PMID- 19943222
OWN - NLM
STAT- MEDLINE
DCOM- 20100128
LR  - 20210504
IS  - 2040-3410 (Electronic)
IS  - 1369-7056 (Linking)
VI  - 12
IP  - 12
DP  - 2009 Dec
TI  - Dapagliflozin, an oral sodium glucose cotransporter type 2 inhibitor for the 
      treatment of type 2 diabetes mellitus.
PG  - 785-98
AB  - Dapagliflozin (BMS-512148), a specific inhibitor of the sodium-glucose 
      cotransporter SGLT2, is under development by AstraZeneca plc and Bristol-Myers 
      Squibb Co for the potential oral treatment of type 2 diabetes mellitus (T2DM); a 
      fixed-dose combination of dapagliflozin and metformin is also being developed by 
      the companies for the potential treatment of diabetes mellitus. Phlorizin, a 
      naturally occurring O-glucoside, inhibits renal glucose transport and induces 
      glucosuria in rodent models of diabetes; however, phlorizin inhibits other 
      glucose transporters in addition to SGLT2 and thus is not suitable for oral 
      administration. The chemical synthesis of more specific SGLT2 inhibitors led to 
      the identification of dapagliflozin, a C-aryl glucoside that was highly selective 
      for SGLT2 compared with SGLT1. In phase II clinical trials in patients with T2DM, 
      once-daily dapagliflozin induced dose-dependent increases in glucosuria and 
      efficiently reduced HbA1c, fasting and postprandial glucose levels. Dapagliflozin 
      was not associated with significant hypoglycemic episodes or weight gain; rather, 
      the caloric losses related to renal glucose wasting induced a net weight loss. In 
      addition, the diuretic effect observed with dapagliflozin may help to control 
      hypertension, an associated finding in patients with T2DM. The major adverse 
      effect associated with dapagliflozin appears to be an increased occurrence of 
      mycotic genital infections.
FAU - Calado, Joaquim
AU  - Calado J
AD  - New University of Lisbon, Department of Genetics, Faculty of Medical Sciences, 
      Rua da Junqueira no 96, Lisbon, 1349-008, Portugal. jcalado.gene@fcm.unl.pt
LA  - eng
PT  - Journal Article
PT  - Review
PL  - England
TA  - IDrugs
JT  - IDrugs : the investigational drugs journal
JID - 100883655
RN  - 0 (Benzhydryl Compounds)
RN  - 0 (Drug Combinations)
RN  - 0 (Glucosides)
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (Sodium-Glucose Transporter 2 Inhibitors)
RN  - 1ULL0QJ8UC (dapagliflozin)
RN  - 9100L32L2N (Metformin)
SB  - IM
MH  - Administration, Oral
MH  - Animals
MH  - Benzhydryl Compounds
MH  - Clinical Trials as Topic
MH  - Diabetes Mellitus, Type 2/*drug therapy/physiopathology
MH  - Dose-Response Relationship, Drug
MH  - Drug Combinations
MH  - Glucosides/adverse effects/*pharmacology/therapeutic use
MH  - Humans
MH  - Hypoglycemic Agents/adverse effects/*pharmacology/therapeutic use
MH  - Metformin/administration & dosage
MH  - Sodium-Glucose Transporter 2 Inhibitors
RF  - 74
EDAT- 2009/11/28 06:00
MHDA- 2010/01/29 06:00
CRDT- 2009/11/28 06:00
PHST- 2009/11/28 06:00 [entrez]
PHST- 2009/11/28 06:00 [pubmed]
PHST- 2010/01/29 06:00 [medline]
PST - ppublish
SO  - IDrugs. 2009 Dec;12(12):785-98.