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Empagliflozin

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Also known as BI 10773BI-10773Bi10773Empagliflozin component of glyxambiEmpagliflozin component of synjardyEmpagliflozin component of trijardy xrEmpagliflozinaEmpagliflozineJardianceEMPAGLIFLOZIN (BI10773)

Summary

Empagliflozin (CHEMBL2107830) is an approved small-molecule sodium-glucose transport protein subtype 2 inhibitor (ATC A10BK03) targeting SLC5A1 and SLC5A2; indicated across 37 conditions including diabetes mellitus and heart failure.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: A10BK03
  • Targets: 2 (SLC5A1, SLC5A2)
  • Indications: 37 conditions
  • Clinical trials: 407
  • Chemistry: 450.9 Da · C23H27ClO7

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2107830
NameEmpagliflozin
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID11949646
ChEBICHEBI:82720
ATCA10BK03
Molecular formulaC23H27ClO7
Molecular weight450.9
InChIKeyOBWASQILIWPZMG-QZMOQZSNSA-N

SMILES: C1COC[C@H]1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)Cl

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

ChEBI definition: A C-glycosyl compound consisting of a β-glucosyl residue having a (4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl group at the anomeric centre. A sodium-glucose co-transporter 2 inhibitor used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

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

Also known as: BI 10773, Bi 10773, BI-10773, Bi10773, Empagliflozin, Empagliflozin component of glyxambi, Empagliflozin component of synjardy, Empagliflozin component of trijardy xr, Empagliflozina, Empagliflozine, Jardiance, EMPAGLIFLOZIN

Patent coverage: 1,682 distinct patent families (3,982 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,463 (87%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
SLC5A1Sodium/glucose cotransporter 1Inhibition5.10%P13866
SLC5A2Sodium/glucose cotransporter 2Inhibition8.50.2%P31639

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Sodium/glucose cotransporter 2, Synaptic vesicular amine transporter, Sodium/glucose cotransporter 1.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 13 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
SLC5A28.52EC503nMCHEMBL_ACT_19005392
SLC5A28.51IC503.1nMCHEMBL_ACT_16259933
SLC5A28.51IC503.1nMCHEMBL_ACT_18665717
SLC5A28.51IC503.1nMCHEMBL_ACT_18728730
SLC5A28.51IC503.1nMCHEMBL_ACT_25634248
SLC5A28.51IC503.1nMCHEMBL_ACT_25874431
SLC5A28.51IC503.1nMCHEMBL_ACT_26593976
SLC5A28.51IC503.1nMCHEMBL_ACT_29054648
SLC5A15.49IC503235nMCHEMBL_ACT_16299538
SLC5A15.49IC503235nMCHEMBL_ACT_26594060
SLC5A15.08EC508300nMCHEMBL_ACT_19005391
SLC5A15.08IC508300nMCHEMBL_ACT_25634259

Target pathways

Aggregated over 2 target gene(s): SLC5A1, SLC5A2.

Top Reactome pathways

11 total, by targets touching each:

PathwayTargetsGenes
Disease2SLC5A1, SLC5A2
Cellular hexose transport2SLC5A1, SLC5A2
Transport of small molecules2SLC5A1, SLC5A2
SLC-mediated transmembrane transport2SLC5A1, SLC5A2
SLC transporter disorders2SLC5A1, SLC5A2
Disorders of transmembrane transporters2SLC5A1, SLC5A2
Defective SLC5A1 causes congenital glucose/galactose malabsorption (GGM)1SLC5A1
Defective SLC5A2 causes renal glucosuria (GLYS1)1SLC5A2
Intestinal absorption1SLC5A1
Digestion and absorption1SLC5A1
Intestinal hexose absorption1SLC5A1

Dominant GO biological processes

GO termTargets
alpha-glucoside transport2
sodium ion transport2
renal D-glucose absorption2
D-glucose import across plasma membrane2
sodium ion import across plasma membrane2
D-glucose transmembrane transport2
monoatomic ion transport2
transmembrane transport2
intestinal D-glucose absorption1
pentose transmembrane transport1
fucose transmembrane transport1
galactose transmembrane transport1
myo-inositol transport1
transepithelial water transport1
intestinal hexose absorption1

Indications & clinical

Indications

37 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).

IndicationTrial phaseMONDOEFO
diabetes mellitus4MONDO:0005015EFO:0000400
heart failure4MONDO:0005252EFO:0003144
chronic kidney disease4MONDO:0005300EFO:0003884
type 2 diabetes mellitus4MONDO:0005148MONDO:0005148
gestational diabetes3MONDO:0005406EFO:0004593
diabetic kidney disease3MONDO:0005016EFO:0000401
metabolic dysfunction-associated steatotic liver disease3MONDO:0013209EFO:0003095
myocardial infarction3MONDO:0005068EFO:0000612
acute myocardial infarction3MONDO:0004781EFO:0008583
severe acute respiratory syndrome3MONDO:0005091EFO:0000694
type 1 diabetes mellitus3MONDO:0005147MONDO:0005147
metabolic syndrome X3MONDO:0011565EFO:0000195
polycystic ovary syndrome2MONDO:0008487EFO:0000660
kidney disorder2MONDO:0005240EFO:0003086
inappropriate ADH syndrome2MONDO:0006802EFO:1000982
prediabetes syndrome2MONDO:0006920EFO:1001121
glycogen storage disease I2MONDO:0002413Orphanet:364
nephrolithiasis2MONDO:0008171EFO:0004253
portal hypertension2MONDO:0005080EFO:0000666
ulcerative colitis2MONDO:0005101EFO:0000729
hypoglycemia2MONDO:0004946HP:0001943
autosomal dominant polycystic kidney disease2MONDO:0004691EFO:1001496
major depressive disorder2MONDO:0002009MONDO:0002009
ST-elevation myocardial infarction2MONDO:0041656EFO:0008585
neoplasm2MONDO:0005070MONDO:0004992
Crohn disease1MONDO:0005011EFO:0000384
acute kidney injury1MONDO:0002492HP:0001919
inflammatory bowel disease1MONDO:0005265EFO:0003767
diabetic neuropathy1MONDO:0006626EFO:1000783
epilepsy0MONDO:0005027EFO:0000474

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

Clinical trials

Total trials: 407.

Phase distribution

PhaseTrials
PHASE4101
PHASE381
PHASE167
Not specified67
PHASE264
PHASE2/PHASE315
EARLY_PHASE18
PHASE1/PHASE24

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04447911PHASE4RECRUITINGEffects of the SGLT2 Inhibitor Empagliflozin in Patients With Euvolemic and Hypervolemic Hyponatremia
NCT05147090PHASE4ACTIVE_NOT_RECRUITINGEffects of Empagliflozin on Fibrosis and Cirrhosis in Chronic Hepatitis B Patients
NCT05164263PHASE4RECRUITINGReal World Safety & Efficacy Experience of Empagliflozin With or Without Metformin in T2DM Patients - EASE Study
NCT05426525PHASE4ACTIVE_NOT_RECRUITINGUse of Empagliflozin to Treat Prediabetes
NCT05671991PHASE4RECRUITINGEffect of Empagliflozin on Peritoneal and Kidney Function in End Stage Renal Disease
NCT06013865PHASE4RECRUITINGEmpagliflozin Treatment in Kidney Transplant Recipients
NCT06021145PHASE4RECRUITINGEffectiveness of Empagliflozin Added to Automated Insulin Delivery (AID) Systems in Adults With Type 1 Diabetes With Sub-optimal Glycemic Outcomes
NCT06055452PHASE4RECRUITINGEffects of SGLT2 Inhibitors in Pre-heart Failure Populations With Hypertension
NCT06110130PHASE4RECRUITINGEffect of Empagliflozin on Podocyte Specific Proteins in African American Veterans With NDKD
NCT06249932PHASE4RECRUITINGEmpagliflozin in Heart Failure with Reduced Ejection Fraction and End Stage Renal Disease
NCT06249945PHASE4RECRUITINGEMPAgliflozin in Heart Failure With PReserved Ejection Fraction and End Stage Renal Disease
NCT06260059PHASE4RECRUITINGEfficacy Of Sodium Glucose Transporter Inhibitor (SGLT2I) In Adult Patients With Congenital Heart Disease
NCT06391450PHASE4ACTIVE_NOT_RECRUITINGStudy of Empagliflozin in Patients With Autosomal Dominant Polycystic Kidney Disease (EMPA-PKD)
NCT06401343PHASE4RECRUITINGUse of SGLT2i in noHCM With HFpEF
NCT06410352PHASE4RECRUITINGEffectiveness of Weight Loss Methods on Lifespan for Metabolic Syndrome
NCT06613854PHASE4RECRUITINGEffect of Early Combination Antihyperglycemic Treatment on Metabolic Control in Individuals With Type 2 Diabetes
NCT06625073PHASE4RECRUITINGRandomized Trial of SGLT2i in Heart Transplant Recipients
NCT06642272PHASE4RECRUITINGA Pragmatic Trial Comparing Empagliflozin and Dapagliflozin Through Cluster Randomization Embedded in the Electronic Health Record
NCT06674109PHASE4NOT_YET_RECRUITINGSAVE-Care (Sodium Glucose Cotransporter-2 Inhibitors [SGLT2i] As Novel Gout Care) Trial
NCT06706791PHASE4RECRUITINGEffect of Empagliflozin on Quality of Life in Chronic Heart Failure Patients With Diabetes Mellitus Type II
NCT06846411PHASE4RECRUITINGThe EMPA-FIT Study
NCT06862739PHASE4RECRUITINGGlycemic Control With Triple Pathway Approach Through Empagliflozin, Linagliptin and Metformin Combination
NCT06933355PHASE4ACTIVE_NOT_RECRUITINGAcute Effects of SGLT2 Inhibitor on Kidney Allograft Oxygen Tension
NCT07155694PHASE4NOT_YET_RECRUITINGRole of Finerenone in African American Veterans With Diabetic Kidney Disease
NCT07180745PHASE4NOT_YET_RECRUITINGEmpagliflozin Versus Statins in Non-Alcoholic Fatty Liver Disease
NCT07292909PHASE4RECRUITINGEffect of Empagliflozin on Inflammation
NCT07322237PHASE4RECRUITINGDICE Study- Diastolic Improvement With Carvedilol & Empagliflozin in Patients With Cirrhosis
NCT07365358PHASE4NOT_YET_RECRUITINGEvaluate the Efficacy and Safety of Empagliflozin or Glimepiride Combination Therapy in Type 2 Diabetes Mellitus Patients
NCT07442006PHASE4RECRUITINGGlycemic Variability of Combination Therapies in T2DM
NCT07452913PHASE4ENROLLING_BY_INVITATIONMetformin, Empagliflozin With Sitagliptin vs Linagliptin in Type 2 Diabetes
NCT07547878PHASE4NOT_YET_RECRUITINGRapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD)
NCT01001962PHASE4UNKNOWNDouble Blind Placebo Study of JARDIANCE® (Empagliflozin) in Prehypertensives Type II Diabetics
NCT02401880PHASE4COMPLETEDEffects of Linagliptin in Addition to Empagliflozin on Islet Cell Physiology
NCT02589626PHASE4COMPLETEDLong-term Safety and Efficacy of Empagliflozin as Add on to GLP-1 RA
NCT02589639PHASE4COMPLETEDEfficacy and Safety Study of Empagliflozin as add-on to Insulin in Japanese Patients With Type 2 Diabetes Mellitus
NCT02637973PHASE4COMPLETEDEffects of Empagliflozin on Liver Fat Content, Energy Metabolism and Body Composition in Patients With Type 2 Diabetes
NCT02728453PHASE4TERMINATEDSGLT2 Inhibition and Left Ventricular Mass
NCT02768220PHASE4WITHDRAWNThe Effect of Sodium-Glucose Cotransporter 2 Inhibitors on Advanced Glycation End Products
NCT02798744PHASE4COMPLETEDSGLT-2 Inhibitor Empagliflozin Effects on Appetite and Weight Regulation.
NCT02833415PHASE4COMPLETEDVisceral Adiposity and Diabetes: Translating Form to Function Using Imaging

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 7 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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:

MoleculeSourceStatusShared targets
BEXAGLIFLOZINChEMBL + PubChemPhase 4 (approved)SLC5A1, SLC5A2
CanagliflozinChEMBL + PubChemPhase 4 (approved)SLC5A1, SLC5A2
ERTUGLIFLOZINChEMBL + PubChemPhase 4 (approved)SLC5A1, SLC5A2
SOTAGLIFLOZINChEMBL + PubChemPhase 4 (approved)SLC5A1, SLC5A2
DAPAGLIFLOZINChEMBLPhase 4 (approved)SLC5A1, SLC5A2
IPRAGLIFLOZINChEMBLPhase 4 (approved)SLC5A1, SLC5A2
TOFOGLIFLOZINChEMBLPhase 4 (approved)SLC5A1, SLC5A2
ENAVOGLIFLOZINChEMBLPhase 3SLC5A1, SLC5A2
HENAGLIFLOZINChEMBLPhase 3SLC5A1, SLC5A2
LICOGLIFLOZINChEMBLPhase 2SLC5A1, SLC5A2
LUSEOGLIFLOZINChEMBLPhase 2SLC5A1, SLC5A2
REMOGLIFLOZIN ETABONATEChEMBLPhase 2SLC5A1, SLC5A2
SERGLIFLOZIN ETABONATEChEMBLPhase 2SLC5A1, SLC5A2
MIZAGLIFLOZINChEMBLPhase 2SLC5A1
YM-543 FREE ACIDChEMBLPhase 2SLC5A2
PhlorizinPubChemApprovedSLC5A1

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot