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

Stem definitionDrug idCAS RN
sodium glucose co-transporter inhibitors, phlorizin derivatives 4892 903565-83-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tofogliflozin
  • tofogliflozin hydrate
  • deberza
  • apleway
  • CSG452
inhibits sodium-glucose cotransporter 2
  • Molecular weight: 386.44
  • Formula: C22H26O6
  • CLOGP: 3.06
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 4
  • TPSA: 99.38
  • ALOGS: -3.07
  • ROTB: 4

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.63 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.07 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.46 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.70 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 0.98 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

DateAgencyCompanyOrphan
March 24, 2014 PMDA

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
MeSH PA D000077203 Sodium-Glucose Transporter 2 Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.04 acidic
pKa2 12.63 acidic
pKa3 13.27 acidic
pKa4 13.54 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium/glucose cotransporter 2 Transporter INHIBITOR IC50 8.54 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium/glucose cotransporter 1 Transporter IC50 5.07 SCIENTIFIC LITERATURE

External reference:

IDSource
P8DD8KX4O4 UNII
D09978 KEGG_DRUG
C3501434 UMLSCUI
CHEBI:136041 CHEBI
RT2 PDB_CHEM_ID
CHEMBL2110731 ChEMBL_ID
CHEMBL2105711 ChEMBL_ID
46908928 PUBCHEM_CID
DB11824 DRUGBANK_ID
C575086 MESH_SUPPLEMENTAL_RECORD_UI
9395 IUPHAR_LIGAND_ID
1201913-82-7 SECONDARY_CAS_RN

Pharmaceutical products:

None