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

Stem definition	Drug id	CAS RN
antihyperlipidaemic substances, HMG CoA reductase inhibitors	2406	287714-41-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: rosuvastatin rosuvastatin calcium crestor rosuvastatin zinc ZD4522	A HYDROXYMETHYLGLUTARYL-COA-REDUCTASE INHIBITOR, or statin, that reduces the plasma concentrations of LDL-CHOLESTEROL; APOLIPOPROTEIN B, and TRIGLYCERIDES while increasing HDL-CHOLESTEROL levels in patients with HYPERCHOLESTEROLEMIA and those at risk for CARDIOVASCULAR DISEASES. Molecular weight: 481.54 Formula: C22H28FN3O6S CLOGP: 1.90 LIPINSKI: 0 HAC: 9 HDO: 3 TPSA: 140.92 ALOGS: -3.74 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

rosuvastatin
rosuvastatin calcium
crestor
rosuvastatin zinc
ZD4522

A HYDROXYMETHYLGLUTARYL-COA-REDUCTASE INHIBITOR, or statin, that reduces the plasma concentrations of LDL-CHOLESTEROL; APOLIPOPROTEIN B, and TRIGLYCERIDES while increasing HDL-CHOLESTEROL levels in patients with HYPERCHOLESTEROLEMIA and those at risk for CARDIOVASCULAR DISEASES.

Molecular weight: 481.54
Formula: C22H28FN3O6S
CLOGP: 1.90
LIPINSKI: 0
HAC: 9
HDO: 3
TPSA: 140.92
ALOGS: -3.74
ROTB: 9

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	30 %	Hosey CM, Chan R, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Hosey CM, Chan R, Benet LZ
BA (Bioavailability)	20 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	2 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	11 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.70 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.19 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.33 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.12 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 12, 2003	FDA	IPR
Jan. 19, 2005	PMDA	AstraZeneca K.K.

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
Rhabdomyolysis	1210.49	9.59	1006	181329	42945	63263742
Myalgia	916.28	9.59	1566	180769	144963	63161724
Maternal exposure during pregnancy	505.53	9.59	32	182303	220030	63086657
Pemphigus	456.43	9.59	16	182319	183710	63122977
Blood creatine phosphokinase increased	444.32	9.59	491	181844	29939	63276748
Sedation complication	421.59	9.59	336	181999	13486	63293201
Creatinine renal clearance decreased	419.27	9.59	359	181976	15949	63290738
Orthostatic hypotension	379.15	9.59	493	181842	35667	63271020
Systemic lupus erythematosus	378.23	9.59	71	182264	208847	63097840
Glossodynia	364.67	9.59	43	182292	178833	63127854

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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	1263.02	10.74	1711	154593	82399	34718228
Rhabdomyolysis	1047.73	10.74	1403	154901	66760	34733867
Blood creatine phosphokinase increased	507.09	10.74	799	155505	44058	34756569
Toxicity to various agents	357.31	10.74	228	156076	200134	34600493
Myopathy	276.06	10.74	298	156006	11256	34789371
Drug abuse	275.92	10.74	54	156250	99042	34701585
Death	228.10	10.74	962	155342	397087	34403540
Completed suicide	205.14	10.74	91	156213	98077	34702550
High density lipoprotein decreased	189.79	10.74	141	156163	3219	34797408
Low density lipoprotein increased	169.33	10.74	148	156156	4288	34796339

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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
Rhabdomyolysis	2034.66	9.81	2171	285748	100960	79355509
Myalgia	1752.09	9.81	2709	285210	182932	79273537
Blood creatine phosphokinase increased	842.45	9.81	1114	286805	64976	79391493
Myopathy	449.84	9.81	458	287461	20105	79436364
Maternal exposure during pregnancy	390.85	9.81	26	287893	136512	79319957
Sedation complication	362.94	9.81	360	287559	15309	79441160
Creatinine renal clearance decreased	353.04	9.81	388	287531	18614	79437855
Completed suicide	348.92	9.81	229	287690	245538	79210931
Orthostatic hypotension	297.54	9.81	639	287280	55525	79400944
Drug abuse	286.89	9.81	114	287805	162577	79293892

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A10BH52	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Dipeptidyl peptidase 4 (DPP-4) inhibitors
ATC	C10AA07	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN HMG CoA reductase inhibitors
ATC	C10BA06	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BA07	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BA09	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BX05	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX07	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX09	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX10	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX13	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
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
Prevention of Transient Ischemic Attacks	indication
Primary Prevention of Coronary Heart Disease	indication

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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	4.29	acidic
pKa2	13.84	acidic
pKa3	3.67	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;EQ 10MG BASE	ROSZET	ALTHERA PHARMS	N213072	March 23, 2021	DISCN	TABLET	ORAL	10376470	May 1, 2033	TREATMENT OF HYPERLIPIDEMIA
10MG;EQ 10MG BASE	ROSZET	ALTHERA PHARMS	N213072	March 23, 2021	DISCN	TABLET	ORAL	9763885	May 1, 2033	TREATMENT OF HYPERLIPIDEMIA
10MG;EQ 20MG BASE	ROSZET	ALTHERA PHARMS	N213072	March 23, 2021	DISCN	TABLET	ORAL	10376470	May 1, 2033	TREATMENT OF HYPERLIPIDEMIA
10MG;EQ 20MG BASE	ROSZET	ALTHERA PHARMS	N213072	March 23, 2021	DISCN	TABLET	ORAL	9763885	May 1, 2033	TREATMENT OF HYPERLIPIDEMIA
10MG;EQ 40MG BASE	ROSZET	ALTHERA PHARMS	N213072	March 23, 2021	DISCN	TABLET	ORAL	10376470	May 1, 2033	TREATMENT OF HYPERLIPIDEMIA
10MG;EQ 40MG BASE	ROSZET	ALTHERA PHARMS	N213072	March 23, 2021	DISCN	TABLET	ORAL	9763885	May 1, 2033	TREATMENT OF HYPERLIPIDEMIA
10MG;EQ 5MG BASE	ROSZET	ALTHERA PHARMS	N213072	March 23, 2021	DISCN	TABLET	ORAL	10376470	May 1, 2033	TREATMENT OF HYPERLIPIDEMIA
10MG;EQ 5MG BASE	ROSZET	ALTHERA PHARMS	N213072	March 23, 2021	DISCN	TABLET	ORAL	9763885	May 1, 2033	TREATMENT OF HYPERLIPIDEMIA

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 10MG BASE	CRESTOR	IPR	N021366	Aug. 12, 2003	RX	TABLET	ORAL	May 27, 2023	AN ADJUNCT TO DIET TO REDUCE LDL-C, TOTAL-C, NONHDL-C AND APOB IN CHILDREN AND ADOLESCENTS 7 TO 17 YEARS OF AGE WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA, EITHER ALONE OR WITH OTHER LIPID-LOWERING TREATMENTS (E.G., LDL APHERESIS)
EQ 20MG BASE	CRESTOR	IPR	N021366	Aug. 12, 2003	RX	TABLET	ORAL	May 27, 2023	AN ADJUNCT TO DIET TO REDUCE LDL-C, TOTAL-C, NONHDL-C AND APOB IN CHILDREN AND ADOLESCENTS 7 TO 17 YEARS OF AGE WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA, EITHER ALONE OR WITH OTHER LIPID-LOWERING TREATMENTS (E.G., LDL APHERESIS)
EQ 40MG BASE	CRESTOR	IPR	N021366	Aug. 12, 2003	RX	TABLET	ORAL	May 27, 2023	AN ADJUNCT TO DIET TO REDUCE LDL-C, TOTAL-C, NONHDL-C AND APOB IN CHILDREN AND ADOLESCENTS 7 TO 17 YEARS OF AGE WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA, EITHER ALONE OR WITH OTHER LIPID-LOWERING TREATMENTS (E.G., LDL APHERESIS)
EQ 5MG BASE	CRESTOR	IPR	N021366	Aug. 12, 2003	RX	TABLET	ORAL	May 27, 2023	AN ADJUNCT TO DIET TO REDUCE LDL-C, TOTAL-C, NONHDL-C AND APOB IN CHILDREN AND ADOLESCENTS 7 TO 17 YEARS OF AGE WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA, EITHER ALONE OR WITH OTHER LIPID-LOWERING TREATMENTS (E.G., LDL APHERESIS)

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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	Ki	9.05	CHEMBL	CHEMBL
Phosphodiesterase 6D	Enzyme	O43924	PDE6D_HUMAN		Kd	5.90	CHEMBL
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme		HMDH_RAT		IC50	8.68	CHEMBL

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External reference:

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ID	Source
FBI	PDB_CHEM_ID
009902	NDDF
009903	NDDF
019242	NDDF
107656	MMSL
1217216007	SNOMEDCT_US
147098-20-2	SECONDARY_CAS_RN
17146	MMSL
17536	MMSL
2954	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0751	TABLET, FILM COATED	10 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0751	TABLET, FILM COATED	10 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0751	TABLET, FILM COATED	10 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0752	TABLET, FILM COATED	20 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0752	TABLET, FILM COATED	20 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0752	TABLET, FILM COATED	20 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0754	TABLET, FILM COATED	40 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0754	TABLET, FILM COATED	40 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0754	TABLET, FILM COATED	40 mg	ORAL	NDA	27 sections
CRESTOR	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0755	TABLET, FILM COATED	5 mg	ORAL	NDA	27 sections

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