Sergliflozin Etabonate
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Sergliflozin Etabonate
Sergliflozin etabonate (INN/USAN, codenamed GW869682X) is an investigational anti-diabetic drug being developed by GlaxoSmithKline. It did not undergo further development after phase II. Method of action Sergliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. Chemistry ''Etabonate Etabonate or ethyl carbonate is the chemical group with formula –, or –. The names are also used for esters R–, for the anion [], and for salt (chemistry), salts of the latter. Pharmaceutical aspects "Etabonate" is an international non ...'' refers to the ethyl carbonate group. The remaining structure, which is the active substance, is called ''sergliflozin''. References SGLT2 inhibitors Glucosides Prodrugs Phenol ethers Abandoned drugs {{gastrointestinal-drug-stub ...
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United States Adopted Name
A United States Adopted Name (USAN) is a unique nonproprietary name assigned to a medication marketed in the United States. Each name is assigned by the USAN Council, which is co-sponsored by the American Medical Association (AMA), the United States Pharmacopeial Convention (USP), and the American Pharmacists Association (APhA). The USAN Program states that its goal is to select simple, informative, and unique nonproprietary names (also called generic names) for drugs by establishing logical nomenclature classifications based on pharmacological or chemical relationships. In addition to drugs, the USAN Council names agents for gene therapy and cell therapy, List of soft contact lens materials, contact lens polymers, surgical materials, diagnostics, carriers, and substances used as an excipient. The USAN Council works in conjunction with the World Health Organization (WHO) international nonproprietary name (INN) Expert Committee and national nomenclature groups to standardize drug ...
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World Health Organization
The World Health Organization (WHO) is a specialized agency of the United Nations responsible for international public health. The WHO Constitution states its main objective as "the attainment by all peoples of the highest possible level of health". Headquartered in Geneva, Switzerland, it has six regional offices and 150 field offices worldwide. The WHO was established on 7 April 1948. The first meeting of the World Health Assembly (WHA), the agency's governing body, took place on 24 July of that year. The WHO incorporated the assets, personnel, and duties of the League of Nations' Health Organization and the , including the International Classification of Diseases (ICD). Its work began in earnest in 1951 after a significant infusion of financial and technical resources. The WHO's mandate seeks and includes: working worldwide to promote health, keeping the world safe, and serve the vulnerable. It advocates that a billion more people should have: universal health care coverag ...
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American Medical Association
The American Medical Association (AMA) is a professional association and lobbying group of physicians and medical students. Founded in 1847, it is headquartered in Chicago, Illinois. Membership was approximately 240,000 in 2016. The AMA's stated mission is "to promote the art and science of medicine and the betterment of public health." The Association also publishes the ''Journal of the American Medical Association'' (JAMA). The AMA also publishes a list of Physician Specialty Codes which are the standard method in the U.S. for identifying physician and practice specialties. The American Medical Association is governed by a House of Delegates as well as a board of trustees in addition to executive management. The organization maintains the AMA Code of Medical Ethics, and the AMA Physician Masterfile containing data on United States Physicians. The ''Current Procedural Terminology'' coding system was first published in 1966 and is maintained by the Association. It has also publi ...
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Anti-diabetic Drug
Drugs used in diabetes treat diabetes mellitus by altering the glucose level in the blood. With the exceptions of insulin, most GLP receptor agonists (liraglutide, exenatide, and others), and pramlintide, all are administered orally and are thus also called oral hypoglycemic agents or oral antihyperglycemic agents. There are different classes of anti-diabetic drugs, and their selection depends on the nature of the diabetes, age and situation of the person, as well as other factors. Diabetes mellitus type 1 is a disease caused by the lack of insulin. Insulin must be used in type 1, which must be injected. Diabetes mellitus type 2 is a disease of insulin resistance by cells. Type 2 diabetes mellitus is the most common type of diabetes. Treatments include agents that (1) increase the amount of insulin secreted by the pancreas, (2) increase the sensitivity of target organs to insulin, (3) decrease the rate at which glucose is absorbed from the gastrointestinal tract, and (4) inc ...
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GlaxoSmithKline
GSK plc, formerly GlaxoSmithKline plc, is a British multinational pharmaceutical and biotechnology company with global headquarters in London, England. Established in 2000 by a merger of Glaxo Wellcome and SmithKline Beecham. GSK is the tenth largest pharmaceutical company and #294 on the 2022 ''Fortune'' Global 500, ranked behind other pharmaceutical companies China Resources, Sinopharm, Johnson & Johnson, Pfizer, Roche, AbbVie, Novartis, Bayer, and Merck. The company has a primary listing on the London Stock Exchange and is a constituent of the FTSE 100 Index. , it had a market capitalisation of £70 billion, the eighth largest on the London Stock Exchange. It has a secondary listing on the New York Stock Exchange. The company developed the first malaria vaccine, RTS,S, which it said in 2014 it would make available for five percent above cost. Legacy products developed at GSK include several listed in the World Health Organization's List of Essential Medicines, such ...
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Sodium-glucose Transport Proteins
Sodium-dependent glucose cotransporters (or sodium-glucose linked transporter, SGLT) are a family of glucose transporter found in the intestinal mucosa (enterocytes) of the small intestine (SGLT1) and the proximal tubule of the nephron (SGLT2 in PCT and SGLT1 in PST). They contribute to renal glucose reabsorption. In the kidneys, 100% of the filtered glucose in the glomerulus has to be reabsorbed along the nephron (98% in PCT, via SGLT2). If the plasma glucose concentration is too high (hyperglycemia), glucose passes into the urine (glucosuria) because SGLT are saturated with the filtered glucose. Types The two most well known members of SGLT family are SGLT1 and SGLT2, which are members of the SLC5A gene family. In addition to SGLT1 and SGLT2, there are 10 other members in the human protein family SLC5A. Of these, SLC5A4/SGLT3 (SAAT1) is a low-affinity transporter for glucose, but seems to have more of an electric function. The other SLC5 proteins transport mannose, my ...
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Reabsorption
In renal physiology, reabsorption or tubular reabsorption is the process by which the nephron removes water and solutes from the tubular fluid (pre-urine) and returns them to the circulating blood. It is called ''reabsorption'' (and not ''absorption'') because these substances have already been absorbed once (particularly in the intestines) and the body is reclaiming them from a postglomerular fluid stream that is on its way to becoming urine (that is, they will soon be lost to the urine unless they are reabsorbed from the tubule into the peritubular capillaries. This happens as a result of sodium transport from the lumen into the blood by the Na+/K+ATPase in the basolateral membrane of the epithelial cells. Thus, the glomerular filtrate becomes more concentrated, which is one of the steps in forming urine. Nephrons are divided into five segments, with different segments responsible for reabsorbing different substances. Reabsorption allows many useful solutes (primarily gluc ...
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Etabonate
Etabonate or ethyl carbonate is the chemical group with formula –, or –. The names are also used for esters R–, for the anion [], and for salt (chemistry), salts of the latter. Pharmaceutical aspects "Etabonate" is an international nonproprietary name (INN) and United States Adopted Name (USAN) for pharmaceutical substances and is the name almost universally used in pharmacology. some important drugs featuring that group are * Loteprednol etabonate, a corticosteroid * Remogliflozin etabonate, an anti-diabetic drug * Sergliflozin etabonate, another anti-diabetic drug Chemical aspects "Ethyl carbonate"is the name commonly used in chemistry. Important non-medical esters with that group are * Diethyl carbonate, * methyl ethyl carbonate, Alkali salts of that anion, such as sodium ethyl carbonate, are known and fairly stable at ambient conditions. They have been proposed as an economical and environmentally friendly intermediate for the synthesis of organic compound ...
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Sergliflozin Skeletal
Sergliflozin etabonate (INN/USAN, codenamed GW869682X) is an investigational anti-diabetic drug being developed by GlaxoSmithKline. It did not undergo further development after phase II. Method of action Sergliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. Chemistry ''Etabonate Etabonate or ethyl carbonate is the chemical group with formula –, or –. The names are also used for esters R–, for the anion [], and for salt (chemistry), salts of the latter. Pharmaceutical aspects "Etabonate" is an international non ...'' refers to the ethyl carbonate group. The remaining structure, which is the active substance, is called ''sergliflozin''. References SGLT2 inhibitors Glucosides Prodrugs Phenol ethers Abandoned drugs {{gastrointestinal-drug-stub ...
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SGLT2 Inhibitors
SGLT2 inhibitors, also called gliflozins or flozins, are a class of medications that modulate sodium-glucose transport proteins in the nephron (the functional units of the kidney), unlike SGLT1 inhibitors that perform a similar function in the intestinal mucosa. The foremost metabolic effect of this is to inhibit reabsorption of glucose in the kidney and therefore lower blood sugar. They act by inhibiting sodium-glucose transport protein 2 (SGLT2). SGLT2 inhibitors are used in the treatment of type II diabetes mellitus (T2DM). Apart from blood sugar control, gliflozins have been shown to provide significant cardiovascular benefit in patients with type II diabetes (T2DM). Several medications of this class have been approved or are currently under development. In studies on canagliflozin, a member of this class, the medication was found to enhance blood sugar control as well as reduce body weight and systolic and diastolic blood pressure. Medical uses The 2022 ADA standards of medi ...
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Glucosides
A glucoside is a glycoside that is derived from glucose. Glucosides are common in plants, but rare in animals. Glucose is produced when a glucoside is hydrolysed by purely chemical means, or decomposed by fermentation or enzymes. The name was originally given to plant products of this nature, in which the other part of the molecule was, in the greater number of cases, an aromatic aldehydic or phenolic compound (exceptions are Jinigrin and Jalapin or Scammonin). It has now been extended to include synthetic ethers, such as those obtained by acting on alcoholic glucose solutions with hydrochloric acid, and also the polysaccharoses, e.g. cane sugar, which appear to be ethers also. Although glucose is the most common sugar present in glucosides, many are known which yield rhamnose or iso-dulcite; these may be termed pentosides. Much attention has been given to the non-sugar parts (aglyca) of the molecules; the constitutions of many have been determined, and the compounds synthes ...
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