Dapagliflozin

Summary

Dapagliflozin (CHEMBL429910) is an approved small-molecule hypoglycemic agent (ATC A10BK01) targeting KCNK7, SLC5A1, and SLC5A2; indicated across 45 conditions including diabetes mellitus and heart failure.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A10BK01
• Targets: 3 (KCNK7, SLC5A1, SLC5A2)
• Indications: 45 conditions
• Clinical trials: 412
• Chemistry: 408.9 Da · C21H25ClO6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL429910
Name	Dapagliflozin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9887712
ChEBI	CHEBI:85078
ATC	A10BK01
Molecular formula	C21H25ClO6
Molecular weight	408.9
InChIKey	JVHXJTBJCFBINQ-ADAARDCZSA-N

SMILES: CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)Cl

IUPAC name: (2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol

ChEBI definition: A C-glycosyl comprising β-D-glucose in which the anomeric hydroxy group is replaced by a 4-chloro-3-(4-ethoxybenzyl)phenyl group. Used (in the form of its propanediol monohydrate) to improve glycemic control, along with diet and exercise, in adults with type 2 diabetes.

Pharmacological roles (ChEBI): hypoglycemic agent, sodium-glucose transport protein subtype 2 inhibitor.

Also known as: BMS-512148, Dapagliflozin, Dapagliflozin component of br1019, Dapagliflozin component of qtern, Dapagliflozin component of qternmet, Dapagliflozin component of qternmet xr, Dapagliflozin viatris, Dapagliflozina, Dapagliflozine, LYN-045, dapagliflozin, DAPAGLIFLOZIN

Parent form; salt/anhydrous children: CHEMBL2103802, CHEMBL3125316, CHEMBL3125317, CHEMBL3125318, CHEMBL3125455, CHEMBL3125456, CHEMBL3125457, CHEMBL3125458

Patent coverage: 2,347 distinct patent families (5,323 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 5,092 (96%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
KCNK7	K2P7.1	Activation	4	1.9%	Q9Y2U2
SLC5A1	Sodium/glucose cotransporter 1	Inhibition	6.4	0%	P13866
SLC5A2	Sodium/glucose cotransporter 2	Inhibition	9.3	0.2%	P31639

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Sodium/myo-inositol cotransporter 2, Alpha-2A adrenergic receptor, Sodium/glucose cotransporter 2, Sodium/glucose cotransporter 2, Sodium/glucose cotransporter 1.

Bioactivity

ChEMBL activities: 71 potent at pChembl ≥ 5 of 72 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_24836682
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_3128774
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_3309053
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_3403336
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_3600494
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_5124488
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_5221964
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_6229998
SLC5A2	9.31	IC50	0.49	nM	CHEMBL_ACT_6355978
SLC5A2	9.1	IC50	0.8	nM	CHEMBL_ACT_18011147
SLC5A2	9	IC50	1	nM	CHEMBL_ACT_14715531
SLC5A2	8.98	IC50	1.05	nM	CHEMBL_ACT_18293101
SLC5A2	8.96	IC50	1.1	nM	CHEMBL_ACT_18665720
SLC5A2	8.96	EC50	1.1	nM	CHEMBL_ACT_19005387
SLC5A2	8.96	EC50	1.1	nM	CHEMBL_ACT_2109157
SLC5A2	8.96	EC50	1.1	nM	CHEMBL_ACT_2274629
SLC5A2	8.96	IC50	1.1	nM	CHEMBL_ACT_29054643
SLC5A2	8.95	IC50	1.12	nM	CHEMBL_ACT_19001163
SLC5A2	8.94	IC50	1.16	nM	CHEMBL_ACT_13941708
SLC5A2	8.92	IC50	1.2	nM	CHEMBL_ACT_25634246
SLC5A2	8.89	IC50	1.3	nM	CHEMBL_ACT_10949233
SLC5A2	8.89	IC50	1.3	nM	CHEMBL_ACT_12109347
SLC5A2	8.87	IC50	1.35	nM	CHEMBL_ACT_6211675
SLC5A2	8.87	IC50	1.35	nM	CHEMBL_ACT_6335483
SLC5A2	8.85	IC50	1.4	nM	CHEMBL_ACT_18665714
SLC5A2	8.85	IC50	1.4	nM	CHEMBL_ACT_3190450
SLC5A2	8.82	IC50	1.5	nM	CHEMBL_ACT_18072025
SLC5A2	8.7	EC50	2	nM	CHEMBL_ACT_18369226
SLC5A2	8.62	EC50	2.4	nM	CHEMBL_ACT_10981994
SLC5A2	8.62	IC50	2.4	nM	CHEMBL_ACT_25050100

Target pathways

Aggregated over 3 target gene(s): KCNK7, SLC5A1, SLC5A2.

Top Reactome pathways

18 total, by targets touching each:

Pathway	Targets	Genes
Disease	2	SLC5A1, SLC5A2
Cellular hexose transport	2	SLC5A1, SLC5A2
Transport of small molecules	2	SLC5A1, SLC5A2
SLC-mediated transmembrane transport	2	SLC5A1, SLC5A2
SLC transporter disorders	2	SLC5A1, SLC5A2
Disorders of transmembrane transporters	2	SLC5A1, SLC5A2
Neuronal System	1	KCNK7
Potassium Channels	1	KCNK7
Tandem pore domain potassium channels	1	KCNK7
Tandem of pore domain in a weak inwardly rectifying K+ channels (TWIK)	1	KCNK7
Muscle contraction	1	KCNK7
Phase 4 - resting membrane potential	1	KCNK7
Cardiac conduction	1	KCNK7
Defective SLC5A1 causes congenital glucose/galactose malabsorption (GGM)	1	SLC5A1
Defective SLC5A2 causes renal glucosuria (GLYS1)	1	SLC5A2
Intestinal absorption	1	SLC5A1
Digestion and absorption	1	SLC5A1
Intestinal hexose absorption	1	SLC5A1

Dominant GO biological processes

GO term	Targets
monoatomic ion transport	3
alpha-glucoside transport	2
sodium ion transport	2
renal D-glucose absorption	2
D-glucose import across plasma membrane	2
sodium ion import across plasma membrane	2
D-glucose transmembrane transport	2
transmembrane transport	2
potassium ion transport	1
potassium ion transmembrane transport	1
monoatomic ion transmembrane transport	1
intestinal D-glucose absorption	1
pentose transmembrane transport	1
fucose transmembrane transport	1
galactose transmembrane transport	1

Indications & clinical

Indications

45 indications (4 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
diabetes mellitus	4	MONDO:0005015	EFO:0000400
heart failure	4	MONDO:0005252	EFO:0003144
chronic kidney disease	4	MONDO:0005300	EFO:0003884
type 2 diabetes mellitus	4	MONDO:0005148	MONDO:0005148
metabolic dysfunction-associated steatohepatitis	3	MONDO:0007027	EFO:1001249
polycystic ovary syndrome	3	MONDO:0008487	EFO:0000660
atrial fibrillation	3	MONDO:0004981	EFO:0000275
coronary artery disorder	3	MONDO:0005010	EFO:0001645
acute kidney injury	3	MONDO:0002492	HP:0001919
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
diabetic retinopathy	3	MONDO:0005266	EFO:0003770
kidney failure	3	MONDO:0001106	EFO:1002048
fatty liver disease	3	MONDO:0004790	HP:0001397
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
IgA glomerulonephritis	3	MONDO:0005342	EFO:0004194
ST-elevation myocardial infarction	3	MONDO:0041656	EFO:0008585
obesity disorder	2	MONDO:0011122	EFO:0001073
metabolic syndrome X	2	MONDO:0011565	EFO:0000195
diabetic kidney disease	2	MONDO:0005016	EFO:0000401
diastolic heart failure	2	MONDO:0006727	EFO:1000899
breast neoplasm	2	MONDO:0021100	MONDO:0007254
myocardial infarction	2	MONDO:0005068	EFO:0000612
pulmonary arterial hypertension	2	MONDO:0015924	EFO:0001361
diabetic neuropathy	2	MONDO:0006626	EFO:1000783
cystinuria	2	MONDO:0009067	MONDO:0009067
cirrhosis of liver	2	MONDO:0005155	EFO:0001422
depressive disorder	2	MONDO:0002050	MONDO:0002050
Fabry disease	2	MONDO:0010526	MONDO:0010526
inflammatory bowel disease	2	MONDO:0005265	EFO:0003767
hereditary amyloidosis	2	MONDO:0018634	MONDO:0019438
exocrine pancreatic carcinoma	1	MONDO:0005192	EFO:0002618
prostate carcinoma	1	MONDO:0005159	EFO:0001663
ischemia reperfusion injury	1	MONDO:0005203	EFO:0002687
Alzheimer disease	1	MONDO:0004975	MONDO:0004975
brain neoplasm	1	MONDO:0021211	EFO:0003833
myocardial ischemia	1	MONDO:0024644	EFO:1001375
lupus nephritis	1	MONDO:0005556	EFO:0005761

8 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 412.

Phase distribution

Phase	Trials
PHASE4	133
PHASE3	104
PHASE2	60
PHASE1	58
Not specified	34
PHASE2/PHASE3	15
PHASE1/PHASE2	4
EARLY_PHASE1	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04707261	PHASE4	RECRUITING	Association Between Dapagliflozin-induced Improvement and Anemia in Heart Failure Patients (ADIDAS)
NCT05782972	PHASE4	ACTIVE_NOT_RECRUITING	Therapeutic Response of Sodium-glucose Co-transporter Type-2 Inhibitor in Non-diabetic MAFLD Patients: a Pilot Study
NCT06054035	PHASE4	RECRUITING	SGLT2 Inhibition in Addition to Lifestyle Intervention and Risk for Complications in Subtypes of Patients With Prediabetes
NCT06442280	PHASE4	NOT_YET_RECRUITING	SGLT-2 Inhibitor and High-Dose Furosemide Plus Small-Volume Hypertonic Saline Solution in Acute HF
NCT06532682	PHASE4	ACTIVE_NOT_RECRUITING	Efficacy of Dapagliflozin in Early Diabetic Nephropathy in Type 1 Diabetes
NCT06562582	PHASE4	RECRUITING	STunning in Acute Myocardial Infarction - BAS
NCT06578520	PHASE4	RECRUITING	Effect of the Use of Dapagliflozin in Patients With Refractory Heart Failure
NCT06610526	PHASE4	ACTIVE_NOT_RECRUITING	A Study of Dapagliflozin in Chinese Adult Patients With Chronic Kidney Disease
NCT06642272	PHASE4	RECRUITING	A Pragmatic Trial Comparing Empagliflozin and Dapagliflozin Through Cluster Randomization Embedded in the Electronic Health Record
NCT06851962	PHASE4	ACTIVE_NOT_RECRUITING	Impact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes.
NCT06922656	PHASE4	NOT_YET_RECRUITING	Can the Addition of Pioglitazone to SGLT2 Inhibitor in Type 1 Diabetic Patients Amplify the Decrease in HbA1c and Prevent the Increase in Plasma Ketone Concentration?
NCT06954090	PHASE4	ENROLLING_BY_INVITATION	Urinary Proteomics to Guide Early Intervention to Prevent Complications in Type 2 Diabetes - a Feasibility Study
NCT06972732	PHASE4	RECRUITING	A Phase IV Clinical Trial to Compare the Efficacy and Safety of Metformin+Sodium-Glucose Cotransporter 2 Inhibitor(SGLT2-i)+Thiazolidinedione (TZD) in Patients With Type 2 Diabetes
NCT07076615	PHASE4	RECRUITING	The Effect of Dapagliflozin on Patients With Cardiomyopathy
NCT07239570	PHASE4	RECRUITING	A Biomarker-targeted Clinical Trial to Optimize Treatment for Patients With Chronic Kidney Disease
NCT07254572	PHASE4	RECRUITING	Anti-atherosclerotic Efficacy of Selected Antidiabetic Drugs in Patients With Coronary Artery Disease and Pre-diabetes
NCT07342764	PHASE4	NOT_YET_RECRUITING	Comparative Effectiveness of Dapagliflozin, Metformin, and Lifestyle Modification for Antipsychotic-Induced Weight Gain: An Open-Label Pragmatic Trial
NCT07351643	PHASE4	NOT_YET_RECRUITING	CCTA Evaluation of SGLT2i-related Pericoronary Fat Changes in Non-diabetic ACS Patients Without HF
NCT07351864	PHASE4	NOT_YET_RECRUITING	Finerenone Plus SGLT2 Inhibitors in Heart Failure
NCT07614230	PHASE4	RECRUITING	SGLT2 Inhibitors on Coronary Atherosclerosis Progression Via Perivascular Adipose Tissue in Diabetes
NCT02157298	PHASE4	COMPLETED	Phase IV Study With a 36-week Extension Period to Evaluate the Efficacy and Safety of Dapagliflozin Therapy When Added to the Therapy of Japanese Patients With Type 2 Diabetes With Inadequate Glycemic Control on Insulin.
NCT02211742	PHASE4	COMPLETED	Dapagliflozin in Type 1 Diabetes
NCT02235298	PHASE4	COMPLETED	Dapagliflozin Effects on Epicardial Fat
NCT02253121	PHASE4	COMPLETED	Glucose Control During Glucocorticoid Therapy in Acute Exacerbation of Chronic Obstructive Pulmonary Disease
NCT02327039	PHASE4	COMPLETED	The Effects of Dapagliflozin on HDL Particles Subtypes and Reverse Cholesterol Transport in Type 2 Diabetic Patients
NCT02338921	PHASE4	COMPLETED	Triple Combination Therapy in Type 2 Diabetic Patients Who Had Inadequate Glycemic Control With Combination Therapy
NCT02372955	PHASE4	UNKNOWN	Mechanistic Study of the Systolic Blood Pressure Lowering Effect of Dapagliflozin in Type 2 Diabetes
NCT02397421	PHASE4	COMPLETED	Safety and Effectiveness of SGLT-2 Inhibitors in Patients With Heart Failure and Diabetes
NCT02426541	PHASE4	COMPLETED	Effects of Dapagliflozin 10 mg on Insulin Resistance in Patients With Type 2 Diabetes Mellitus
NCT02433678	PHASE4	COMPLETED	An Investigation Into The Anti-hypertensive And Potential Anti-inflammatory Actions Of Dapagliflozin
NCT02459353	PHASE4	COMPLETED	Effect of Dapagliflozin on Glycemic Variability
NCT02471404	PHASE4	COMPLETED	Efficacy and Safety of Dapagliflozin and Dapagliflozin Plus Saxagliptin in Combination With Metformin in Type 2 Diabetes Patients Compared With Sulphonylurea
NCT02475070	PHASE4	COMPLETED	Vildagliptin Versus Dapagliflozin on Glucagon
NCT02501616	PHASE4	UNKNOWN	Effect of Dapagliflozine on Systemic and Renal Endothelial Function
NCT02564926	PHASE4	COMPLETED	Foxiga Korea Local Phase 4 Study
NCT02577159	PHASE4	UNKNOWN	Dapagliflozin on Hyperlipidemia and Insulin Resistance in Type 2 Diabetic Patients (DAPHNIS Study)
NCT02585804	PHASE4	COMPLETED	Treating to Reduce Albuminuria and Normalize Hemodynamic Function in Focal ScLerosis With dApagliflozin Trial Effects
NCT02608905	PHASE4	TERMINATED	Effect of Dapagliflozin on Inflammation and Endothelial Function
NCT02610088	PHASE4	COMPLETED	Effect of Dapagliflozin on Vascular Functions in Patients With Type 2 Diabetes Compared to Gliclazide
NCT02616666	PHASE4	COMPLETED	A Pragmatic Randomized Trial to Evaluate the Comparative Effectiveness Between Dapagliflozin and Standard of Care in Type 2 Diabetes Patients

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

16 molecules share ≥1 primary target. Top 16 by shared-target count:

Molecule	Source	Status	Shared targets
BEXAGLIFLOZIN	ChEMBL + PubChem	Phase 4 (approved)	SLC5A1, SLC5A2
Canagliflozin	ChEMBL + PubChem	Phase 4 (approved)	SLC5A1, SLC5A2
EMPAGLIFLOZIN	ChEMBL + PubChem	Phase 4 (approved)	SLC5A1, SLC5A2
ERTUGLIFLOZIN	ChEMBL + PubChem	Phase 4 (approved)	SLC5A1, SLC5A2
SOTAGLIFLOZIN	ChEMBL + PubChem	Phase 4 (approved)	SLC5A1, SLC5A2
IPRAGLIFLOZIN	ChEMBL	Phase 4 (approved)	SLC5A1, SLC5A2
TOFOGLIFLOZIN	ChEMBL	Phase 4 (approved)	SLC5A1, SLC5A2
ENAVOGLIFLOZIN	ChEMBL	Phase 3	SLC5A1, SLC5A2
HENAGLIFLOZIN	ChEMBL	Phase 3	SLC5A1, SLC5A2
LICOGLIFLOZIN	ChEMBL	Phase 2	SLC5A1, SLC5A2
LUSEOGLIFLOZIN	ChEMBL	Phase 2	SLC5A1, SLC5A2
REMOGLIFLOZIN ETABONATE	ChEMBL	Phase 2	SLC5A1, SLC5A2
SERGLIFLOZIN ETABONATE	ChEMBL	Phase 2	SLC5A1, SLC5A2
MIZAGLIFLOZIN	ChEMBL	Phase 2	SLC5A1
YM-543 FREE ACID	ChEMBL	Phase 2	SLC5A2
Phlorizin	PubChem	Approved	SLC5A1