Empagliflozin

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Empagliflozin
Empagliflozin.svg
Clinical data
Trade names Jardiance
AHFS/Drugs.com jardiance
License data
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration
by mouth
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
Chemical and physical data
Formula C23H27ClO7
Molar mass 450.91 g·mol−1
3D model (JSmol)

Empagliflozin (trade name Jardiance) is a drug of the gliflozin class, 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 excreted by the kidneys and eliminated in urine.

Medical use[edit]

Empaglifozin in people with type 2 diabetes reduces the risk of death from cardiovascular disease in those with a previous history of cardiovascular disease.[2]

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 urinary tract infections.[3][4]

There are concerns it may increase the risk of diabetic ketoacidosis (DKA). Interestingly, DKA may develop despite only mildly elevated blood glucose levels in people taking SGLT-2 inhibitors, potentially complicating the diagnosis. [5]

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.[6][7][8]

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).[3] The drug was approved in Europe in May 2014 and was approved by the FDA in August 2014.[9] 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.[9]

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. ^ Commissioner, Office of the. "Press Announcements - FDA approves Jardiance to reduce cardiovascular death in adults with type 2 diabetes". www.fda.gov. Retrieved 12 December 2016. 
  3. ^ a b Miriam E. Tucker for Medscape Medical News. May 07, 2013 First Details of Empagliflozin Trials Follow US and EU Filings
  4. ^ NICE. Type 2 diabetes: empagliflozin
  5. ^ FDA (2015-05-15). "SGLT2 inhibitors: Drug Safety Communication - FDA Warns Medicines May Result in a Serious Condition of Too Much Acid in the Blood". Retrieved 19 May 2015. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ 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. 
  9. ^ a b Elizabeth Mechatie for Clinical Endocrinology News Digital Network August 1, 2014 FDA approves empagliflozin for adults with type 2 diabetes