phenformin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihyperglycaemics, phenformin derivatives 2126 114-86-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • phenformin
  • phenformin hydrochloride
  • phenformin HCl
A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)
  • Molecular weight: 205.27
  • Formula: C10H15N5
  • CLOGP: -1.03
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 5
  • TPSA: 97.78
  • ALOGS: -2.95
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 8.14 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 55 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility) 48 mg/mL Bocci G, Oprea TI, Benet LZ

Approvals:

None

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
ATC A10BA01 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Biguanides
ATC A10BD01 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
MeSH PA D007004 Hypoglycemic Agents
CHEBI has role CHEBI:35526 antidiabetic
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:176497 geroprotectors

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

None




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.51 Basic
pKa2 2.78 Basic

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
5'-AMP-activated protein kinase subunit beta-1 Kinase WOMBAT-PK

External reference:

IDSource
4025255 VUID
N0000171785 NUI
D08351 KEGG_DRUG
4025255 VANDF
C0031404 UMLSCUI
CHEBI:8064 CHEBI
8CV PDB_CHEM_ID
CHEMBL170988 ChEMBL_ID
DB00914 DRUGBANK_ID
D010629 MESH_DESCRIPTOR_UI
8249 PUBCHEM_CID
931 INN_ID
834-28-6 SECONDARY_CAS_RN
DD5K7529CE UNII
235288 RXNORM
000914 NDDF
004533 NDDF
362949009 SNOMEDCT_US
CHEMBL1528839 ChEMBL_ID

Pharmaceutical products:

None