Bexagliflozin
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Also known as BexagliflozinaBexagliflozineBrenzavvyEGT-0001442EGT-1442EGT0001442EGT1442THR-1442THR1442
Summary
Bexagliflozin (CHEMBL1808388) is an approved small-molecule sodium-glucose transport protein subtype 2 inhibitor (ATC A10BK08) targeting SLC5A1 and SLC5A2; indicated across 3 conditions including diabetes mellitus and type 2 diabetes mellitus.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: A10BK08
- Targets: 2 (SLC5A1, SLC5A2)
- Indications: 3 conditions
- Clinical trials: 20
- Chemistry: 464.9 Da · C24H29ClO7
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1808388 |
| Name | Bexagliflozin |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 25195624 |
| ChEBI | CHEBI:229225 |
| ATC | A10BK08 |
| Molecular formula | C24H29ClO7 |
| Molecular weight | 464.9 |
| InChIKey | BTCRKOKVYTVOLU-SJSRKZJXSA-N |
SMILES: C1CC1OCCOC2=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-(2-cyclopropyloxyethoxy)phenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
ChEBI definition: A C-glycosyl comprising of β-D-glucose in which the anomeric hydroxy group is replaced by a 4-chloro-3-({4-[2-(cyclopropyloxy)ethoxy]phenyl}methyl)phenyl group. It is a sodium-glucose co-transporter 2 (SGLT2) inhibitor indicated 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, antihypertensive agent.
Also known as: Bexagliflozin, Bexagliflozina, Bexagliflozine, Brenzavvy, EGT-0001442, EGT-1442, EGT0001442, EGT1442, THR-1442, THR1442, BEXAGLIFLOZIN
Patent coverage: 172 distinct patent families (463 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 451 (97%) 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 |
|---|---|---|---|---|---|
| SLC5A1 | Sodium/glucose cotransporter 1 | Inhibition | 5.25 | 0% | P13866 |
| SLC5A2 | Sodium/glucose cotransporter 2 | Inhibition | 8.64 | 0.2% | P31639 |
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Sodium/glucose cotransporter 2, Sodium/glucose cotransporter 1.
Bioactivity
ChEMBL activities: 3 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| SLC5A2 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_26335985 |
| SLC5A2 | 8.64 | IC50 | 2.3 | nM | CHEMBL_ACT_6294971 |
| SLC5A1 | 5.25 | IC50 | 5600 | nM | CHEMBL_ACT_6294955 |
Target pathways
Aggregated over 2 target gene(s): SLC5A1, SLC5A2.
Top Reactome pathways
11 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 |
| 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 |
|---|---|
| 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 |
| monoatomic ion transport | 2 |
| transmembrane transport | 2 |
| intestinal D-glucose absorption | 1 |
| pentose transmembrane transport | 1 |
| fucose transmembrane transport | 1 |
| galactose transmembrane transport | 1 |
| myo-inositol transport | 1 |
| transepithelial water transport | 1 |
| intestinal hexose absorption | 1 |
Indications & clinical
Indications
3 indications (2 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 |
| type 2 diabetes mellitus | 4 | MONDO:0005148 | MONDO:0005148 |
| essential hypertension | 2 | MONDO:0001134 | MONDO:0001134 |
Clinical trials
Total trials: 20.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 7 |
| PHASE1 | 7 |
| PHASE2 | 3 |
| PHASE4 | 2 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05612594 | PHASE4 | RECRUITING | Adipose Dysfunction, Imaging, Physiology, and Outcomes With Sodium Glucose Cotransporter 2 Inhibitor (SGLT2i) for Sleep Apnea: The ADIPOSA Study |
| NCT07547878 | PHASE4 | NOT_YET_RECRUITING | Rapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD) |
| NCT02558296 | PHASE3 | COMPLETED | Bexagliflozin Efficacy and Safety Trial |
| NCT02715258 | PHASE3 | COMPLETED | Safety and Efficacy of Bexagliflozin as Monotherapy in Patients With Type 2 Diabetes |
| NCT02769481 | PHASE3 | COMPLETED | Safety and Efficacy of Bexagliflozin Compared to Glimepiride as Add-on Therapy to Metformin in Type 2 Diabetes Subjects |
| NCT02836873 | PHASE3 | COMPLETED | Safety and Efficacy of Bexagliflozin in Type 2 Diabetes Mellitus Patients With Moderate Renal Impairment |
| NCT03115112 | PHASE3 | COMPLETED | Safety and Efficacy of Bexagliflozin Compared to Sitagliptin as Add-on Therapy to Metformin in Type 2 Diabetes Subjects |
| NCT03259789 | PHASE3 | COMPLETED | Safety and Efficacy of Bexagliflozin Compared to Placebo as Add-on Therapy to Metformin in Type 2 Diabetes Subjects |
| NCT03514641 | PHASE2/PHASE3 | COMPLETED | An Integrated Assessment of the Safety and Effectiveness of Bexagliflozin for the Management of Essential Hypertension |
| NCT05159882 | PHASE3 | UNKNOWN | Safety and Efficacy of THR-1442 Compared to Dapagliflozin as Add-on Therapy to Metformin in T2DM |
| NCT01029704 | PHASE2 | COMPLETED | Safety and Efficacy Study of EGT0001442 in Subjects With Type 2 Diabetes Mellitus |
| NCT01377844 | PHASE2 | COMPLETED | Efficacy and Safety of EGT0001442 in Patients With Type 2 Diabetes Mellitus |
| NCT02390050 | PHASE2 | COMPLETED | A Dose Range Finding Study to Evaluate the Effect of Bexagliflozin Tablets in Subjects With Type 2 Diabetes Mellitus |
| NCT02820298 | PHASE1 | COMPLETED | Study to Evaluate the Effects of a High-Fat Meal on Bexagliflozin in Healthy Subjects |
| NCT02956044 | PHASE1 | COMPLETED | Interaction of Bexagliflozin With Metformin, Glimepiride and Sitagliptin |
| NCT03167411 | PHASE1 | COMPLETED | Bexagliflozin Drug/Drug Interaction Study With Exenatide Injection |
| NCT03197324 | PHASE1 | COMPLETED | Bexagliflozin Drug/Drug Interaction Study With Digoxin |
| NCT03296800 | PHASE1 | COMPLETED | Study to Evaluate Effects of Probenecid, Rifampin and Verapamil on Bexagliflozin in Healthy Subjects |
| NCT03417076 | PHASE1 | WITHDRAWN | Absolute Bioavailability Study With Bexagliflozin |
| NCT03557658 | PHASE1 | COMPLETED | Safety and Efficacy of Bexagliflozin in Subjects With Moderate Hepatic Impairment |
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 |
|---|---|---|---|
| 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 |
| DAPAGLIFLOZIN | ChEMBL | 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 |
Related Atlas pages
- Genes: SLC5A1, SLC5A2
- Diseases: diabetes mellitus, type 2 diabetes mellitus
- Drugs: Canagliflozin, Empagliflozin, Ertugliflozin, Sotagliflozin, Dapagliflozin, Ipragliflozin, Tofogliflozin, Enavogliflozin, Henagliflozin