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

Stem definitionDrug idCAS RN
angiotensin-converting enzyme inhibitors 1245 98048-97-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fosinopril
  • fosinopril sodium
  • fosenopril
  • fozitec
  • fosinapril
A phosphinic acid-containing angiotensin-converting enzyme inhibitor that is effective in the treatment of hypertension. It is a prodrug that is converted to its active metabolite fosinoprilat.
  • Molecular weight: 563.67
  • Formula: C30H46NO7P
  • CLOGP: 7.44
  • LIPINSKI: 2
  • HAC: 8
  • HDO: 1
  • TPSA: 110.21
  • ALOGS: -5.75
  • ROTB: 15

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
15 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.02 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) 2.36 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 34 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
May 16, 1991 FDA

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
Hyperkalaemia 73.64 50.98 15 111 5878 2352081
Acute kidney injury 68.54 50.98 19 107 28103 2329856
Orthostatic hypotension 58.28 50.98 11 115 2868 2355091
Renal failure 57.52 50.98 15 111 17334 2340625
Angioedema 51.86 50.98 12 114 8384 2349575

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
Angioedema 374.38 54.94 81 275 9583 1736842
Hyperkalaemia 216.02 54.94 51 305 8496 1737929
Acute kidney injury 197.48 54.94 64 292 34880 1711545
Cough 71.07 54.94 26 330 19171 1727254
Hypotension 63.43 54.94 27 329 29627 1716798
Blood urea increased 57.99 54.94 16 340 4695 1741730
Wheezing 55.26 54.94 15 341 4138 1742287

Pharmacologic Action:

SourceCodeDescription
ATC C09AA09 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, PLAIN
ACE inhibitors, plain
ATC C09BA09 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and diuretics
FDA EPC N0000175562 Angiotensin Converting Enzyme Inhibitor
MeSH PA D000806 Angiotensin-Converting Enzyme Inhibitors
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
CHEBI has role CHEBI:35457 EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:35674 antihypertensive agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Chronic heart failure indication 48447003
Atrial fibrillation off-label use 49436004 DOID:0060224
Diabetic renal disease off-label use 127013003
Acute scleroderma renal crisis off-label use 236503001
Diastolic heart failure off-label use 418304008 DOID:9775
Nondiabetic Proteinuric Nephropathy off-label use
Hypertension due to Scleroderma off-label use
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Acute cerebrovascular insufficiency contraindication 29322000
Dehydration contraindication 34095006
Hyperuricemia contraindication 35885006 DOID:1920
Immunosuppression contraindication 38013005
Angioedema contraindication 41291007 DOID:1558
Hypokalemia contraindication 43339004
Low blood pressure contraindication 45007003
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Aortic valve stenosis contraindication 60573004 DOID:1712
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Transplantation contraindication 77465005
Hereditary angioneurotic edema contraindication 82966003 DOID:14735
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:557
Disorder of connective tissue contraindication 105969002 DOID:65
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Hypertrophic cardiomyopathy contraindication 233873004 DOID:11984
Disease of liver contraindication 235856003 DOID:409
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Azotemia contraindication 445009001
Hemodialysis with High-Flux Membrane contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.98 acidic

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 9 CHEMBL CHEMBL
Angiotensin-converting enzyme Enzyme Ki 8.82 CHEMBL

External reference:

IDSource
4020531 VUID
N0000148247 NUI
C0118168 UMLSCUI
D00622 KEGG_DRUG
108569005 SNOMEDCT_US
4020531 VANDF
004501 NDDF
50166 RXNORM
372510000 SNOMEDCT_US
d00242 MMSL
CHEMBL581 ChEMBL_ID
C046965 MESH_SUPPLEMENTAL_RECORD_UI
DB00492 DRUGBANK_ID
NW2RTH6T2N UNII
88889-14-9 SECONDARY_CAS_RN
5833 INN_ID
KS8 PDB_CHEM_ID
CHEBI:5163 CHEBI
D017328 MESH_DESCRIPTOR_UI
CHEMBL3039596 ChEMBL_ID
CHEMBL3039598 ChEMBL_ID
55891 PUBCHEM_CID
6456 IUPHAR_LIGAND_ID
DB14207 DRUGBANK_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0185-0041 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0185-0042 TABLET 20 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0185-0047 TABLET 40 mg ORAL ANDA 12 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 23155-060 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 23155-061 TABLET 20 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 31722-200 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 31722-201 TABLET 20 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 31722-202 TABLET 40 mg ORAL ANDA 12 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 43353-870 TABLET 40 mg ORAL ANDA 13 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 43547-386 TABLET 10 mg ORAL ANDA 13 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 43547-387 TABLET 20 mg ORAL ANDA 13 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 43547-388 TABLET 40 mg ORAL ANDA 13 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-1112 TABLET 40 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-1504 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-3780 TABLET 10 mg ORAL ANDA 13 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-4743 TABLET 40 mg ORAL ANDA 13 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50436-0274 TABLET 40 mg ORAL ANDA 11 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50436-3138 TABLET 20 mg ORAL ANDA 11 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 53217-277 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 53217-278 TABLET 40 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-5055 TABLET 20 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-5064 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-5182 TABLET 40 mg ORAL ANDA 12 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 54868-5346 TABLET 10 mg ORAL ANDA 13 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 54868-5469 TABLET 20 mg ORAL ANDA 13 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 57237-026 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 57237-027 TABLET 20 mg ORAL ANDA 12 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 63304-403 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 63304-404 TABLET 20 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-5279 TABLET 10 mg ORAL ANDA 12 sections