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

Stem definition	Drug id	CAS RN
angiotensin-converting enzyme inhibitors	1245	98048-97-6

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
15	mg	O

ADMET properties:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
May 16, 1991	FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure congestive	75.45	17.67	56	4060	92377	63392529
Myocardial infarction	63.05	17.67	52	4064	99841	63385065
Diverticular perforation	60.78	17.67	18	4098	3524	63481382
Cerebrovascular accident	42.20	17.67	43	4073	107981	63376925
International normalised ratio increased	30.99	17.67	25	4091	46400	63438506
Steatorrhoea	30.68	17.67	7	4109	492	63484414
Hypertensive crisis	29.53	17.67	16	4100	15270	63469636
Angioedema	28.21	17.67	24	4092	47941	63436965
Body temperature decreased	27.83	17.67	17	4099	20302	63464604
Orthostatic hypotension	27.43	17.67	21	4095	36139	63448767
Skin reaction	27.18	17.67	15	4101	14834	63470072
Diabetes mellitus inadequate control	26.92	17.67	15	4101	15111	63469795
Swollen tongue	25.94	17.67	20	4096	34780	63450126
Labelled drug-food interaction medication error	25.21	17.67	5	4111	179	63484727
Muscle haemorrhage	25.21	17.67	9	4107	3170	63481736
Intercepted medication error	24.06	17.67	6	4110	616	63484290
Nephropathy	22.34	17.67	10	4106	6331	63478575
Hyperkalaemia	21.91	17.67	22	4094	54181	63430725
Renal failure	20.16	17.67	31	4085	117621	63367285
Psoriasis	17.92	17.67	25	4091	86932	63397974
Lacunar infarction	17.68	17.67	7	4109	3273	63481633

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Angioedema	166.76	18.25	89	4946	37285	34914611
Bradycardia	103.36	18.25	86	4949	75332	34876564
Acute kidney injury	81.79	18.25	152	4883	304836	34647060
Cardiac failure congestive	60.56	18.25	67	4968	83203	34868693
Hyperkalaemia	59.59	18.25	61	4974	69328	34882568
Hypoglycaemia	58.08	18.25	54	4981	54586	34897310
Myocardial infarction	53.65	18.25	76	4959	121009	34830887
Treatment noncompliance	44.65	18.25	35	5000	28065	34923831
Rhabdomyolysis	38.14	18.25	48	4987	68115	34883781
Coronary artery disease	37.03	18.25	40	4995	48265	34903631
Acidosis	29.90	18.25	19	5016	10926	34940970
Schizophrenia	28.67	18.25	17	5018	8649	34943247
Blood urea increased	28.42	18.25	28	5007	30336	34921560
Hyperparathyroidism	26.58	18.25	9	5026	1215	34950681
Hyperlactacidaemia	24.99	18.25	11	5024	3005	34948891
Swollen tongue	24.95	18.25	19	5016	14586	34937310
End stage renal disease	23.26	18.25	15	5020	8846	34943050
Hypotension	22.92	18.25	77	4958	221572	34730324
Inappropriate affect	22.76	18.25	7	5028	696	34951200
Metabolic acidosis	21.66	18.25	29	5006	43651	34908245
Swelling face	21.05	18.25	21	5014	23084	34928812
Cerebrovascular accident	18.56	18.25	39	4996	84772	34867124
Off label use	18.48	18.25	20	5015	419504	34532392

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Angioedema	163.59	15.25	100	8066	75935	79660287
Cardiac failure congestive	117.37	15.25	105	8061	142297	79593925
Myocardial infarction	116.02	15.25	117	8049	184012	79552210
Bradycardia	96.25	15.25	92	8074	135465	79600757
Acute kidney injury	93.63	15.25	180	7986	519224	79216998
Hyperkalaemia	81.86	15.25	78	8088	114320	79621902
Cerebrovascular accident	57.44	15.25	75	8091	155217	79581005
Coronary artery disease	55.28	15.25	49	8117	65425	79670797
Hypoglycaemia	48.79	15.25	56	8110	101538	79634684
Rhabdomyolysis	46.44	15.25	55	8111	103076	79633146
Diverticular perforation	43.74	15.25	18	8148	5875	79730347
Treatment noncompliance	41.90	15.25	38	8128	52230	79683992
Orthostatic hypotension	34.01	15.25	35	8131	56129	79680093
Renal failure	32.80	15.25	67	8099	200901	79535321
International normalised ratio increased	29.87	15.25	40	8126	84681	79651541
Acidosis	25.59	15.25	19	8147	19743	79716479
Schizophrenia	24.97	15.25	17	8149	15423	79720799
Faeces discoloured	24.97	15.25	22	8144	29105	79707117
End stage renal disease	23.52	15.25	15	8151	12205	79724017
Steatorrhoea	23.25	15.25	7	8159	914	79735308
Body temperature decreased	23.11	15.25	22	8144	32123	79704099
Hyperlactacidaemia	22.08	15.25	11	8155	5584	79730638
Swollen tongue	21.32	15.25	24	8142	42546	79693676
Drug ineffective	21.18	15.25	50	8116	1080863	78655359
Hyperparathyroidism	21.08	15.25	9	8157	3215	79733007
Hypotension	21.04	15.25	95	8071	440222	79296000
Skin reaction	19.81	15.25	15	8151	16053	79720169
Inappropriate affect	19.73	15.25	7	8159	1529	79734693
Blood urea increased	18.68	15.25	24	8142	48766	79687456
Behaviour disorder	18.04	15.25	10	8156	6303	79729919
Labelled drug-food interaction medication error	17.72	15.25	4	8162	168	79736054
Blood creatinine increased	16.77	15.25	44	8122	155013	79581209
Acute myocardial infarction	16.67	15.25	29	8137	77007	79659215
Syncope	16.52	15.25	48	8118	179401	79556821
Off label use	15.42	15.25	45	8121	907170	78829052

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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
CHEBI has role	CHEBI:35457	ACE inhibitor
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:50266	Prodrugs
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

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	3.98	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Angiotensin-converting enzyme	Enzyme	P12821	ACE_HUMAN	INHIBITOR	IC50	9		CHEMBL	CHEMBL
Angiotensin-converting enzyme	Enzyme		ACE_RABIT		Ki	8.82		CHEMBL

External reference:

ID	Source
4020531	VUID
N0000148247	NUI
D00622	KEGG_DRUG
88889-14-9	SECONDARY_CAS_RN
4020186	VANDF
4020531	VANDF
C0118168	UMLSCUI
CHEBI:5163	CHEBI
CHEBI:116962	CHEBI
KS8	PDB_CHEM_ID
CHEMBL3039598	ChEMBL_ID
CHEMBL3039596	ChEMBL_ID
D017328	MESH_DESCRIPTOR_UI
DB00492	DRUGBANK_ID
6456	IUPHAR_LIGAND_ID
C046965	MESH_SUPPLEMENTAL_RECORD_UI
5833	INN_ID
R43D2573WO	UNII
55891	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
6555	INN_ID
95399-71-6	SECONDARY_CAS_RN
62956	PUBCHEM_CID
6457	IUPHAR_LIGAND_ID
S312EY6ZT8	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Fosinopril Sodium	Human Prescription Drug Label	1	16571-770	TABLET	10 mg	ORAL	ANDA	21 sections
Fosinopril Sodium	Human Prescription Drug Label	1	16571-771	TABLET	20 mg	ORAL	ANDA	21 sections
Fosinopril Sodium	Human Prescription Drug Label	1	16571-772	TABLET	40 mg	ORAL	ANDA	21 sections
Fosinopril Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	31722-200	TABLET	10 mg	ORAL	ANDA	23 sections
Fosinopril Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	31722-201	TABLET	20 mg	ORAL	ANDA	23 sections
Fosinopril Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	31722-202	TABLET	40 mg	ORAL	ANDA	23 sections
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	50090-2500	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	50268-327	TABLET	10 mg	ORAL	ANDA	24 sections
Fosinopril sodium	HUMAN PRESCRIPTION DRUG LABEL	1	50268-328	TABLET	20 mg	ORAL	ANDA	24 sections
Fosinopril sodium	HUMAN PRESCRIPTION DRUG LABEL	1	50268-329	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 and Hydrochlorothiazide	Human Prescription Drug Label	2	57237-026	TABLET	10 mg	ORAL	ANDA	21 sections
Fosinopril Sodium and Hydrochlorothiazide	Human Prescription Drug Label	2	57237-027	TABLET	20 mg	ORAL	ANDA	21 sections
Fosinopril Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	62135-041	TABLET	10 mg	ORAL	ANDA	12 sections