Empagliflozin

Empagliflozin
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

    Empagliflozin is primarily used in type 2 diabetics to lower blood glucose levels. Empaglifozin in people with type 2 diabetes reduces the risk of cardiovascular death and congestive heart failure.[2][3]

    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.[4][5]

    There are concerns it may increase the risk of diabetic ketoacidosis (DKA). DKA may develop despite only mildly elevated blood glucose levels in people taking SGLT-2 inhibitors, potentially complicating the diagnosis.[6]

    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.[7][8][9]

    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).[4] The drug was approved in Europe in May 2014 and was approved by the FDA in August 2014.[10] The FDA required four postmarketing studies: a cardiovascular outcomes trial, two studies in children, and a toxicity study in animals related to the pediatric trials.[10]

    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, Obesity & Metabolism. 14 (1): 83–90. doi:10.1111/j.1463-1326.2011.01517.x. PMID 21985634.
    2. ↑ Usman MS, Siddiqi TJ, Memon MM, Khan MS, Rawasia WF, Talha Ayub M, Sreenivasan J, Golzar Y (January 2018). "Sodium-glucose co-transporter 2 inhibitors and cardiovascular outcomes: A systematic review and meta-analysis". European Journal of Preventive Cardiology: 2047487318755531. doi:10.1177/2047487318755531. PMID 29372664.
    3. ↑ Office of the Commissioner. "FDA approves Jardiance to reduce cardiovascular death in adults with type 2 diabetes". Press Announcement. United States Food and Drug Administration. Retrieved 12 December 2016.
    4. 1 2 Miriam E. Tucker for Medscape Medical News. May 07, 2013 First Details of Empagliflozin Trials Follow US and EU Filings
    5. ↑ "Type 2 diabetes: empagliflozin". UK National Institutes for Care and Excellence (NICE).
    6. ↑ "SGLT2 inhibitors: Drug Safety Communication - FDA Warns Medicines May Result in a Serious Condition of Too Much Acid in the Blood". United States Food and Drug Administration. 2015-05-15. Retrieved 19 May 2015.
    7. ↑ Abdul-Ghani MA, DeFronzo RA (September 2008). "Inhibition of renal glucose reabsorption: a novel strategy for achieving glucose control in type 2 diabetes mellitus". Endocrine Practice. 14 (6): 782–90. doi:10.4158/ep.14.6.782. PMID 18996802.
    8. ↑ Nair S, Wilding JP (January 2010). "Sodium glucose cotransporter 2 inhibitors as a new treatment for diabetes mellitus". The Journal of Clinical Endocrinology and Metabolism. 95 (1): 34–42. doi:10.1210/jc.2009-0473. PMID 19892839.
    9. ↑ Bays H (March 2009). "From victim to ally: the kidney as an emerging target for the treatment of diabetes mellitus". Current Medical Research and Opinion. 25 (3): 671–81. doi:10.1185/03007990802710422. PMID 19232040.
    10. 1 2 Mechatie E (August 1, 2014). "FDA approves empagliflozin for adults with type 2 diabetes". Clinical Endocrinology News Digital Network.


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