Remogliflozin Etabonate
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Remogliflozin etabonate (
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USAN 280px, "Samguk Sagi" Book 04. Silla's Records. In 512, Usan-guk(于山國)was Ulleungdo(鬱陵島) Usan-guk, or the State of Usan, occupied Ulleung-do and the adjacent islands during the Korean Three Kingdoms period. According to th ...
)Statement on a nonproprietory name adopted by the USAN council
/ref> is a drug of the
gliflozin 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 SLC5A1, SGLT1 inhibitors that perform a similar function in ...
class for the treatment of
non-alcoholic steatohepatitis Non-alcoholic fatty liver disease (NAFLD), also known as metabolic (dysfunction) associated fatty liver disease (MAFLD), is excessive fat build-up in the liver without another clear cause such as alcohol use. There are two types; non-alcoholic ...
("NASH") and type 2
diabetes Diabetes, also known as diabetes mellitus, is a group of metabolic disorders characterized by a high blood sugar level ( hyperglycemia) over a prolonged period of time. Symptoms often include frequent urination, increased thirst and increased ap ...
. Remogliflozin was discovered by the Japanese company
Kissei Pharmaceutical Kissei Pharmaceutical is a pharmaceutical company based in Matsumoto, Nagano, Japan. Products discovered or developed by Kissei include: * Difelikefalin * Fostamatinib (trade name Tavalisse) * Linzagolix * Mitiglinide (Glufast) * Remogliflozin e ...
and is currently being developed by BHV Pharma, a wholly owned subsidiary of North Carolina USA-based Avolynt, and
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 na ...
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 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-enzymat ...
and that it was generally well tolerated. In a meta-analysis published by Dutta et al. involving data from 3 randomized controlled trials (535 patients), remogliflozin was noted to have similar glycaemic efficacy (reduction in HbA1c and fasting glucose) as compared to dapagliflozin and pioglitazone.


Method of action

Remogliflozin etabonate is a pro-drug of remogliflozin. Remogliflozin inhibits the
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 ...
(SGLT), which are responsible for glucose
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 ''absorpt ...
in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. Remogliflozin is selective for
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-d ...
.


See also

*
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 no ...


References

{{Sodium-glucose transporter modulators SGLT2 inhibitors Phenol ethers Pyrazoles Glucosides Experimental drugs