bexagliflozin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
sodium glucose co-transporter inhibitors, phlorizin derivatives 5708 1118567-05-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bexagliflozin
  • brenzavvy
  • EGT0001442
  • EGT1442
  • THR1442
  • THR-1442
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.
  • Molecular weight: 464.94
  • Formula: C24H29ClO7
  • CLOGP:
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 4
  • TPSA: 108.61
  • ALOGS:
  • ROTB: 9

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
MeSH PA D007004 Hypoglycemic Agents
FDA MoA N0000187058 Sodium-Glucose Transporter 2 Inhibitors
FDA EPC N0000187059 Sodium-Glucose Cotransporter 2 Inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
20MG BRENZAVVY THERACOSBIO N214373 Jan. 20, 2023 RX TABLET ORAL Jan. 20, 2028 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
CHEMBL1808388 ChEMBL_ID
C000705992 MESH_SUPPLEMENTAL_RECORD_UI
12335 IUPHAR_LIGAND_ID
DB12236 DRUGBANK_ID
019273 NDDF
C4519094 UMLSCUI
10159 INN_ID
25195624 PUBCHEM_CID
2627044 RXNORM
364775 MMSL
41199 MMSL
D10865 KEGG_DRUG
EY00JF42FV UNII
d09978 MMSL

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BRENZAVVY Human Prescription Drug Label 1 82381-2174 TABLET 20 mg ORAL NDA 26 sections