Empagliflozin

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Empagliflozin
Empagliflozin.svg
Systematic (IUPAC) name
(2S,3R,4R,5S,6R)-2-[4-chloro-3-[[4-[(3S)-oxolan-3-yl]oxyphenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
Clinical data
Trade names Jardiance
AHFS/Drugs.com entry
  • US: C (Risk not ruled out)
Identifiers
864070-44-0
A10BX12
PubChem CID 11949646
ChemSpider 10123957
UNII HDC1R2M35U
ChEBI CHEBI:82720 YesY
Chemical data
Formula C23H27ClO7
450.91 g/mol

Empagliflozin (trade name Jardiance) is drug approved for the treatment of type 2 diabetes in adults in 2014. It was developed by Boehringer Ingelheim and Eli Lilly and Company.[1]

Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), and causes sugar in the blood to be absorbed by the kidneys and eliminated in urine.

Mode of action[edit]

Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), which is found almost exclusively in the proximal tubules of nephronic components in the kidneys. SGLT-2 accounts for about 90 percent of glucose reabsorption into the blood. Blocking SGLT-2 reduces blood glucose by blocking glucose reabsorption in the kidney and thereby excreting glucose (i.e., blood sugar) via the urine.[2][3][4]

Side effects[edit]

When taken in dosages of 10 or 25 mg once a day, the incidence of adverse events was similar to placebo. However, there was a higher frequency of genital infections at both the 10 mg and the 25 mg dosages.[5][6]

Regulatory status[edit]

As of May 2013, Boehringer and Lilly had submitted applications for marketing approval to the European Medicines Agency and the U.S. Food and Drug Administration (FDA).[5] The drug was approved in Europe in May 2014 and was approved by the FDA in August 2014[7] The FDA required four postmarketing studies: a cardiovascular outcomes trial, and two studies in children, and a toxicity study in animals related to the pediatric trials.[7]

See also[edit]

References[edit]

  1. ^ Grempler R, Thomas L, Eckhardt M, Himmelsbach F, Sauer A, Sharp DE, Bakker RA, Mark M, Klein T, Eickelmann P (January 2012). "Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors". Diabetes Obes Metab 14 (1): 83–90. doi:10.1111/j.1463-1326.2011.01517.x. PMID 21985634. 
  2. ^ Abdul-Ghani MA, DeFronzo RA (September 2008). "Inhibition of renal glucose reabsorption: a novel strategy for achieving glucose control in type 2 diabetes mellitus". Endocr Pract 14 (6): 782–90. doi:10.4158/ep.14.6.782. PMID 18996802. 
  3. ^ Nair S, Wilding JP (January 2010). "Sodium glucose cotransporter 2 inhibitors as a new treatment for diabetes mellitus". J. Clin. Endocrinol. Metab. 95 (1): 34–42. doi:10.1210/jc.2009-0473. PMID 19892839. 
  4. ^ Bays H (March 2009). "From victim to ally: the kidney as an emerging target for the treatment of diabetes mellitus". Curr Med Res Opin 25 (3): 671–81. doi:10.1185/03007990802710422. PMID 19232040. 
  5. ^ a b Miriam E. Tucker for Medscape Medical News. May 07, 2013 First Details of Empagliflozin Trials Follow US and EU Filings
  6. ^ NICE. Type 2 diabetes: empagliflozin
  7. ^ a b Elizabeth Mechatie for Clinical Endocrinology News Digital Network August 1, 2014 FDA approves empagliflozin for adults with type 2 diabetes