union in November 2014. In 2022, it was the 74th most commonly prescribed medication in the United States, with more than 8million ...
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