Remogliflozin Etabonate
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Remogliflozin Etabonate
Remogliflozin etabonate (INN/USAN) is a drug of the gliflozin class for the treatment of non-alcoholic steatohepatitis ("NASH") and type 2 diabetes. Remogliflozin was discovered by the Japanese company Kissei Pharmaceutical and is currently being developed by BHV Pharma, a wholly owned subsidiary of North Carolina USA-based Avolynt, and Glenmark Pharmaceuticals through a collaboration with BHV. Remogliflozin was commercially launched first in India by Glenmark in May 2019. Clinical trials Remogliflozin etabonate was shown to enhance urinary glucose excretion in rodents and humans. Early studies in diabetics improved plasma glucose levels. Remogliflozin etabonate has been studied at doses up to 1000 mg. A pair of 12-week phase 2b randomized clinical trials of diabetics published in 2015, found reductions in glycated hemoglobin and that it was generally well tolerated. In a meta-analysis published by Dutta et al. involving data from 3 randomized controlled trials (535 patie ...
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Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as 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 willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ...
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Glycated Hemoglobin
Glycated hemoglobin, also known as HbA1c, glycohemoglobin, hemoglobin A1c, A1C, is a form of hemoglobin (Hb) that is chemically linked to a sugar. Most monosaccharides, including glucose, galactose and fructose, spontaneously (i.e. non-enzymatically) bond with hemoglobin when present in the bloodstream. However, glucose is less likely to do so than galactose and fructose (13% that of fructose and 21% that of galactose), which may explain why glucose is used as the primary metabolic fuel in humans. The formation of the sugar-hemoglobin linkage indicates the presence of excessive sugar in the bloodstream, often indicative of diabetes in high concentration (HbA1c ≥ 5.7%). A1C is of particular interest because it is easy to detect. The process by which sugars attach to hemoglobin is called glycation. HbA1c is a measure of the component of hemoglobin. HbA1c is measured primarily to determine the three-month average blood sugar level and can be used as a diagnostic test for diabet ...
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Pyrazoles
Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. Pyrazole is a weak base, with p''K''b 11.5 (p''K''a of the conjugate acid 2.49 at 25 °C). Pyrazoles are also a class of compounds that have the ring C3N2 with adjacent nitrogen atoms. Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Preparation and reactions Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation: : Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine ( Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole: :CH3C(O)CH2C(O)CH3   +   N2H4   →   (CH3)2C3HN2H   +   2 H2O History The term pyrazole was given to this class of compounds by German ...
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Phenol Ethers
Phenol (also called carbolic acid) is an aromatic organic compound with the molecular formula . It is a white crystalline solid that is volatile. The molecule consists of a phenyl group () bonded to a hydroxy group (). Mildly acidic, it requires careful handling because it can cause chemical burns. Phenol was first extracted from coal tar, but today is produced on a large scale (about 7 billion kg/year) from petroleum-derived feedstocks. It is an important industrial commodity as a precursor to many materials and useful compounds. It is primarily used to synthesize plastics and related materials. Phenol and its chemical derivatives are essential for production of polycarbonates, epoxies, Bakelite, nylon, detergents, herbicides such as phenoxy herbicides, and numerous pharmaceutical drugs. Properties Phenol is an organic compound appreciably soluble in water, with about 84.2 g dissolving in 1000 mL (0.895 M). Homogeneous mixtures of phenol and water at phenol to ...
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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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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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SGLT2
The sodium/glucose cotransporter 2 (SGLT2) is a protein that in humans is encoded by the (solute carrier family 5 (sodium/glucose cotransporter)) gene. Function SGLT2 is a member of the sodium glucose cotransporter family, which are sodium-dependent glucose transport proteins. SGLT2 is the major cotransporter involved in glucose reabsorption in the kidney. SGLT2 is located in the early proximal tubule, and is responsible for reabsorption of 80-90% of the glucose filtered by the kidney glomerulus. Most of the remaining glucose absorption is by sodium/glucose cotransporter 1 (SGLT1) in more distal sections of the proximal tubule. SGLT2 inhibitors for diabetes SGLT2 inhibitors are called gliflozins. They lead to a reduction in blood glucose levels, and therefore have potential use in the treatment of type II diabetes. Gliflozins enhance glycemic control as well as reduce body weight and systolic and diastolic blood pressure. The gliflozins canagliflozin, dapagliflozin, and ...
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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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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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Glenmark Pharmaceuticals
Glenmark Pharmaceuticals Limited is an Indian multinational pharmaceutical company headquartered in Mumbai, India. History it was founded in 1977 by Gracias Saldanha as a generic drug and active pharmaceutical ingredient manufacturer; he named the company after his two sons. The company initially sold its products in India, Russia, and Africa. The company went public in India in 1999, and used some of the proceeds to build its first research facility. Saldanha's son Glenn took over as CEO in 2001, having returned to India after working at PricewaterhouseCoopers. By 2008 Glenmark was the fifth-biggest pharmaceutical company in India. By 2011 the founder of the company was one of the richest men in India, and Glenmark had worldwide sales of $778 million, a 37% increase over the last year's sales; the growth was driven by Glenmark's entry into the US and European generics markets. In the mid-2010s the generics industry in general began transitioning to the end of an era of gia ...
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