- ►diabetesjournals.org S Han, DL Hagan, JR Taylor, L Xin, W Meng, SA Biller, … - Diabetes, 2008 - Am Diabetes Assoc RESULTS—Dapagliflozin potently and selectively inhibited human SGLT2 versus human
SGLT1, the major cotransporter of glucose in the gut, and did not significantly inhibit facilitative
glucose transport in human adipocytes. In vivo, dapagliflozin acutely induced renal ... Cited by 26 - Related articles - All 5 versions
W Meng, BA Ellsworth, AA Nirschl, PJ … - Journal of medicinal …, 2008 - ncbi.nlm.nih.gov The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor
which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic
streptozotocin (STZ) rats. These findings, combined with a favorable ADME profile, have ... Cited by 22 - Related articles - All 4 versions
- ►aspetjournals.org K Katsuno, Y Fujimori, Y Takemura, M Hiratochi, F … - Journal of Pharmacology …, 2007 - ASPET The low-affinity sodium glucose cotransporter (SGLT2), which is expressed specifically in the
kidney, plays a major role in renal glucose reabsorption in the proximal tubule. We have discovered
sergliflozin, a prodrug of a novel selective SGLT2 inhibitor, based on benzylphenol ... Cited by 31 - Related articles - All 5 versions
B Komoroski, N Vachharajani, Y Feng, L Li, D … - Clinical Pharmacology & …, 2009 - nature.com Dapagliflozin, administered to patients in once-daily oral doses, is a sodium–glucose cotransporter
2 (SGLT2) inhibitor that blocks the reabsorption of glucose from urine into the blood. This
14-day study randomized patients with type 2 diabetes mellitus (T2DM) to four treatment ... Cited by 11 - Related articles - All 4 versions
B Komoroski, N Vachharajani, D Boulton, D … - Clinical Pharmacology & …, 2009 - nature.com Dapagliflozin selectively inhibits renal glucose reabsorption by inhibiting sodium–glucose
cotransporter-2 (SGLT2). It was developed as an insulin-independent treatment approach for
type 2 diabetes mellitus (T2DM). The safety, tolerability, pharmacokinetics, and ... Cited by 6 - Related articles - All 4 versions
[CITATION] Dapagliflozin (BMS-512148), a selective inhibitor of the sodium-glucose uptake …
J Calado, J Loeffler, O Sakallioglu, F Gok, K Lhotta, J … - Kidney International, 2006 - nature.com Familial renal glucosuria (FRG) is an inherited renal tubular disorder characterized by persistent
isolated glucosuria in the absence of hyperglycemia. Mutations in the sodium/glucose co-transporter
SGLT2 coding gene, SLC5A2, were recently found to be responsible for the disorder. ... Cited by 19 - Related articles - BL Direct - All 4 versions
- ►diabetesjournals.org JF List, V Woo, E Morales, W Tang, FT Fiedorek - Diabetes Care, 2009 - Am Diabetes Assoc RESEARCH DESIGN AND METHODS Type 2 diabetic patients were randomly assigned to one
of five dapagliflozin doses, metformin XR, or placebo for 12 weeks. The primary objective was
to compare mean change from baseline in A1C. Other objectives included comparison of ... Cited by 13 - Related articles - All 3 versions
MA Abdul-Ghani, RA DeFronzo - Endocrine Practice, 2008 - AACE The prevalence of type 2 diabetes mellitus (T2DM) has increased progressively to epidemic
proportions dur- ing the past 20 years (1). Patients with T2DM have increased morbidity and
mortality, the majority of which results from vascular damage including both macrovascu- ... Cited by 5 - Related articles - All 2 versions
AL Handlon - Expert Opin. Ther. Patents, 2005 - Informa Pharma Science Sodium glucose co-transporter 2 (SGLT2) plays a key role in maintaining glu- cose equilibrium
in the human body. SGLT2 is a kidney transporter that reab- sorbs glucose from the renal filtrate
and prevents the loss of glucose in the urine. Competitive inhibitors of SGLT2 cause the ... Cited by 11 - Related articles - BL Direct - All 4 versions
