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

Stem definition	Drug id	CAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic)	1610	114798-26-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: losartan allisartan lortaan losartan potassium losartan monopotassium losartan monopotassium salt	An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II. Molecular weight: 422.92 Formula: C22H23ClN6O CLOGP: 3.85 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 92.51 ALOGS: -4.97 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

losartan
allisartan
lortaan
losartan potassium
losartan monopotassium
losartan monopotassium salt

An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.

Molecular weight: 422.92
Formula: C22H23ClN6O
CLOGP: 3.85
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 92.51
ALOGS: -4.97
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
50	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	8.20 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	35 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	3.95 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	12 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	1.80 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.37 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.05 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
April 14, 1995	FDA	MERCK SHARP DOHME

FDA Adverse Event Reporting System (Female)

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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
Pemphigus	460.02	9.62	4	166732	183722	63138564
Synovitis	377.68	9.62	30	166706	186888	63135398
Systemic lupus erythematosus	365.59	9.62	56	166680	208862	63113424
Hand deformity	364.64	9.62	12	166724	159445	63162841
Maternal exposure during pregnancy	328.82	9.62	86	166650	219976	63102310
Contraindicated product administered	299.69	9.62	99	166637	217549	63104737
Glossodynia	284.75	9.62	61	166675	178815	63143471
Wound	259.19	9.62	56	166680	163207	63159079
Drug intolerance	244.66	9.62	270	166466	308391	63013895
Infusion related reaction	242.23	9.62	175	166561	245346	63076940

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FDA Adverse Event Reporting System (Male)

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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	195.75	10.28	383	106137	36991	34813420
Drug abuse	189.73	10.28	36	106484	99060	34751351
Febrile neutropenia	119.18	10.28	145	106375	136704	34713707
Toxicity to various agents	115.14	10.28	277	106243	200085	34650326
Cardiospasm	111.31	10.28	66	106454	1522	34848889
Dizziness	105.12	10.28	1072	105448	217449	34632962
Off label use	103.53	10.28	802	105718	418722	34431689
Neutropenia	97.12	10.28	208	106312	156570	34693841
Palmoplantar keratoderma	96.37	10.28	65	106455	1888	34848523
Myocardial infarction	95.53	10.28	664	105856	120421	34729990

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FDA Adverse Event Reporting System (Geriatric)

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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
Synovitis	296.79	9.58	34	219819	150700	79373835
Cardiac failure congestive	263.56	9.58	928	218925	141474	79383061
Drug abuse	258.32	9.58	65	219788	162626	79361909
Maternal exposure during pregnancy	249.27	9.58	39	219814	136499	79388036
Drug ineffective	244.77	9.58	1863	217990	1079050	78445485
Hand deformity	239.82	9.58	11	219842	103908	79420627
Angioedema	229.45	9.58	589	219264	75446	79449089
Myocardial infarction	227.29	9.58	1058	218795	183071	79341464
Off label use	214.48	9.58	1544	218309	905671	78618864
Pemphigus	213.22	9.58	16	219837	99566	79424969

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C09CA01	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN Angiotensin II receptor blockers (ARBs), plain
ATC	C09DA01	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and diuretics
ATC	C09DB06	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and calcium channel blockers
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:51451	ERA
CHEBI has role	CHEBI:61016	angiotensin receptor antagonists
FDA EPC	N0000175561	Angiotensin 2 Receptor Blocker
FDA MoA	N0000000070	Angiotensin 2 Receptor Antagonists
MeSH PA	D047228	Angiotensin II Type 1 Receptor Blockers

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

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Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Diabetic renal disease	indication	127013003
Hypertensive urgency	indication	443482000
Hypertension with Left Ventricular Hypertrophy	indication
Chronic heart failure	off-label use	48447003
Atrial fibrillation	off-label use	49436004	DOID:0060224
Diastolic heart failure	off-label use	418304008	DOID:9775
Nondiabetic Proteinuric Nephropathy	off-label use
Anuria	contraindication	2472002	DOID:2983
Hypercholesterolemia	contraindication	13644009

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.5	acidic
pKa2	13.19	acidic
pKa3	3.89	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Type-1 angiotensin II receptor	GPCR	P30556	AGTR1_HUMAN	ANTAGONIST	IC50	9.48	CHEMBL	CHEMBL
Angiotensin-converting enzyme	Enzyme	P12821	ACE_HUMAN		IC50	7.72	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.46	CHEMBL
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	5.54	DRUG MATRIX
Thromboxane A2 receptor	GPCR	P21731	TA2R_HUMAN		IC50	4.70	CHEMBL
Type-2 angiotensin II receptor	GPCR	P50052	AGTR2_HUMAN		IC50	5	CHEMBL
Phosphodiesterase 3	Enzyme	Q13370 Q14432	PDE3B_HUMAN PDE3A_HUMAN		IC50	4.89	CHEMBL
Phosphodiesterase 4	Enzyme	P27815 Q07343 Q08493 Q08499	PDE4A_HUMAN PDE4B_HUMAN PDE4C_HUMAN PDE4D_HUMAN		IC50	4.59	CHEMBL
Angiotensin II receptor	GPCR	P30556 P50052	AGTR1_HUMAN AGTR2_HUMAN		Kd	8.43	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		Km	3.50	WOMBAT-PK

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External reference:

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ID	Source
LSN	PDB_CHEM_ID
004991	NDDF
004992	NDDF
108582002	SNOMEDCT_US
124750-99-8	SECONDARY_CAS_RN
172424	MMSL
203160	RXNORM
373567002	SNOMEDCT_US
3961	PUBCHEM_CID
4020913	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0123	TABLET	25 mg	ORAL	ANDA	26 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0124	TABLET	50 mg	ORAL	ANDA	26 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0125	TABLET	100 mg	ORAL	ANDA	26 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7958	TABLET, FILM COATED	25 mg	ORAL	ANDA	28 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7959	TABLET, FILM COATED	50 mg	ORAL	ANDA	28 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7960	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7047	TABLET, FILM COATED	25 mg	ORAL	ANDA	27 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7047	TABLET, FILM COATED	25 mg	ORAL	ANDA	27 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7048	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections
Losartan Potassium	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7048	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections

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