Empagliflozin

Empagliflozin
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
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration		 Oral
Legal status
  • ℞ (Prescription only)
Identifiers
CAS Number 864070-44-0
ATC code A10BX12 (WHO)
PubChem CID 11949646
IUPHAR/BPS 4754
ChemSpider 10123957
UNII HDC1R2M35U
ChEBI CHEBI:82720 YesY
Chemical data
Formula C23H27ClO7
Molar mass 450.91 g/mol

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.

Side effects

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.[2][3]

There are concerns it may increase the risk of diabetic ketoacidosis.[4]

Post-Market Studies

In August 2015, release of the post-marketing clinical trial EMPA-REG OUTCOME addressed the addition of empagliflozin to the standard of care for preventing myocardial infarction, stroke, and cardiovascular death.[5]

Mode of action

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

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).[2] 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

References

  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. 1 2 Miriam E. Tucker for Medscape Medical News. May 07, 2013 First Details of Empagliflozin Trials Follow US and EU Filings
  3. ↑ NICE. Type 2 diabetes: empagliflozin
  4. ↑ 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.
  5. ↑ Staton, T. (20 August 2015). "In a first for diabetes, Lilly and Boehringer's Jardiance prevents heart attacks, strokes in trial". FierceMarkets/Questex. Retrieved 20 August 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. 1 2 Elizabeth Mechatie for Clinical Endocrinology News Digital Network August 1, 2014 FDA approves empagliflozin for adults with type 2 diabetes
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