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

Stem definition	Drug id	CAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic)	475	145040-37-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: candesartan cilexetil TCV-116 TCV 116	a nonpeptide angiotensin II receptor antagonist Molecular weight: 610.67 Formula: C33H34N6O6 CLOGP: 7.08 LIPINSKI: 3 HAC: 12 HDO: 1 TPSA: 143.34 ALOGS: -5.48 ROTB: 13 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

candesartan cilexetil
TCV-116
TCV 116

a nonpeptide angiotensin II receptor antagonist

Molecular weight: 610.67
Formula: C33H34N6O6
CLOGP: 7.08
LIPINSKI: 3
HAC: 12
HDO: 1
TPSA: 143.34
ALOGS: -5.48
ROTB: 13

Status: OFP

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

Drug dosage:

Dose	Unit	Route
8	mg	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.61 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	0.42 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
June 4, 1998	FDA	ASTRAZENECA
March 12, 1999	PMDA	Takeda Pharmaceutical Company Limited

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
Acute kidney injury	489.30	10.20	1076	82854	262339	63142753
Hyponatraemia	361.50	10.20	580	83350	111320	63293772
Pemphigus	201.30	10.20	10	83920	183716	63221376
General physical health deterioration	199.99	10.20	653	83277	200749	63204343
Drug ineffective	192.14	10.20	724	83206	1044041	62361051
Synovitis	184.91	10.20	17	83913	186901	63218191
Hyperkalaemia	177.65	10.20	283	83647	53920	63351172
Glossodynia	167.35	10.20	20	83910	178856	63226236
Arthropathy	160.60	10.20	55	83875	234737	63170355
Hand deformity	151.22	10.20	17	83913	159440	63245652

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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
General physical health deterioration	229.43	10.82	625	62312	127644	34766350
Death	212.64	10.82	243	62694	397806	34496188
Product monitoring error	174.77	10.82	105	62832	4276	34889718
Hyperkalaemia	157.14	10.82	370	62567	69019	34824975
Acute kidney injury	155.71	10.82	1009	61928	303979	34590015
Completed suicide	141.17	10.82	9	62928	98159	34795835
Cardiospasm	140.94	10.82	65	62872	1523	34892471
Toxicity to various agents	135.57	10.82	98	62839	200264	34693730
Palmoplantar keratoderma	128.15	10.82	65	62872	1888	34892106
Tension headache	121.58	10.82	73	62864	2969	34891025

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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
Acute kidney injury	541.46	9.76	1970	128448	517434	79096536
General physical health deterioration	421.07	9.76	1192	129226	274046	79339924
Completed suicide	319.51	9.76	21	130397	245746	79368224
Product monitoring error	304.99	9.76	187	130231	8719	79605251
Hyperkalaemia	296.35	9.76	608	129810	113790	79500180
Cardiospasm	239.15	9.76	114	130304	3187	79610783
Haematochezia	229.51	9.76	468	129950	87177	79526793
Death	227.43	9.76	360	130058	566154	79047816
Palmoplantar keratoderma	226.33	9.76	114	130304	3602	79610368
Product prescribing error	223.70	9.76	319	130099	44494	79569476

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C09CA06	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN Angiotensin II receptor blockers (ARBs), plain
ATC	C09DA06	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and diuretics
ATC	C09DB07	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and calcium channel blockers
ATC	C09DX06	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs), other combinations
ATC	C10BX19	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
FDA EPC	N0000175561	Angiotensin 2 Receptor Blocker
FDA MoA	N0000000070	Angiotensin 2 Receptor Antagonists
MeSH PA	D047228	Angiotensin II Type 1 Receptor Blockers
MeSH PA	D057911	Angiotensin Receptor Antagonists
MeSH PA	D000959	Antihypertensive 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
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
Diastolic heart failure	off-label use	418304008	DOID:9775
Nondiabetic Proteinuric Nephropathy	off-label use
Anuria	contraindication	2472002	DOID:2983
Hypercholesterolemia	contraindication	13644009
Hyperkalemia	contraindication	14140009
Secondary angle-closure glaucoma	contraindication	21571006

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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	4.25	acidic
pKa2	3.2	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	9.16	CHEMBL	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.52	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	5.76	CHEMBL
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		Ki	5.49	CHEMBL
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	6.16	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.30	CHEMBL
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	5.52	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		IC50	5.48	CHEMBL
Peroxisome proliferator-activated receptor gamma	Nuclear hormone receptor	P37231	PPARG_HUMAN		EC50	5.38	CHEMBL
Receptor tyrosine-protein kinase erbB-2	Kinase	P04626	ERBB2_HUMAN		IC50	5.23	CHEMBL

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External reference:

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ID	Source
007275	NDDF
007276	NDDF
108587008	SNOMEDCT_US
135481	RXNORM
139481-59-7	SECONDARY_CAS_RN
188909	MMSL
2540	PUBCHEM_CID
2541	PUBCHEM_CID
372512008	SNOMEDCT_US
386878000	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Candesartan	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7034	TABLET	32 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-114	TABLET	4 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-114	TABLET	4 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-114	TABLET	4 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-115	TABLET	8 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-115	TABLET	8 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-115	TABLET	8 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-116	TABLET	16 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-116	TABLET	16 mg	ORAL	ANDA	28 sections
Candesartan	Human Prescription Drug Label	1	33342-116	TABLET	16 mg	ORAL	ANDA	28 sections

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