cilazapril Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
angiotensin-converting enzyme inhibitors 641 88768-40-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cilazapril monohydrobromide
  • cilazapril anhydrous
  • cilazapril
  • inhibace
  • vascace
  • cilazapril monohydrate
  • cilazapril hydrate
One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors) used for hypertension. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat.
  • Molecular weight: 417.51
  • Formula: C22H31N3O5
  • CLOGP: 1.47
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 99.18
  • ALOGS: -2.59
  • ROTB: 9

Drug dosage:

DoseUnitRoute
2.50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 1 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.34 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 60 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

None

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
Labile hypertension 136.62 127.09 13 22 66 2357984

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
Hypertension 10.41 0 3 17 19445 1727316

Pharmacologic Action:

SourceCodeDescription
ATC C09AA08 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, PLAIN
ACE inhibitors, plain
ATC C09BA08 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and diuretics
MeSH PA D000806 Angiotensin-Converting Enzyme Inhibitors
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35457 EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor

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 1.93 acidic
pKa2 7.61 Basic
pKa3 3.71 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
Angiotensin-converting enzyme Enzyme INHIBITOR IC50 8.70 WOMBAT-PK SCIENTIFIC LITERATURE

External reference:

IDSource
4025239 VUID
N0000171771 NUI
C0055723 UMLSCUI
D01069 KEGG_DRUG
19KW7PI29F UNII
92077-78-6 SECONDARY_CAS_RN
318913001 SNOMEDCT_US
4025239 VANDF
21102 RXNORM
395947008 SNOMEDCT_US
003950 NDDF
5675 INN_ID
CHEMBL515606 ChEMBL_ID
DB01340 DRUGBANK_ID
CHEBI:3698 CHEBI
6459 IUPHAR_LIGAND_ID
D017315 MESH_DESCRIPTOR_UI
C045980 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL2104578 ChEMBL_ID
56330 PUBCHEM_CID
DB15565 DRUGBANK_ID

Pharmaceutical products:

None