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

Stem definition	Drug id	CAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic)	4322	863031-21-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: TAK 491 edarbi azilsartan medoxomil azilsartan kamedoxomil	an angiotensin type 1 receptor blocker; receptor blocker Molecular weight: 568.54 Formula: C30H24N4O8 CLOGP: 5 LIPINSKI: 2 HAC: 12 HDO: 1 TPSA: 139.57 ALOGS: -4.91 ROTB: 10 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

TAK 491
edarbi
azilsartan medoxomil
azilsartan kamedoxomil

an angiotensin type 1 receptor blocker; receptor blocker

Molecular weight: 568.54
Formula: C30H24N4O8
CLOGP: 5
LIPINSKI: 2
HAC: 12
HDO: 1
TPSA: 139.57
ALOGS: -4.91
ROTB: 10

Status: ONP

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

Drug dosage:

Dose	Unit	Route
40	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company
Feb. 25, 2011	FDA	ARBOR PHARMS IRELAND
Dec. 7, 2011	EMA	Takeda Pharma A/S
Jan. 18, 2001	PMDA	TAKEDA PHARMACEUTICAL COMPANY LIMITED

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
Platelet count decreased	68.23	24.93	47	2408	116075	63370492
Hepatic function abnormal	62.78	24.93	30	2425	37112	63449455
Cerebral infarction	55.21	24.93	24	2431	23869	63462698
Renal impairment	54.79	24.93	37	2418	88318	63398249
Hyperkalaemia	36.71	24.93	24	2431	54179	63432388
Decreased appetite	35.54	24.93	46	2409	251006	63235561
Interstitial lung disease	33.81	24.93	24	2431	61884	63424683
Altered state of consciousness	32.61	24.93	17	2438	25213	63461354
Cardiac failure	30.09	24.93	26	2429	89116	63397451
Proteinuria	27.93	24.93	14	2441	19131	63467436
Palmar-plantar erythrodysaesthesia syndrome	25.50	24.93	14	2441	23001	63463566

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
Cerebral infarction	102.43	21.19	49	2951	27406	34926525
Hepatic function abnormal	93.44	21.19	54	2946	44309	34909622
Renal impairment	81.04	21.19	66	2934	94447	34859484
Interstitial lung disease	69.82	21.19	52	2948	65230	34888701
Fibrillary glomerulonephritis	51.65	21.19	8	2992	46	34953885
Proteinuria	42.68	21.19	24	2976	18618	34935313
Decreased appetite	37.89	21.19	58	2942	166334	34787597
Palmar-plantar erythrodysaesthesia syndrome	34.10	21.19	20	2980	16775	34937156
Nephrotic syndrome	33.29	21.19	15	2985	7288	34946643
Thalamus haemorrhage	32.93	21.19	9	2991	996	34952935
Pemphigoid	30.84	21.19	15	2985	8651	34945280
Altered state of consciousness	30.78	21.19	21	2979	22872	34931059
Hepatocellular carcinoma	29.77	21.19	14	2986	7495	34946436
Cardiac failure	28.43	21.19	37	2963	91211	34862720
Thrombotic cerebral infarction	25.33	21.19	6	2994	374	34953557
Anti-neutrophil cytoplasmic antibody positive vasculitis	24.41	21.19	7	2993	922	34953009
Hyperuricaemia	22.98	21.19	12	2988	8031	34945900
Liver disorder	21.98	21.19	20	2980	32977	34920954

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
Hepatic function abnormal	150.04	18.21	82	5579	73025	79665702
Cerebral infarction	142.55	18.21	68	5593	45608	79693119
Renal impairment	119.92	18.21	95	5566	157688	79581039
Interstitial lung disease	92.41	18.21	71	5590	112529	79626198
Proteinuria	65.32	18.21	36	5625	32466	79706261
Decreased appetite	63.42	18.21	98	5563	342320	79396407
Platelet count decreased	62.63	18.21	73	5588	194591	79544136
Altered state of consciousness	60.32	18.21	38	5623	43784	79694943
Cardiac failure	53.04	18.21	60	5601	154782	79583945
Thalamus haemorrhage	52.04	18.21	14	5647	1768	79736959
Fibrillary glomerulonephritis	51.92	18.21	8	5653	55	79738672
Palmar-plantar erythrodysaesthesia syndrome	48.80	18.21	30	5631	33104	79705623
Hyperkalaemia	43.77	18.21	47	5614	114351	79624376
Liver disorder	41.26	18.21	37	5624	72380	79666347
Malignant neoplasm progression	38.77	18.21	48	5613	135942	79602785
Hyperuricaemia	38.08	18.21	18	5643	11781	79726946
Pemphigoid	36.47	18.21	19	5642	15296	79723431
Aortic dissection	36.46	18.21	13	5648	4162	79734565
Nephrotic syndrome	35.92	18.21	17	5644	11157	79727570
Thrombotic cerebral infarction	34.31	18.21	8	5653	564	79738163
Sinus node dysfunction	31.96	18.21	14	5647	7687	79731040
Hepatocellular carcinoma	29.84	18.21	14	5647	9007	79729720
Blood pressure decreased	29.78	18.21	36	5625	99430	79639297
Renal disorder	29.02	18.21	24	5637	42081	79696646
Hypothyroidism	20.85	18.21	22	5639	52370	79686357
Shunt stenosis	18.74	18.21	6	5655	1385	79737342
Enterocolitis	18.50	18.21	12	5649	14500	79724227
Haemorrhagic cerebral infarction	18.38	18.21	6	5655	1473	79737254
Fulminant type 1 diabetes mellitus	18.37	18.21	6	5655	1477	79737250

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C09CA09	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN Angiotensin II receptor blockers (ARBs), plain
ATC	C09DA09	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and diuretics
FDA EPC	N0000175561	Angiotensin 2 Receptor Blocker
MeSH PA	D047228	Angiotensin II Type 1 Receptor Blockers
MeSH PA	D057911	Angiotensin Receptor Antagonists
FDA PE	N0000178477	Decreased Blood Pressure
FDA MoA	N0000180999	Angiotensin 2 Type 1 Receptor Antagonists
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:61016	angiotensin receptor antagonists

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

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Hypovolemia	contraindication	28560003
Low blood pressure	contraindication	45007003
Hyponatremia	contraindication	89627008
Impaired renal function disorder	contraindication	197663003
Pregnancy, function	contraindication	289908002
Renal artery stenosis	contraindication	302233006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.11	acidic
pKa2	3.02	Basic
pKa3	2.4	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 40MG MEDOXOMIL	EDARBI	AZURITY	N200796	Feb. 25, 2011	RX	TABLET	ORAL	7572920	Jan. 7, 2025	TREATMENT OF HYPERTENSION
EQ 80MG MEDOXOMIL	EDARBI	AZURITY	N200796	Feb. 25, 2011	RX	TABLET	ORAL	7572920	Jan. 7, 2025	TREATMENT OF HYPERTENSION
EQ 40MG MEDOXOMIL;12.5MG	EDARBYCLOR	AZURITY	N202331	Dec. 20, 2011	RX	TABLET	ORAL	7572920	Jan. 7, 2025	TREATMENT OF HYPERTENSION
EQ 40MG MEDOXOMIL;25MG	EDARBYCLOR	AZURITY	N202331	Dec. 20, 2011	RX	TABLET	ORAL	7572920	Jan. 7, 2025	TREATMENT OF HYPERTENSION
EQ 40MG MEDOXOMIL;12.5MG	EDARBYCLOR	AZURITY	N202331	Dec. 20, 2011	RX	TABLET	ORAL	9387249	July 1, 2031	TREATMENT OF HYPERTENSION
EQ 40MG MEDOXOMIL;25MG	EDARBYCLOR	AZURITY	N202331	Dec. 20, 2011	RX	TABLET	ORAL	9387249	July 1, 2031	TREATMENT OF HYPERTENSION

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
Type-1 angiotensin II receptor	GPCR	P30556	AGTR1_HUMAN	ANTAGONIST	IC50	8.13		IUPHAR	CHEMBL
Type-1 angiotensin II receptor	GPCR		AGTR1_BOVIN		IC50	6.38		CHEMBL

External reference:

ID	Source
D08067	KEGG_DRUG
863031-24-7	SECONDARY_CAS_RN
4030593	VANDF
4030594	VANDF
C2698291	UMLSCUI
CHEBI:68845	CHEBI
CHEBI:68850	CHEBI
CHEMBL2028661	ChEMBL_ID
CHEMBL2103795	ChEMBL_ID
DB08822	DRUGBANK_ID
C557413	MESH_SUPPLEMENTAL_RECORD_UI
C521273	MESH_SUPPLEMENTAL_RECORD_UI
6900	IUPHAR_LIGAND_ID
8874	INN_ID
LL0G25K7I2	UNII
135409642	PUBCHEM_CID
1091642	RXNORM
180314	MMSL
27787	MMSL
d07754	MMSL
013661	NDDF
013662	NDDF
448917007	SNOMEDCT_US
449042005	SNOMEDCT_US
449561004	SNOMEDCT_US
C1958569	UMLSCUI
CHEMBL57242	ChEMBL_ID
8724	INN_ID
147403-03-0	SECONDARY_CAS_RN
135415867	PUBCHEM_CID
6901	IUPHAR_LIGAND_ID
F9NUX55P23	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Edarbi	HUMAN PRESCRIPTION DRUG LABEL	1	60631-040	TABLET	40 mg	ORAL	NDA	32 sections
Edarbi	HUMAN PRESCRIPTION DRUG LABEL	1	60631-040	TABLET	40 mg	ORAL	NDA	32 sections
Edarbi	HUMAN PRESCRIPTION DRUG LABEL	1	60631-080	TABLET	80 mg	ORAL	NDA	32 sections
Edarbi	HUMAN PRESCRIPTION DRUG LABEL	1	60631-080	TABLET	80 mg	ORAL	NDA	32 sections
Edarbyclor	HUMAN PRESCRIPTION DRUG LABEL	2	60631-412	TABLET	40 mg	ORAL	NDA	32 sections
Edarbyclor	HUMAN PRESCRIPTION DRUG LABEL	2	60631-412	TABLET	40 mg	ORAL	NDA	32 sections
Edarbyclor	HUMAN PRESCRIPTION DRUG LABEL	2	60631-425	TABLET	40 mg	ORAL	NDA	32 sections
Edarbyclor	HUMAN PRESCRIPTION DRUG LABEL	2	60631-425	TABLET	40 mg	ORAL	NDA	32 sections