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

Stem definition	Drug id	CAS RN
endothelin receptor antagonists	4337	177036-94-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: LU208075 LU 208075 ambrisentan letairis volibris	an endothelin receptor antagonist that is selective for the endothelin type-A (ETA) receptor Molecular weight: 378.43 Formula: C22H22N2O4 CLOGP: 3.35 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 81.54 ALOGS: -3.88 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

LU208075
LU 208075
ambrisentan
letairis
volibris

an endothelin receptor antagonist that is selective for the endothelin type-A (ETA) receptor

Molecular weight: 378.43
Formula: C22H22N2O4
CLOGP: 3.35
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 81.54
ALOGS: -3.88
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
7.50	mg	O

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.38 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.06 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

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Date	Agency	Company
June 15, 2007	FDA	GILEAD
June 20, 2019	EMA	MYLAN SAS
March 23, 2021	PMDA	GlaxoSmithKline K.K.

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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
Dyspnoea	4202.19	17.71	5321	101530	655992	62726179
Fluid retention	2463.18	17.71	1425	105426	58261	63323910
Death	2095.57	17.71	2844	104007	371537	63010634
Nasal congestion	1673.54	17.71	1156	105695	64504	63317667
Headache	1600.72	17.71	3370	103481	629871	62752300
Pain in jaw	1579.90	17.71	957	105894	42539	63339632
Pulmonary arterial hypertension	1298.38	17.71	672	106179	21905	63360266
Oedema	1196.40	17.71	1119	105732	96503	63285668
Right ventricular failure	1035.57	17.71	528	106323	16660	63365511
Unevaluable event	986.93	17.71	763	106088	50623	63331548

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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
Dyspnoea	1336.72	22.89	1642	29312	375140	34550837
Fluid retention	979.95	22.89	477	30477	26410	34899567
Death	764.00	22.89	1300	29654	396749	34529228
Headache	595.43	22.89	805	30149	199830	34726147
Oedema	563.24	22.89	402	30552	45339	34880638
Nasal congestion	525.22	22.89	299	30655	22758	34903219
Pulmonary arterial hypertension	518.21	22.89	218	30736	8521	34917456
Pain in jaw	506.70	22.89	242	30712	12798	34913179
Right ventricular failure	403.22	22.89	183	30771	8601	34917376
Pulmonary hypertension	396.62	22.89	241	30713	20683	34905294

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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
Dyspnoea	4511.65	18.80	5773	107797	851252	78779566
Fluid retention	2907.46	18.80	1583	111987	68226	79562592
Headache	2177.92	18.80	3561	110009	650211	78980607
Nasal congestion	2007.61	18.80	1288	112282	75264	79555554
Pain in jaw	1924.04	18.80	1048	112522	45103	79585715
Death	1854.10	18.80	3064	110506	563450	79067368
Oedema	1518.25	18.80	1300	112270	118280	79512538
Pulmonary arterial hypertension	1422.41	18.80	729	112841	27637	79603181
Unevaluable event	1085.81	18.80	780	112790	54805	79576013
Oedema peripheral	1077.03	18.80	1547	112023	250741	79380077

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	C02KX02	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES OTHER ANTIHYPERTENSIVES Antihypertensives for pulmonary arterial hypertension
ATC	C02KX52	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES OTHER ANTIHYPERTENSIVES Antihypertensives for pulmonary arterial hypertension
FDA EPC	N0000175581	Endothelin Receptor Antagonist
FDA MoA	N0000175364	Endothelin Receptor Antagonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents

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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
Pulmonary arterial hypertension	indication	11399002
Body fluid retention	contraindication	43498006
Chronic heart failure	contraindication	48447003
Oligozoospermia	contraindication	88311004
Pulmonary veno-occlusive disease	contraindication	89420002	DOID:5453
Liver function tests abnormal	contraindication	166603001
Edema	contraindication	267038008
Anemia	contraindication	271737000	DOID:2355
Pregnancy, function	contraindication	289908002
Breastfeeding (mother)	contraindication	413712001

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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	3.3	acidic
pKa2	2.68	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG	LETAIRIS	GILEAD	N022081	June 15, 2007	RX	TABLET	ORAL	8377933	Dec. 11, 2027	FOR THE TREATMENT OF PULMONARY HYPERTENSION (PAH) IN COMBINATION WITH TADALAFIL
10MG	LETAIRIS	GILEAD	N022081	June 15, 2007	RX	TABLET	ORAL	9474752	Dec. 11, 2027	FOR THE TREATMENT OF PULMONARY HYPERTENSION (PAH) IN COMBINATION WITH TADALAFIL
10MG	LETAIRIS	GILEAD	N022081	June 15, 2007	RX	TABLET	ORAL	9549926	Oct. 14, 2031	FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) IN COMBINATION WITH TADALAFIL, WHEREIN THE WEIGHT RATIO OF AMBRISENTAN TO TADALAFIL IS ABOUT 1:2 TO ABOUT 1:3
5MG	LETAIRIS	GILEAD	N022081	June 15, 2007	RX	TABLET	ORAL	8377933	Dec. 11, 2027	FOR THE TREATMENT OF PULMONARY HYPERTENSION (PAH) IN COMBINATION WITH TADALAFIL
5MG	LETAIRIS	GILEAD	N022081	June 15, 2007	RX	TABLET	ORAL	9474752	Dec. 11, 2027	FOR THE TREATMENT OF PULMONARY HYPERTENSION (PAH) IN COMBINATION WITH TADALAFIL
5MG	LETAIRIS	GILEAD	N022081	June 15, 2007	RX	TABLET	ORAL	9549926	Oct. 14, 2031	FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) IN COMBINATION WITH TADALAFIL, WHEREIN THE WEIGHT RATIO OF AMBRISENTAN TO TADALAFIL IS ABOUT 1:2 TO ABOUT 1:3

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Endothelin-1 receptor	GPCR	P25101	EDNRA_HUMAN	ANTAGONIST	Ki	9.65		WOMBAT-PK	DRUG LABEL
Endothelin B receptor	GPCR	P24530	EDNRB_HUMAN	ANTAGONIST	Ki	6.98		WOMBAT-PK

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External reference:

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ID	Source
012216	NDDF
111024	MMSL
23940	MMSL
313847	MMSL
358274	RXNORM
3951	IUPHAR_LIGAND_ID
4026238	VUID
4026238	VANDF
427735003	SNOMEDCT_US
428159003	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ambrisentan	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4270	TABLET, FILM COATED	5 mg	ORAL	ANDA	29 sections
Ambrisentan	HUMAN PRESCRIPTION DRUG LABEL	1	0378-4271	TABLET, FILM COATED	10 mg	ORAL	ANDA	29 sections
Ambrisentan	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2405	TABLET, FILM COATED	5 mg	ORAL	ANDA	27 sections
Ambrisentan	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2406	TABLET, FILM COATED	10 mg	ORAL	ANDA	27 sections
AMBRISENTAN	HUMAN PRESCRIPTION DRUG LABEL	1	42794-051	TABLET, FILM COATED	5 mg	ORAL	ANDA	19 sections
AMBRISENTAN	HUMAN PRESCRIPTION DRUG LABEL	1	42794-051	TABLET, FILM COATED	5 mg	ORAL	ANDA	19 sections
AMBRISENTAN	HUMAN PRESCRIPTION DRUG LABEL	1	42794-052	TABLET, FILM COATED	10 mg	ORAL	ANDA	19 sections
AMBRISENTAN	HUMAN PRESCRIPTION DRUG LABEL	1	42794-052	TABLET, FILM COATED	10 mg	ORAL	ANDA	19 sections
ambrisentan	Human Prescription Drug Label	1	47335-236	TABLET, FILM COATED	5 mg	ORAL	ANDA	30 sections
ambrisentan	Human Prescription Drug Label	1	47335-237	TABLET, FILM COATED	10 mg	ORAL	ANDA	30 sections

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