U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C21H25ClO6
Molecular Weight 408.8733
Optical Activity UNSPECIFIED
Defined Stereocenters 5 / 5
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DAPAGLIFLOZIN

SMILES

CCOc1ccc(cc1)Cc2cc(ccc2Cl)[C@@]3([H])[C@@]([H])([C@]([H])([C@@]([H])([C@@]([H])(CO)O3)O)O)O

InChI

InChIKey=JVHXJTBJCFBINQ-ADAARDCZSA-N
InChI=1S/C21H25ClO6/c1-2-27-15-6-3-12(4-7-15)9-14-10-13(5-8-16(14)22)21-20(26)19(25)18(24)17(11-23)28-21/h3-8,10,17-21,23-26H,2,9,11H2,1H3/t17-,18-,19+,20-,21+/m1/s1

HIDE SMILES / InChI
Dapagliflozin (trade name Farxiga in the U.S. and Forxiga in the EU and Russia) is a drug of the gliflozin class, developed by Bristol-Myers Squibb in partnership with AstraZeneca. Farxiga is a sodium-glucose cotransporter 2 (SGLT2) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Originator

Curator's Comment:: # Bristol-Myers Squibb

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
FARXIGA

Approved Use

FARXIGA (dapagliflozin) is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

Launch Date

1.3891392E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
154 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
24.6 ng/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
49 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
118 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
24.8 ng/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
48.4 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
119 ng/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
116 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
208 ng*h/mL
5 mg single, oral
dose: 5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
612 ng*h/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
95.8 ng*h/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
105 ng*h/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
232 ng*h/mL
5 mg single, oral
dose: 5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
658 ng*h/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN 3-O-GLUCURONIDE plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
189 ng*h/mL
5 mg single, oral
dose: 5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
418 ng*h/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
92.3 ng*h/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
101 ng*h/mL
2.5 mg single, oral
dose: 2.5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
199 ng*h/mL
5 mg single, oral
dose: 5 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
427 ng*h/mL
10 mg single, oral
dose: 10 mg
route of administration: oral
experiment type: single
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: unhealthy
age: Children
sex:
food status:
506 ng × h/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
368 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
15.77 h
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
3 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DAPAGLIFLOZIN plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
10 mg single, oral
Highest studied dose
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 14.6 years (range: 11–17)
n = 8
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 14.6 years (range: 11–17)
Sex: M+F
Population Size: 8
Sources:
Other AEs: Abdominal pain upper, Back pain...
Other AEs:
Abdominal pain upper (12.5%)
Back pain (12.5%)
Nausea (12.5%)
Sources:
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 23 years
n = 1
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 23 years
Sex: F
Population Size: 1
Sources:
Disc. AE: Ketoacidosis...
AEs leading to
discontinuation/dose reduction:
Ketoacidosis (1 patient)
Sources:
50 mg single, oral
Highest studied dose
Dose: 50 mg
Route: oral
Route: single
Dose: 50 mg
Sources:
healthy, 24 years (range: 20–45 years years)
n = 8
Health Status: healthy
Age Group: 24 years (range: 20–45 years years)
Sex: M
Population Size: 8
Sources:
20 mg 1 times / day steady, oral
Highest studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, 62 years (range: 20 - 70 years)
n = 12
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 62 years (range: 20 - 70 years)
Sex: M
Population Size: 12
Sources:
Other AEs: Protein urine present...
Other AEs:
Protein urine present (2 patients)
Sources:
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Other AEs: Coronary artery disease, Gastritis...
Other AEs:
Coronary artery disease (serious, 1 patient)
Gastritis (serious, 1 patient)
Lung infection (serious, 1 patient)
Acidosis (serious, 1 patient)
Osteoarthritis (serious, 1 patient)
Colorectal cancer (serious, 1 patient)
Syncope (serious, 1 patient)
Ectopic pregnancy (serious, 1 patient)
Calculus ureteric (serious, 1 patient)
Hydronephrosis (serious, 1 patient)
Hyperlipidaemia (below serious, 31 patient)
Sources:
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: Metabolic Syndrome
Population Size: 12
Sources:
Other AEs: Urinary infection...
Other AEs:
Urinary infection (below serious, 1 patient)
Sources:
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 18
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 18
Sources:
Other AEs: Muscle soreness...
Other AEs:
Muscle soreness (below serious, 8 patients)
Sources:
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 22
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 22
Sources:
Other AEs: Increased urinary frequency, Vaginal itching...
Other AEs:
Increased urinary frequency (below serious, 3 patients)
Vaginal itching (below serious, 2 patients)
Nausea (below serious, 1 patient)
Dry mouth (below serious, 2 patients)
Urinary tract infection (below serious, 1 patient)
Sources:
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 12
Sources:
Other AEs: Urinary tract infection, Low back pain...
Other AEs:
Urinary tract infection (below serious, 2 patients)
Low back pain (below serious, 1 patient)
Sources:
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 15
Health Status: unhealthy
Condition: PreDiabetes
Population Size: 15
Sources:
Other AEs: Vaginal infection, Urinary tract infections...
Other AEs:
Vaginal infection (below serious, 3 patients)
Urinary tract infections (below serious, 2 patients)
Sources:
2.5 mg 1 times / day steady, oral
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy
n = 74
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 74
Sources:
Other AEs: Uterine leiomyoma, Pneumonia...
Other AEs:
Uterine leiomyoma (serious, 1 patient)
Pneumonia (serious, 1 patient)
Pharyngitis (below serious, 4 patients)
Dizziness (below serious, 5 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Abdominal pain upper 12.5%
10 mg single, oral
Highest studied dose
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 14.6 years (range: 11–17)
n = 8
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 14.6 years (range: 11–17)
Sex: M+F
Population Size: 8
Sources:
Back pain 12.5%
10 mg single, oral
Highest studied dose
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 14.6 years (range: 11–17)
n = 8
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 14.6 years (range: 11–17)
Sex: M+F
Population Size: 8
Sources:
Nausea 12.5%
10 mg single, oral
Highest studied dose
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
unhealthy, 14.6 years (range: 11–17)
n = 8
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 14.6 years (range: 11–17)
Sex: M+F
Population Size: 8
Sources:
Ketoacidosis 1 patient
Disc. AE
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 23 years
n = 1
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 23 years
Sex: F
Population Size: 1
Sources:
Protein urine present 2 patients
20 mg 1 times / day steady, oral
Highest studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: steady
Dose: 20 mg, 1 times / day
Sources:
unhealthy, 62 years (range: 20 - 70 years)
n = 12
Health Status: unhealthy
Condition: type 2 diabetes mellitus
Age Group: 62 years (range: 20 - 70 years)
Sex: M
Population Size: 12
Sources:
Hyperlipidaemia below serious, 31 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Acidosis serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Calculus ureteric serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Colorectal cancer serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Coronary artery disease serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Ectopic pregnancy serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Gastritis serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Hydronephrosis serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Lung infection serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Osteoarthritis serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Syncope serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 139
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 139
Sources:
Urinary infection below serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: Metabolic Syndrome
Population Size: 12
Sources:
Muscle soreness below serious, 8 patients
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 18
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 18
Sources:
Nausea below serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 22
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 22
Sources:
Urinary tract infection below serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 22
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 22
Sources:
Dry mouth below serious, 2 patients
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 22
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 22
Sources:
Vaginal itching below serious, 2 patients
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 22
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 22
Sources:
Increased urinary frequency below serious, 3 patients
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 22
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 22
Sources:
Low back pain below serious, 1 patient
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 12
Sources:
Urinary tract infection below serious, 2 patients
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 12
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 12
Sources:
Urinary tract infections below serious, 2 patients
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 15
Health Status: unhealthy
Condition: PreDiabetes
Population Size: 15
Sources:
Vaginal infection below serious, 3 patients
10 mg 1 times / day steady, oral
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 15
Health Status: unhealthy
Condition: PreDiabetes
Population Size: 15
Sources:
Pharyngitis below serious, 4 patients
2.5 mg 1 times / day steady, oral
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy
n = 74
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 74
Sources:
Dizziness below serious, 5 patients
2.5 mg 1 times / day steady, oral
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy
n = 74
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 74
Sources:
Pneumonia serious, 1 patient
2.5 mg 1 times / day steady, oral
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy
n = 74
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 74
Sources:
Uterine leiomyoma serious, 1 patient
2.5 mg 1 times / day steady, oral
Dose: 2.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 2.5 mg, 1 times / day
Sources:
unhealthy
n = 74
Health Status: unhealthy
Condition: Type 2 Diabetes
Population Size: 74
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >45 uM]
no [IC50 >45 uM]
no [IC50 >45 uM]
no [IC50 >45 uM]
no [IC50 >45 uM]
no [IC50 >45 uM]
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted
Page: 63, 67
no [IC50 >45 uM]
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted
Page: 63, 67
no [IC50 >45 uM]
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted
Page: 63, 67
no [IC50 >57.6 uM]
no (co-administration study)
Comment: dapagliflozin does not demonstrate any ability to inhibit P-gp mediated efflux of digoxin
Page: 64, 67
no
no
no
no
no
no
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted
Page: 64, 67
weak [IC50 >45 uM]
yes [IC50 33 uM]
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted
Page: 64, 67
yes [IC50 69 uM]
yes [IC50 8 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
minor
no
no
no
no
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted from clinical pharmacology review p67
Page: 29.0
weak
yes
yes
yes
yes
yes
yes
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted
Page: 63, 65
yes
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted
Page: 63, 65
yes
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted
Page: 63, 65
yes
no (co-administration study)
Comment: no clinically meaningful drug-drug interaction observed in the all the DDI studies conducted from clinical pharmacology review p67
Page: 29.0
yes
unlikely (co-administration study)
Comment: coadministration of mefenamic acid showed slight increase in dapagliflozin exposure; the increase in exposure does not warrant any dose adjustment
Page: 65.0
PubMed

PubMed

TitleDatePubMed
Molecule of the month. Dapagliflozin.
2007 Dec
Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats.
2008 Jun
Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
2008 Mar 13
Inhibition of renal glucose reabsorption: a novel strategy for achieving glucose control in type 2 diabetes mellitus.
2008 Sep
Sodium-glucose cotransport inhibition with dapagliflozin in type 2 diabetes.
2009 Apr
Gateways to clinical trials.
2009 Dec
Dapagliflozin, an oral sodium glucose cotransporter type 2 inhibitor for the treatment of type 2 diabetes mellitus.
2009 Dec
Dapagliflozin for the treatment of type 2 diabetes.
2009 Jul
Renal sodium-glucose transport: role in diabetes mellitus and potential clinical implications.
2009 Jun
Gateways to clinical trials.
2009 Mar
Diabetes treatment.
2009 Mar
Dapagliflozin: an emerging treatment option in type 2 diabetes.
2009 Mar
Dapagliflozin, a novel, selective SGLT2 inhibitor, improved glycemic control over 2 weeks in patients with type 2 diabetes mellitus.
2009 May
Dapagliflozin, a novel SGLT2 inhibitor, induces dose-dependent glucosuria in healthy subjects.
2009 May
(5-Bromo-2-chloro-phen-yl)(4-ethoxy-phen-yl)methanone.
2009 Nov 14
Gateways to clinical trials.
2009 Oct
Dapagliflozin: where does it fit in the treatment of type 2 diabetes?
2009 Oct
A study of dapagliflozin in patients with type 2 diabetes receiving high doses of insulin plus insulin sensitizers: applicability of a novel insulin-independent treatment.
2009 Sep
Dapagliflozin: BMS 512148; BMS-512148.
2010
Synthesis of pyridazine and thiazole analogs as SGLT2 inhibitors.
2010 Aug 15
A novel strategy for the treatment of diabetes mellitus - sodium glucose co-transport inhibitors.
2010 Dec
Quantitative PCR tissue expression profiling of the human SGLT2 gene and related family members.
2010 Dec
Dapagliflozin: a sodium glucose cotransporter 2 inhibitor in development for type 2 diabetes.
2010 Dec
Validated LC-MS/MS methods for the determination of dapagliflozin, a sodium-glucose co-transporter 2 inhibitor in normal and ZDF rat plasma.
2010 Dec
Dapagliflozin: more than just another oral glucose-lowering agent?
2010 Dec
(5-Bromo-2-methyl-phen-yl)(4-eth-oxy-phen-yl)methanone.
2010 Jul 17
Gateways to clinical trials.
2010 Jul-Aug
Dapagliflozin treatment in patients with different stages of type 2 diabetes mellitus: effects on glycaemic control and body weight.
2010 Jun
Neuropathy, retinopathy, and glucose-lowering treatments.
2010 Jun
Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with metformin: a randomised, double-blind, placebo-controlled trial.
2010 Jun 26
Dapagliflozin, an SGLT2 inhibitor, for diabetes.
2010 Jun 26
In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans.
2010 Mar
Sodium-glucose co-transport inhibitors: progress and therapeutic potential in type 2 diabetes mellitus.
2010 Mar 5
The novel sodium glucose transporter 2 inhibitor dapagliflozin sustains pancreatic function and preserves islet morphology in obese, diabetic rats.
2010 Nov
Diabetes: Dapagliflozin: an insulin-independent, therapeutic option for type 2 diabetes mellitus.
2010 Oct
Dapagliflozin monotherapy in type 2 diabetic patients with inadequate glycemic control by diet and exercise: a randomized, double-blind, placebo-controlled, phase 3 trial.
2010 Oct
Gateways to clinical trials.
2010 Sep
Discovery of non-glucoside SGLT2 inhibitors.
2011 Apr 15
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
2011 Apr 28
Discovery of novel N-β-D-xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes.
2011 Jan 13
Patents

Sample Use Guides

The recommended starting dose is 5 mg once daily, taken in the morning, with or without food. Dose can be increased to 10 mg once daily in patients tolerating FARXIGA who require additional glycemic control.
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment:: A non-radioactive cell-based method for the screening of SGLT inhibitors using COS-7 cells transiently expressing human SGLT1 (hSGLT1), CHO-K1 cells stably expressing human SGLT2 (hSGLT2), and a novel fluorescent d-glucose analogue 1-NBDG as a substrate was used.
The IC50 values of dapagliflozin for hSGLT2 and hSGLT1 determined using 1-NBDG were 1.86 nM and 880 nM
Name Type Language
DAPAGLIFLOZIN
DASH   INN   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
DAPAGLIFLOZIN [MI]
Common Name English
QTERNMET XR COMPONENT DAPAGLIFLOZIN
Brand Name English
LYN-045
Code English
DAPAGLIFLOZIN COMPONENT QTERNMET
Brand Name English
QTERNMET COMPONENT DAPAGLIFOZIN
Common Name English
(2S,3R,4R,5S,6R)-2-(4-CHLORO-3-(4-ETHOXYBENZYL)PHENYL)-6-(HYDROXYMETHYL)TETRAHYDRO-2H-PYRAN-3,4,5-TRIOL
Systematic Name English
DAPAGLIFLOZIN [WHO-DD]
Common Name English
DAPAGLIFLOZIN [USAN]
Common Name English
DAPAGLIFLOZIN [ORANGE BOOK]
Common Name English
D-GLUCITOL, 1,5-ANHYDRO-1-C-(4-CHLORO-3-((4-ETHOXYPHENYL)METHYL)PHENYL)-, (1S)-
Systematic Name English
DAPAGLIFLOZIN COMPONENT OF QTERNMET XR
Brand Name English
DAPAGLIFLOZIN [INN]
Common Name English
DAPAGLIFLOZIN [VANDF]
Common Name English
BMS-512148
Code English
Classification Tree Code System Code
WHO-ATC A10BD25
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
NDF-RT N0000187059
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
WHO-ATC A10BK01
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
NCI_THESAURUS C98083
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
WHO-VATC QA10BD15
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
WHO-ATC A10BX09
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
WHO-ATC A10BD15
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
WHO-VATC QA10BX09
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
WHO-ATC A10BD21
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
Code System Code Type Description
EVMPD
SUB31650
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
NDF-RT
N0000187058
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY Sodium-Glucose Transporter 2 Inhibitors [MoA]
DRUG BANK
DB06292
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
RXCUI
1488564
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
4304
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
LACTMED
Dapagliflozin
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
MERCK INDEX
M4086
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY Merck Index
MESH
C529054
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
ChEMBL
CHEMBL429910
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
NCI_THESAURUS
C78126
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
FDA UNII
1ULL0QJ8UC
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
IUPHAR
4594
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
CAS
461432-26-8
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
PUBCHEM
9887712
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY
INN
8886
Created by admin on Sat Jun 26 10:04:27 UTC 2021 , Edited by admin on Sat Jun 26 10:04:27 UTC 2021
PRIMARY