azilsartan medoxomil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic) 4322 863031-21-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • TAK 491
  • edarbi
  • azilsartan medoxomil
  • azilsartan kamedoxomil
an angiotensin type 1 receptor blocker; receptor blocker
  • Molecular weight: 568.54
  • Formula: C30H24N4O8
  • CLOGP: 4.24
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 1
  • TPSA: 139.57
  • ALOGS: -4.91
  • ROTB: 10

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
40 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 25, 2011 FDA ARBOR PHARMS IRELAND

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Renal failure 39.27 38.83 11 108 17338 2340628

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
ATC C09CA09 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN
Angiotensin II receptor blockers (ARBs), plain
ATC C09DA09 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
Angiotensin II receptor blockers (ARBs) and diuretics
FDA MoA N0000180999 Angiotensin 2 Type 1 Receptor Antagonists
FDA EPC N0000175561 Angiotensin 2 Receptor Blocker
FDA PE N0000178477 Decreased Blood Pressure
MeSH PA D047228 Angiotensin II Type 1 Receptor Blockers
MeSH PA D057911 Angiotensin Receptor Antagonists
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:61016 angiotensin receptor antagonist
CHEBI has role CHEBI:35674 antihypertensive agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Hypovolemia contraindication 28560003
Low blood pressure contraindication 45007003
Hyponatremia contraindication 89627008
Impaired renal function disorder contraindication 197663003
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.11 acidic
pKa2 3.02 Basic
pKa3 2.4 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 40MG MEDOXOMIL EDARBI ARBOR PHARMS LLC N200796 Feb. 25, 2011 RX TABLET ORAL 7572920 Jan. 7, 2025 TREATMENT OF HYPERTENSION
EQ 80MG MEDOXOMIL EDARBI ARBOR PHARMS LLC N200796 Feb. 25, 2011 RX TABLET ORAL 7572920 Jan. 7, 2025 TREATMENT OF HYPERTENSION
EQ 40MG MEDOXOMIL EDARBYCLOR ARBOR PHARMS LLC N202331 Dec. 20, 2011 RX TABLET ORAL 7572920 Jan. 7, 2025 TREATMENT OF HYPERTENSION
EQ 40MG MEDOXOMIL EDARBYCLOR ARBOR PHARMS LLC N202331 Dec. 20, 2011 RX TABLET ORAL 9387249 July 1, 2031 TREATMENT OF HYPERTENSION

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 UNKNOWN CHEMBL
Type-1 angiotensin II receptor GPCR IC50 6.38 CHEMBL

External reference:

IDSource
C2979837 UMLSCUI
D08067 KEGG_DRUG
013662 NDDF
27787 MMSL
4030594 VANDF
449561004 SNOMEDCT_US
1091642 RXNORM
CHEMBL57242 ChEMBL_ID
F9NUX55P23 UNII
8724 INN_ID
147403-03-0 SECONDARY_CAS_RN
C521273 MESH_SUPPLEMENTAL_RECORD_UI
DB08822 DRUGBANK_ID
CHEBI:68845 CHEBI
6900 IUPHAR_LIGAND_ID
CHEMBL2028661 ChEMBL_ID
CHEMBL2103795 ChEMBL_ID
135409642 PUBCHEM_CID
C557413 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None