fimasartan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic) 4906 247257-48-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fimasartan
  • kanarb
  • fimasartan potassium
  • fimasartan potassium hydrate
  • fimasartan potassium trihydrate
  • BR-A-657
an angiotensin II receptor antagonist
  • Molecular weight: 501.65
  • Formula: C27H31N7OS
  • CLOGP: 3.02
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 1
  • TPSA: 90.37
  • ALOGS: -5.03
  • ROTB: 9

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.60 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.50 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.635 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 14.689 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 9.354 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 6.067 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 7.250 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 8.590 % High 1
herg hERG pIC50 4.259 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 4.742 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 13.243 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 3.040 % High 1
kinase-safety-class ACVR2B,AXL,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,MAPK7,PDK1,PDK4,PRKDC,TEK 13
kinase-selectivity-class EIF2AK3 1
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 8.872 Moderate 0.65
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 5.297 High 1
mh-clint Mouse hepatocyte intrinsic clearance 25.586 High 1
mppb Mouse plasma protein binding (% unbound) 4.060 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 10.789 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 6.510 % High 1
rat-kpuu-brain Rat brain Kpuu 0.012 % Moderate 0.65
rh-clint Rat hepatocyte intrinsic clearance 12.417 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 57.320 % High 1
rppb Rat plasma protein binding (% unbound) 2.020 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 972.747 uM High 1

Approvals:

DateAgencyCompanyOrphan
Sept. 1, 2010 Korean Food and Drug Administration (KFDA)

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 C09CA10 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN
Angiotensin II receptor blockers (ARBs), plain
ATC C09DA10 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
Angiotensin II receptor blockers (ARBs) and diuretics
ATC C09DB09 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
Angiotensin II receptor blockers (ARBs) and calcium channel blockers
ATC C10BX16 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
Lipid modifying agents in combination with other drugs
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35821 anticholesteremic drug
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

C09CA Angiotensin II receptor blockers (ARBs), plain 9 drugs
azilsartan medoxomilcandesartan cilexetileprosartanirbesartanlosartanolmesartan medoxomiltasosartantelmisartanvalsartan
C09DA Angiotensin II receptor blockers (ARBs) and diuretics 8 drugs
azilsartan medoxomilcandesartan cilexetileprosartanirbesartanlosartanolmesartan medoxomiltelmisartanvalsartan
C09DB Angiotensin II receptor blockers (ARBs) and calcium channel blockers 8 drugs
amlodipinecandesartan cilexetilirbesartanlercanidipinelosartanolmesartan medoxomiltelmisartanvalsartan
C10BX Lipid modifying agents in combination with other drugs 14 drugs
acetylsalicylic acidamlodipineatorvastatincandesartan cilexetilindapamidelisinoprilnebivololperindoprilpravastatinramiprilrosuvastatinsimvastatin show all 14 →

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

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.25 acidic
pKa2 3.3 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
Type-1 angiotensin II receptor GPCR ANTAGONIST IC50 9.38 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
D10556 KEGG_DRUG
CHEBI:136044 CHEBI
CHEMBL1951143 ChEMBL_ID
CHEMBL4297548 ChEMBL_ID
C558933 MESH_SUPPLEMENTAL_RECORD_UI
1020110-23-9 SECONDARY_CAS_RN
DB09279 DRUGBANK_ID
1332433003 SNOMEDCT_US
1332434009 SNOMEDCT_US
C2825622 UMLSCUI
8678 INN_ID
9870652 PUBCHEM_CID
P58222188P UNII

Pharmaceutical products:

None