Empagliflozin

Empagliflozin
Clinical data
Trade names Jardiance
AHFS/Drugs.com jardiance
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration		 Oral
ATC code A10BX12 (WHO)
Legal status
Legal status
  • ℞ (Prescription only)
Identifiers
CAS Number 864070-44-0
PubChem (CID) 11949646
IUPHAR/BPS 4754
ChemSpider 10123957
UNII HDC1R2M35U
ChEBI CHEBI:82720 YesY
Chemical and physical data
Formula C23H27ClO7
Molar mass 450.91 g/mol
3D model (Jmol) Interactive image

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[5] addressed the addition of empagliflozin to the standard of care for preventing myocardial infarction, stroke, and cardiovascular death.[6] Empaglifozin was the first and, to date, only oral type-2 diabetes medicine shown to reduce the risk of cardiovascular death in a clinical trial.[7]

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.[8][9][10]

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.[11] 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.[11]

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. ↑ Zinman, Bernard; Wanner, Christoph; Lachin, John M.; Fitchett, David; Bluhmki, Erich; Hantel, Stefan; Mattheus, Michaela; Devins, Theresa; Johansen, Odd Erik (2015-11-25). "Empagliflozin, Cardiovascular Outcomes, and Mortality in Type 2 Diabetes". New England Journal of Medicine. 373 (22): 2117–2128. doi:10.1056/nejmoa1504720.
  6. ↑ 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.
  7. ↑ "FDA Advisory Committee recommends approval of Jardiance® (empagliflozin) for cardiovascular indication in 12-11 vote". Yahoo! Finance. 28 June 2016. Retrieved 10 August 2016.
  8. ↑ 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.
  9. ↑ 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.
  10. ↑ 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.
  11. 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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