Dapagliflozin

Dapagliflozin
Dapagliflozin
Systematic (IUPAC) name
(2S,3R,4R,5S,6R)-2-[4-chloro-3-
Clinical data
Pregnancy cat.  ?
Legal status  ?
Routes Oral
Identifiers
CAS number 461432-26-8 N
ATC code None
PubChem CID 9887712
ChemSpider 8063384 YesY
UNII 1ULL0QJ8UC YesY
ChEMBL CHEMBL429910 YesY
Synonyms BMS-512148
Chemical data
Formula C21H25ClO6 
Mol. mass 408.873 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Dapagliflozin (rINN/USAN)[1] is an experimental drug being studied by Bristol-Myers Squibb in partnership with AstraZeneca as a potential treatment for type 1[1] and 2 diabetes. Although dapagliflozin's method of action would operate on either type of diabetes or other conditions resulting in hyperglycemia, the current clinical trials specifically exclude participants with Type 1 diabetes.[2][3]

In July 2011 an FDA committee recommended against approval until more data was available.[4] The Prescription Drug User Fee Act (PDUFA) date for dapagliflozin for the treatment of Type 2 diabetes was extended three months by the FDA to January 28, 2012.[citation needed]

Method of action

Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine.[5]

Selectivity

The IC50 for SGLT2 is less than one thousandth of the IC50 for SGLT1 (1.1 versus 1390 nmol/l), so that the drug does not interfere with the intestinal glucose absorption.[6]

References

  1. ^ a b Statement on a nonproprietory name adopted by the USAN council
  2. ^ Efficacy and Safety of Dapagliflozin, Added to Therapy of Patients With Type 2 Diabetes With Inadequate Glycemic Control on Insulin, ClinicalTrials.gov, April 2009
  3. ^ Trial Details for Trial MB102-020, Bristol-Myers Squibb, May 2009
  4. ^ "FDA panel advises against approval of dapagliflozin". 19 July 2011. http://www.hemonctoday.com/article.aspx?rid=85812. 
  5. ^ Prous Science: Molecule of the Month November 2007
  6. ^ Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009


v · d · eOral anti-diabetic drugs and Insulin analogs (A10)
Insulin
Metformin# • Buformin‡ • Phenformin‡
K+ ATP
Meglitinides/"glinides"
GLP-1 analogs
Exenatide • Liraglutide • Taspoglutide† • Albiglutide† • Lixisenatide
Analogs/other insulins
fast-acting (Insulin lispro • Insulin aspart • Insulin glulisine) • short-acting (Regular insulin) • long-acting (Insulin glargine • Insulin detemir • NPH insulin) • ultra-long-acting (Insulin degludec†) • inhalable Exubera‡
Other
Amylin analog
SGLT2 inhibitors
Canagliflozin† • Dapagliflozin† • Remogliflozin§ • Sergliflozin§
Other

M: END

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