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phenformin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihyperglycaemics, phenformin derivatives | 2126 | 114-86-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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)
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 8.14 µM/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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.318 | Moderate | 0.68 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.276 | Moderate | 0.68 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.867 | 10^-6 cm/s | Moderate | 0.68 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.945 | uL/min/10^6 cells | Moderate | 0.68 |
| dppb | Dog plasma protein binding (% unbound) | 14.690 | % | Moderate | 0.68 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 35.310 | % | Moderate | 0.68 |
| herg | hERG pIC50 | 4.760 | pIC50 | Moderate | 0.68 |
| hh-clint | Human hepatocyte intrinsic clearance | 27.290 | uL/min/10^6 cells | Moderate | 0.68 |
| hlm-clint | Human liver microsomal intrinsic clearance | 17.579 | uL/min/mg protein | Moderate | 0.68 |
| hppb | Human plasma protein binding (% unbound) | 15.970 | % | Moderate | 0.68 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK4,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK1,JAK2,KIT,MAP2K1,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 | 69 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,CAMK2D,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,FLT3,GRK2,MAP3K10,MAP3K21,MAPK7,PDK4,PIK3CD,SIK2,STK33,TEK | 19 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.127 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.748 | Moderate | 0.68 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 13.836 | Moderate | 0.68 | |
| mppb | Mouse plasma protein binding (% unbound) | 12.960 | Moderate | 0.68 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.710 | Moderate | 0.68 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 29.710 | % | Moderate | 0.68 |
| rh-clint | Rat hepatocyte intrinsic clearance | 17.298 | uL/min/10^6 cells | Moderate | 0.68 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 48.270 | % | Moderate | 0.68 |
| rppb | Rat plasma protein binding (% unbound) | 34.210 | % | Moderate | 0.68 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 680.769 | uM | Moderate | 0.68 |
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:
| Source | Code | Description |
|---|---|---|
| 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 | hypoglycemic agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:176497 | geroprotector |
Related Drugs by ATC class:
A10BD Combinations of oral blood glucose lowering drugs 19 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| 5'-AMP-activated protein kinase subunit beta-1 | Kinase | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 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 |
| DD5K7529CE | INXIGHT DRUGS |
Pharmaceutical products:
None