PMID- 21733056
OWN - NLM
STAT- MEDLINE
DCOM- 20120224
LR  - 20221207
IS  - 1463-1326 (Electronic)
IS  - 1462-8902 (Linking)
VI  - 14
IP  - 1
DP  - 2012 Jan
TI  - Remogliflozin etabonate, a selective inhibitor of the sodium-dependent 
      transporter 2 reduces serum glucose in type 2 diabetes mellitus patients.
PG  - 15-22
LID - 10.1111/j.1463-1326.2011.01462.x [doi]
AB  - AIMS: Remogliflozin etabonate (RE) is the pro-drug of remogliflozin (R), a 
      selective inhibitor of renal sodium-dependent glucose transporter 2 (SGLT2) that 
      improves glucose control via enhanced urinary glucose excretion (UGE). This study 
      evaluated the safety, tolerability, pharmacokinetics and pharmacodynamics of 
      repeated doses of RE in subjects with type 2 diabetes mellitus (T2DM). METHODS: 
      In a double-blinded, randomized, placebo-controlled trial, subjects who were 
      drug-naive or had metformin discontinued received RE [100 mg BID (n = 9), 1000 mg 
      QD (n = 9), 1000 mg BID (n = 9)], or placebo (n = 8) for 12 days. Safety 
      parameters were assessed, including urine studies to evaluate renal function. 
      Plasma concentrations of RE and metabolites were measured with the first dose and 
      at steady state. RE effects on glucose levels were assessed with fasting glucose 
      concentrations, frequently sampled 24-h glucose profiles and oral glucose 
      tolerance tests. RESULTS: No significant laboratory abnormalities or safety 
      events were reported; the most frequent adverse events were headache and 
      flatulence. Plasma exposure to RE and R were proportional to administered dose 
      with negligible accumulation. Mean 24-h UGE increased in RE treatment groups. 
      Compared with the placebo group, 24-h mean (95% CI) changes in plasma glucose 
      were -1.2 (-2.2 to -0.3) (100 mg BID), -0.8 (-1.7 to 0.2) (1000 mg QD) and -1.7 
      (-2.7 to -0.8) mmol/l (1000 mg BID). CONCLUSIONS: Administration of RE for 12 
      days is well-tolerated and results in clinically meaningful improvements in 
      plasma glucose, accompanied by changes in body weight and blood pressure in 
      subjects with T2DM.
CI  - (c) 2011 Blackwell Publishing Ltd.
FAU - Dobbins, R L
AU  - Dobbins RL
AD  - GlaxoSmithKline, Research Triangle Park, NC 27709-3398, USA. 
      robert.l.dobbins@gsk.com
FAU - O'Connor-Semmes, R
AU  - O'Connor-Semmes R
FAU - Kapur, A
AU  - Kapur A
FAU - Kapitza, C
AU  - Kapitza C
FAU - Golor, G
AU  - Golor G
FAU - Mikoshiba, I
AU  - Mikoshiba I
FAU - Tao, W
AU  - Tao W
FAU - Hussey, E K
AU  - Hussey EK
LA  - eng
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
DEP - 20111030
PL  - England
TA  - Diabetes Obes Metab
JT  - Diabetes, obesity & metabolism
JID - 100883645
RN  - 0 (Blood Glucose)
RN  - 0 (Glucosides)
RN  - 0 (Glycated Hemoglobin A)
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (Pyrazoles)
RN  - 0 (Sodium-Glucose Transporter 2)
RN  - 0 (Sodium-Glucose Transporter 2 Inhibitors)
RN  - TR0QT6QSUL (remogliflozin etabonate)
SB  - IM
MH  - Adult
MH  - Aged
MH  - Blood Glucose/*drug effects
MH  - Blood Pressure/drug effects
MH  - Body Mass Index
MH  - Body Weight/drug effects
MH  - Diabetes Mellitus, Type 2/blood/*drug therapy
MH  - Double-Blind Method
MH  - Female
MH  - Glucose Tolerance Test
MH  - Glucosides/pharmacokinetics/pharmacology/*therapeutic use
MH  - Glycated Hemoglobin/*drug effects
MH  - Humans
MH  - Hypoglycemic Agents/pharmacokinetics/pharmacology/*therapeutic use
MH  - Male
MH  - Middle Aged
MH  - Pyrazoles/pharmacokinetics/pharmacology/*therapeutic use
MH  - Sodium-Glucose Transporter 2/blood
MH  - *Sodium-Glucose Transporter 2 Inhibitors
MH  - Treatment Outcome
EDAT- 2011/07/08 06:00
MHDA- 2012/03/01 06:00
CRDT- 2011/07/08 06:00
PHST- 2011/07/08 06:00 [entrez]
PHST- 2011/07/08 06:00 [pubmed]
PHST- 2012/03/01 06:00 [medline]
AID - 10.1111/j.1463-1326.2011.01462.x [doi]
PST - ppublish
SO  - Diabetes Obes Metab. 2012 Jan;14(1):15-22. doi: 10.1111/j.1463-1326.2011.01462.x. 
      Epub 2011 Oct 30.