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bexagliflozin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sodium glucose co-transporter inhibitors, phlorizin derivatives | 5708 | 1118567-05-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Bexagliflozin is an inhibitor of sodium-glucose co-transporter 2 (SGLT2), the transporter responsible for reabsorption of the majority of glucose from the renal glomerular filtrate in the renal proximal tubule. By inhibiting SGLT2, bexagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.216 | Moderate | 0.68 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 25.882 | Moderate | 0.68 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 8.241 | 10^-6 cm/s | Moderate | 0.68 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.420 | uL/min/10^6 cells | Moderate | 0.68 |
| dppb | Dog plasma protein binding (% unbound) | 5.780 | % | Moderate | 0.68 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 10.430 | % | Moderate | 0.68 |
| herg | hERG pIC50 | 4.588 | pIC50 | Moderate | 0.68 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.776 | uL/min/10^6 cells | Moderate | 0.68 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.634 | uL/min/mg protein | Moderate | 0.68 |
| hppb | Human plasma protein binding (% unbound) | 5.030 | % | Moderate | 0.68 |
| kinase-safety-class | ACVR2B,BRAF,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK,ZAP70 | 18 | |||
| kinase-selectivity-class | MAP2K6 | 1 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 24.266 | Moderate | 0.75 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 15.885 | Moderate | 0.68 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 12.618 | Moderate | 0.68 | |
| mppb | Mouse plasma protein binding (% unbound) | 3.830 | Moderate | 0.68 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 46.132 | Moderate | 0.68 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 8.310 | % | Moderate | 0.68 |
| rat-kpuu-brain | Rat brain Kpuu | 0.018 | % | Moderate | 0.75 |
| rh-clint | Rat hepatocyte intrinsic clearance | 9.484 | uL/min/10^6 cells | Moderate | 0.68 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 52.590 | % | Moderate | 0.68 |
| rppb | Rat plasma protein binding (% unbound) | 2.720 | % | Moderate | 0.68 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 279.254 | uM | Moderate | 0.68 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 20, 2023 | FDA | THERACOSBIO LLC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BK08 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Sodium-glucose co-transporter 2 (SGLT2) inhibitors |
| MeSH PA | D007004 | Hypoglycemic Agents |
| FDA MoA | N0000187058 | Sodium-Glucose Transporter 2 Inhibitors |
| FDA EPC | N0000187059 | Sodium-Glucose Cotransporter 2 Inhibitor |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:73273 | sodium-glucose transport protein subtype 2 inhibitor |
Related Drugs by ATC class:
A10BK Sodium-glucose co-transporter 2 (SGLT2) inhibitors 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
| Renal dialysis | contraindication | 265764009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 20MG | BRENZAVVY | THERACOSBIO | N214373 | Jan. 20, 2023 | RX | TABLET | ORAL | 8106021 | Aug. 22, 2028 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 20MG | BRENZAVVY | THERACOSBIO | N214373 | Jan. 20, 2023 | RX | TABLET | ORAL | 8802637 | Aug. 22, 2028 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 20MG | BRENZAVVY | THERACOSBIO | N214373 | Jan. 20, 2023 | RX | TABLET | ORAL | 7838499 | Jan. 30, 2029 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
| 20MG | BRENZAVVY | THERACOSBIO | N214373 | Jan. 20, 2023 | RX | TABLET | ORAL | 10533032 | July 3, 2031 | AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 20MG | BRENZAVVY | THERACOSBIO | N214373 | Jan. 20, 2023 | RX | TABLET | ORAL | Jan. 20, 2028 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium/glucose cotransporter 2 | Transporter | INHIBITOR | IC50 | 8.70 | DRUG LABEL | DRUG LABEL | |||
| Sodium/glucose cotransporter 1 | Transporter | INHIBITOR | IC50 | 5.25 | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:229225 | CHEBI |
| CHEMBL1808388 | ChEMBL_ID |
| C000705992 | MESH_SUPPLEMENTAL_RECORD_UI |
| 12335 | IUPHAR_LIGAND_ID |
| DB12236 | DRUGBANK_ID |
| 4042477 | VANDF |
| C4519094 | UMLSCUI |
| 10159 | INN_ID |
| 25195624 | PUBCHEM_CID |
| 364775 | MMSL |
| 372300 | MMSL |
| 41199 | MMSL |
| d09978 | MMSL |
| 019273 | NDDF |
| D10865 | KEGG_DRUG |
| EY00JF42FV | UNII |
| 2627044 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Bexagliflozin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-918 | TABLET | 20 mg | ORAL | NDA authorized generic | 26 sections |
| Bexagliflozin | Human Prescription Drug Label | 1 | 82381-2000 | TABLET | 20 mg | ORAL | NDA AUTHORIZED GENERIC | 27 sections |
| BRENZAVVY | Human Prescription Drug Label | 1 | 82381-2174 | TABLET | 20 mg | ORAL | NDA | 27 sections |