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

Stem definition	Drug id	CAS RN
antihyperlipidaemic substances, HMG CoA reductase inhibitors	257	134523-00-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: CI-981 CI981 atorvastatin calcium hydrate atorvastatin calcium anhydrous atorvastatin atorvastatin acid cardyl atorvastatin calcium atorvastatin calcium trihydrate	A pyrrole and heptanoic acid derivative, HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITOR (statin), and ANTICHOLESTEREMIC AGENT that is used to reduce serum levels of LDL-CHOLESTEROL; APOLIPOPROTEIN B; and TRIGLYCERIDES. It is used to increase serum levels of HDL-CHOLESTEROL in the treatment of HYPERLIPIDEMIAS, and for the prevention of CARDIOVASCULAR DISEASES in patients with multiple risk factors. Molecular weight: 558.65 Formula: C33H35FN2O5 CLOGP: 4.46 LIPINSKI: 1 HAC: 7 HDO: 4 TPSA: 111.79 ALOGS: -5.95 ROTB: 12 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

CI-981
CI981
atorvastatin calcium hydrate
atorvastatin calcium anhydrous
atorvastatin
atorvastatin acid
cardyl
atorvastatin calcium
atorvastatin calcium trihydrate

A pyrrole and heptanoic acid derivative, HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITOR (statin), and ANTICHOLESTEREMIC AGENT that is used to reduce serum levels of LDL-CHOLESTEROL; APOLIPOPROTEIN B; and TRIGLYCERIDES. It is used to increase serum levels of HDL-CHOLESTEROL in the treatment of HYPERLIPIDEMIAS, and for the prevention of CARDIOVASCULAR DISEASES in patients with multiple risk factors.

Molecular weight: 558.65
Formula: C33H35FN2O5
CLOGP: 4.46
LIPINSKI: 1
HAC: 7
HDO: 4
TPSA: 111.79
ALOGS: -5.95
ROTB: 12

Status: OFP

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

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.05 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Hosey CM, Chan R, Benet LZ
EoM (Fraction excreted unchanged in urine)	1 %	Hosey CM, Chan R, Benet LZ
BA (Bioavailability)	0.12 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
S (Water solubility)	0.02 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 17, 1996	FDA	PFIZER

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
Myalgia	1385.36	9.79	2852	378689	143677	62963804
Maternal exposure during pregnancy	1078.99	9.79	60	381481	220002	62887479
Pemphigus	1039.42	9.79	12	381529	183714	62923767
Rhabdomyolysis	964.73	9.79	1254	380287	42697	63064784
Immune-mediated myositis	884.26	9.79	325	381216	1018	63106463
Glossodynia	826.14	9.79	66	381475	178810	62928671
Systemic lupus erythematosus	818.87	9.79	136	381405	208782	62898699
Hand deformity	818.61	9.79	32	381509	159425	62948056
Contraindicated product administered	704.53	9.79	216	381325	217432	62890049
Drug ineffective	690.84	9.79	3591	377950	1041174	62066307

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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
Myalgia	1303.80	11.69	2785	363856	81325	34508965
Immune-mediated myositis	1288.55	11.69	563	366078	1520	34588770
Rhabdomyolysis	838.54	11.69	2061	364580	66102	34524188
Drug abuse	579.15	11.69	161	366480	98935	34491355
Off label use	545.35	11.69	2409	364232	417115	34173175
Toxicity to various agents	532.14	11.69	799	365842	199563	34390727
Blood creatine phosphokinase increased	514.26	11.69	1321	365320	43536	34546754
Febrile neutropenia	419.92	11.69	490	366151	136359	34453931
Myopathy	415.54	11.69	558	366083	10996	34579294
Myocardial infarction	358.57	11.69	2335	364306	118750	34471540

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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
Immune-mediated myositis	2173.19	10.45	872	629441	2595	79111480
Myalgia	1933.71	10.45	4425	625888	181216	78932859
Rhabdomyolysis	1810.86	10.45	3063	627250	100068	79014007
Drug ineffective	939.75	10.45	4883	625430	1076030	78038045
Acute kidney injury	938.63	10.45	7166	623147	512238	78601837
Maternal exposure during pregnancy	888.92	10.45	46	630267	136492	78977583
Myopathy	817.06	10.45	908	629405	19655	79094420
Blood creatine phosphokinase increased	801.25	10.45	1676	628637	64414	79049661
Myocardial infarction	791.71	10.45	3216	627097	180913	78933162
Off label use	759.53	10.45	4148	626165	903067	78211008

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C10AA05	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN HMG CoA reductase inhibitors
ATC	C10BA05	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BA08	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BX03	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX06	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX08	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX11	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX12	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX15	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX18	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs

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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
Hypercholesterolemia	indication	13644009
Arteriosclerotic vascular disease	indication	72092001
Prinzmetal angina	indication	87343002
Angina pectoris	indication	194828000
Cerebrovascular accident	indication	230690007
Familial hypercholesterolemia - homozygous	indication	238078005
Familial hypercholesterolemia - heterozygous	indication	238079002
Mixed hyperlipidemia	indication	267434003
Hypertriglyceridemia	indication	302870006
Familial type 3 hyperlipoproteinemia	indication	398796005	DOID:3145

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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	4.44	acidic
pKa2	11.82	acidic
pKa3	13.63	acidic

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
20MG/5ML	ATORVALIQ	CMP DEV LLC	N213260	Feb. 1, 2023	RX	SUSPENSION	ORAL	11654106	June 7, 2037	AS AN ADJUNCT TO DIET TO REDUCE LOW-DENSITY LIPOPROTEIN CHOLESTEROL IN ADULTS AND PEDIATRIC PATIENTS AGED 10 YEARS AND OLDER WITH HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA
20MG/5ML	ATORVALIQ	CMP DEV LLC	N213260	Feb. 1, 2023	RX	SUSPENSION	ORAL	11654106	June 7, 2037	AS AN ADJUNCT TO OTHER LOW-DENSITY LIPOPROTEIN CHOLESTEROL (LDL-C) LOWERING THERAPIES, OR ALONE IF SUCH TREATMENTS ARE UNAVAILABLE, TO REDUCE LDL-C IN ADULTS AND PEDIATRIC PATIENTS AGED 10 YEARS AND OLDER WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA

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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])	Bioact source	MoA source
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme	P04035	HMDH_HUMAN	INHIBITOR	IC50	8	WOMBAT-PK	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	5.29	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.37	CHEMBL
Histone deacetylase 2	Enzyme	Q92769	HDAC2_HUMAN		IC50	4.65	CHEMBL
Histone deacetylase 1	Enzyme	Q13547	HDAC1_HUMAN		IC50	4.93	CHEMBL
Histone deacetylase 6	Enzyme	Q9UBN7	HDAC6_HUMAN		IC50	4.84	CHEMBL
Nuclear receptor subfamily 1 group I member 3	Nuclear hormone receptor	Q14994	NR1I3_HUMAN				WOMBAT-PK
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme		HMDH_RAT		IC50	8.42	CHEMBL
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme		HMDH_PIG		IC50	4.49	CHEMBL

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External reference:

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ID	Source
117	PDB_CHEM_ID
006321	NDDF
006322	NDDF
108600003	SNOMEDCT_US
108601004	SNOMEDCT_US
1268949007	SNOMEDCT_US
1297766	RXNORM
134523-03-8	SECONDARY_CAS_RN
186242	MMSL
2949	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2150	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2150	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2150	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2150	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2160	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2160	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2160	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2160	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2170	TABLET, FILM COATED	20 mg	ORAL	NDA	32 sections
Caduet	HUMAN PRESCRIPTION DRUG LABEL	2	0069-2170	TABLET, FILM COATED	20 mg	ORAL	NDA	32 sections

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