Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value
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:

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	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 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	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 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	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:

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
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

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C09BA ACE inhibitors and diuretics 11 drugs

benazepril captopril cilazapril delapril enalapril lisinopril moexipril perindopril quinapril ramipril zofenopril

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
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

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fosinopril 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: