fimasartan Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

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

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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763

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
1020110-23-9 SECONDARY_CAS_RN
CHEBI:136044 CHEBI
CHEMBL1951143 ChEMBL_ID
C558933 MESH_SUPPLEMENTAL_RECORD_UI
8678 INN_ID
DB09279 DRUGBANK_ID
P58222188P UNII
9870652 PUBCHEM_CID
C2825622 UMLSCUI
CHEMBL4297548 ChEMBL_ID
CHEMBL1951146 ChEMBL_ID

Pharmaceutical products:

None