Dapagliflozin
| File:Dapagliflozin structure.svg | |
| Systematic (IUPAC) name | |
|---|---|
|
(2S,3R,4R,5S,6R)-2-[4-chloro-3-
(4-ethoxybenzyl)phenyl]-6-(hydroxymethyl) tetrahydro-2H-pyran-3,4,5-triol | |
| Clinical data | |
| Routes of administration | Oral |
| Identifiers | |
| CAS Number | 461432-26-8 |
| ATC code | none |
| PubChem | CID 9887712 |
| ChemSpider | 8063384 |
| Synonyms |
BMS-512148 |
| Chemical data | |
| Formula | C21H25ClO6 |
| Molar mass | 408.873 g/mol[[Script error: No such module "String".]] |
| Script error: No such module "collapsible list". | |
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]
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.[4]
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.[5]
References
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- ↑ 1.0 1.1 Statement on a nonproprietory name adopted by the USAN council
- ↑ Efficacy and Safety of Dapagliflozin, Added to Therapy of Patients With Type 2 Diabetes With Inadequate Glycemic Control on Insulin, ClinicalTrials.gov, April 2009
- ↑ Trial Details for Trial MB102-020, Bristol-Myers Squibb, May 2009
- ↑ Prous Science: Molecule of the Month November 2007
- ↑ Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009
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