fosinopril 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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: 7.45
  • 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) 1 Bocci G, Oprea TI, Benet LZ
S (Water solubility) 100 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 2.36 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 34 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,STK33,TEK,TGFBR1,ZAP70 27
kinase-selectivity-class AXL,BRAF,EIF2AK3,GRK2,MAP2K6 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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
Cardiac failure congestive 85.18 17.50 56 4482 98638 90525271
Myocardial infarction 67.68 17.50 50 4488 105922 90517987
Diverticular perforation 64.25 17.50 18 4520 3754 90620155
Cerebrovascular accident 44.78 17.50 42 4496 123491 90500418
Steatorrhoea 37.15 17.50 8 4530 560 90623349
International normalised ratio increased 36.33 17.50 25 4513 47291 90576618
Body temperature decreased 34.83 17.50 19 4519 23797 90600112
Acute kidney injury 32.78 17.50 58 4480 320329 90303580
Orthostatic hypotension 31.88 17.50 22 4516 41805 90582104
Hyperkalaemia 31.35 17.50 26 4512 64938 90558971
Hypertensive crisis 31.13 17.50 16 4522 17768 90606141
Diabetes mellitus inadequate control 30.39 17.50 16 4522 18668 90605241
Renal failure 30.25 17.50 35 4503 130972 90492937
Angioedema 29.32 17.50 25 4513 64851 90559058
Urinary incontinence 29.20 17.50 20 4518 37546 90586363
Skin reaction 27.68 17.50 15 4523 18538 90605371
Muscle haemorrhage 27.03 17.50 9 4529 3337 90620572
Anal incontinence 26.68 17.50 14 4524 16216 90607693
Swollen tongue 25.58 17.50 20 4518 45936 90577973
Labelled drug-food interaction medication error 24.40 17.50 5 4533 275 90623634
Nephropathy 24.34 17.50 11 4527 9224 90614685
Intercepted medication error 23.42 17.50 6 4532 891 90623018
Faeces discoloured 23.12 17.50 14 4524 21306 90602603
Ulcer 19.81 17.50 15 4523 32867 90591042
Lacunar infarction 19.24 17.50 7 4531 3370 90620539
Drug interaction 18.55 17.50 42 4496 276411 90347498
Salivary hypersecretion 18.32 17.50 9 4529 9083 90614826
Myalgia 18.25 17.50 32 4506 175093 90448816
Blood pressure increased 17.98 17.50 34 4504 197183 90426726

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 188.64 19.06 96 5194 42381 42573664
Bradycardia 107.22 19.06 87 5203 85397 42530648
Acute kidney injury 102.15 19.06 171 5119 367166 42248879
Cardiac failure congestive 67.31 19.06 67 5223 85535 42530510
Myocardial infarction 61.11 19.06 76 5214 123933 42492112
Hypoglycaemia 60.75 19.06 54 5236 59800 42556245
Hyperkalaemia 59.62 19.06 61 5229 80397 42535648
Rhabdomyolysis 53.94 19.06 57 5233 77962 42538083
Treatment noncompliance 46.40 19.06 38 5252 37634 42578411
Coronary artery disease 38.44 19.06 40 5250 53680 42562365
Schizophrenia 30.51 19.06 18 5272 10532 42605513
Acidosis 30.49 19.06 19 5271 12260 42603785
Blood urea increased 30.12 19.06 28 5262 32765 42583280
Inappropriate affect 27.67 19.06 8 5282 748 42615297
Metabolic acidosis 27.44 19.06 33 5257 51825 42564220
Hyperparathyroidism 27.37 19.06 9 5281 1290 42614755
Hypotension 26.49 19.06 81 5209 257550 42358495
End stage renal disease 25.34 19.06 19 5271 16539 42599506
Off label use 23.42 19.06 27 5263 638308 41977737
Hyperlactacidaemia 22.32 19.06 11 5279 4505 42611540
Swollen tongue 21.20 19.06 19 5271 21212 42594833
Asthenia 20.69 19.06 79 5211 280714 42335331
Therapeutic response changed 20.60 19.06 6 5284 575 42615470
Swelling face 20.56 19.06 21 5269 27533 42588512
International normalised ratio increased 19.73 19.06 27 5263 48141 42567904

FDA Adverse Event Reporting System (Geriatric)

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 183.22 15.88 108 8735 98392 110482064
Acute kidney injury 144.59 15.88 213 8630 635217 109945239
Cardiac failure congestive 134.67 15.88 105 8738 150895 110429561
Myocardial infarction 132.44 15.88 115 8728 191968 110388488
Bradycardia 106.92 15.88 93 8750 155424 110425032
Hyperkalaemia 94.93 15.88 82 8761 135714 110444742
Rhabdomyolysis 67.03 15.88 64 8779 120337 110460119
Coronary artery disease 61.98 15.88 49 8794 71641 110508815
Cerebrovascular accident 61.33 15.88 74 8769 181210 110399246
Hypoglycaemia 57.68 15.88 58 8785 116046 110464410
Treatment noncompliance 46.80 15.88 42 8801 72948 110507508
Diverticular perforation 46.72 15.88 18 8825 6344 110574112
Renal failure 44.25 15.88 71 8772 226503 110353953
International normalised ratio increased 38.84 15.88 41 8802 86731 110493725
Orthostatic hypotension 38.34 15.88 36 8807 66213 110514243
Faeces discoloured 33.25 15.88 25 8818 33923 110546533
Hypotension 31.77 15.88 103 8740 523746 110056710
End stage renal disease 30.84 15.88 20 8823 21453 110559003
Body temperature decreased 29.26 15.88 24 8819 36911 110543545
Steatorrhoea 28.46 15.88 8 8835 1053 110579403
Acidosis 27.58 15.88 19 8824 22512 110557944
Schizophrenia 25.76 15.88 18 8825 21808 110558648
Inappropriate affect 24.74 15.88 8 8835 1691 110578765
Blood creatinine increased 22.56 15.88 47 8796 182842 110397614
Off label use 22.31 15.88 55 8788 1500130 109080326
Urinary incontinence 21.81 15.88 23 8820 48564 110531892
Hyperparathyroidism 21.78 15.88 9 8834 3801 110576655
Acute myocardial infarction 21.71 15.88 30 8813 83747 110496709
Blood urea increased 21.16 15.88 24 8819 54933 110525523
Myalgia 20.58 15.88 51 8792 222330 110358126
Hyperlactacidaemia 20.57 15.88 11 8832 8275 110572181
Syncope 20.40 15.88 48 8795 202488 110377968
Skin reaction 19.44 15.88 15 8828 21129 110559327
Drug ineffective 19.43 15.88 60 8783 1520480 109059976
Swollen tongue 19.34 15.88 24 8819 60338 110520118
Product use in unapproved indication 19.11 15.88 6 8837 447371 110133085
Metabolic acidosis 19.09 15.88 31 8812 99713 110480743
Behaviour disorder 19.01 15.88 11 8832 9636 110570820
Anal incontinence 18.94 15.88 15 8828 21949 110558507
Asthenia 17.95 15.88 105 8738 688894 109891562
Labelled drug-food interaction medication error 17.91 15.88 4 8839 206 110580250
Therapeutic response changed 17.15 15.88 6 8837 1612 110578844
Ulcer 16.89 15.88 19 8824 43097 110537359
Delusional disorder, unspecified type 16.33 15.88 5 8838 886 110579570
Paradoxical drug reaction 16.24 15.88 10 8833 9807 110570649

FDA Adverse Event Reporting System (Pediatric)

None

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 MoA N0000000181 Angiotensin-converting Enzyme Inhibitors
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:35674 antihypertensive agent
CHEBI has role CHEBI:50266 prodrug

Related Drugs by ATC class:

C09AA ACE inhibitors, plain 15 drugs
benazeprilcaptoprilcilazaprildelaprilenalaprilimidaprillisinoprilmoexiprilperindoprilquinaprilramiprilspirapril show all 15 →
C09BA ACE inhibitors and diuretics 11 drugs
benazeprilcaptoprilcilazaprildelaprilenalaprillisinoprilmoexiprilperindoprilquinaprilramiprilzofenopril

Drug Use | Suggest Off label Use Form| |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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
D00622 KEGG_DRUG
88889-14-9 SECONDARY_CAS_RN
4020186 VANDF
4020531 VANDF
C0118168 UMLSCUI
CHEBI:5163 CHEBI
KS8 PDB_CHEM_ID
CHEMBL3039598 ChEMBL_ID
CHEMBL3039596 ChEMBL_ID
D017328 MESH_DESCRIPTOR_UI
DB00492 DRUGBANK_ID
6456 IUPHAR_LIGAND_ID
5833 INN_ID
R43D2573WO UNII
9601226 PUBCHEM_CID
DB14207 DRUGBANK_ID
1546393 RXNORM
4766 MMSL
47869 MMSL
d00242 MMSL
003594 NDDF
004501 NDDF
108569005 SNOMEDCT_US
108570006 SNOMEDCT_US
372510000 SNOMEDCT_US
C0075061 UMLSCUI
CHEMBL581 ChEMBL_ID
95399-71-6 SECONDARY_CAS_RN
62956 PUBCHEM_CID
6457 IUPHAR_LIGAND_ID
6555 INN_ID
C046965 MESH_SUPPLEMENTAL_RECORD_UI
S312EY6ZT8 UNII
CHEBI:116962 CHEBI
R43D2573WO INXIGHT DRUGS
S312EY6ZT8 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fosinopril sodium Human Prescription Drug Label 1 43353-870 TABLET 40 mg ORAL ANDA 21 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 43547-386 TABLET 10 mg ORAL ANDA 24 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 43547-387 TABLET 20 mg ORAL ANDA 24 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 43547-388 TABLET 40 mg ORAL ANDA 24 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-2500 TABLET 40 mg ORAL ANDA 18 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-2977 TABLET 10 mg ORAL ANDA 18 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-3780 TABLET 10 mg ORAL ANDA 24 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 50090-4743 TABLET 40 mg ORAL ANDA 24 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50436-0274 TABLET 40 mg ORAL ANDA 22 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50436-3138 TABLET 20 mg ORAL ANDA 22 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 53217-277 TABLET 10 mg ORAL ANDA 21 sections
Fosinopril sodium HUMAN PRESCRIPTION DRUG LABEL 1 53217-278 TABLET 40 mg ORAL ANDA 21 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-5055 TABLET 20 mg ORAL ANDA 25 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-5064 TABLET 10 mg ORAL ANDA 25 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 54868-5182 TABLET 40 mg ORAL ANDA 25 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 54868-5346 TABLET 10 mg ORAL ANDA 26 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 54868-5469 TABLET 20 mg ORAL ANDA 26 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 62135-041 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 62135-041 TABLET 10 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 62135-042 TABLET 20 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 62135-042 TABLET 20 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 62135-043 TABLET 40 mg ORAL ANDA 12 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 62135-043 TABLET 40 mg ORAL ANDA 12 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 63304-403 TABLET 10 mg ORAL ANDA 23 sections
Fosinopril Sodium and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 63304-404 TABLET 20 mg ORAL ANDA 23 sections
Fosinopril Sodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-5279 TABLET 10 mg ORAL ANDA 23 sections
Fosinopril Sodium and Hydrochlorothiazide Human Prescription Drug Label 2 65862-308 TABLET 10 mg ORAL ANDA 22 sections
Fosinopril Sodium and Hydrochlorothiazide Human Prescription Drug Label 2 65862-309 TABLET 20 mg ORAL ANDA 22 sections
Fosinopril Sodium Human Prescription Drug Label 1 65862-471 TABLET 10 mg ORAL ANDA 21 sections
Fosinopril Sodium Human Prescription Drug Label 1 65862-472 TABLET 20 mg ORAL ANDA 21 sections