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

Stem definition	Drug id	CAS RN
antihyperlipidaemic substances, HMG CoA reductase inhibitors	2445	79902-63-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: simvastatin sinvacor simvastol	A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL. Molecular weight: 418.57 Formula: C25H38O5 CLOGP: 4.48 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 72.83 ALOGS: -4.53 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

simvastatin
sinvacor
simvastol

A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.

Molecular weight: 418.57
Formula: C25H38O5
CLOGP: 4.48
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 72.83
ALOGS: -4.53
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
30	mg	O
30	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	3 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	10 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.37 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.03 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 23, 1991	FDA	MERCK

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	2204.21	9.91	1619	243940	42332	63201131
Myalgia	968.83	9.91	1900	243659	144629	63098834
Drug interaction	831.36	9.91	2349	243210	226782	63016681
Drug ineffective	747.55	9.91	1860	243699	1042905	62200558
Maternal exposure during pregnancy	644.04	9.91	56	245503	220006	63023457
Blood creatine phosphokinase increased	611.83	9.91	669	244890	29761	63213702
Systemic lupus erythematosus	609.10	9.91	54	245505	208864	63034599
Pemphigus	593.01	9.91	28	245531	183698	63059765
Acute kidney injury	575.45	9.91	2276	243283	261139	62982324
Hand deformity	543.05	9.91	16	245543	159441	63084022

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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
Rhabdomyolysis	2696.85	11.25	2836	242940	65327	34645828
Myalgia	1224.13	11.25	2152	243624	81958	34629197
Blood creatine phosphokinase increased	731.28	11.25	1208	244568	43649	34667506
Off label use	673.95	11.25	1203	244573	418321	34292834
Drug ineffective	600.46	11.25	1468	244308	455283	34255872
Myopathy	525.15	11.25	519	245257	11035	34700120
Drug interaction	430.26	11.25	2888	242888	223058	34488097
Drug abuse	429.48	11.25	87	245689	99009	34612146
Myocardial infarction	329.89	11.25	1702	244074	119383	34591772
Febrile neutropenia	300.79	11.25	311	245465	136538	34574617

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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	4513.14	9.72	3922	400971	99209	79240286
Myalgia	1831.37	9.72	3337	401556	182304	79157191
Drug interaction	1346.52	9.72	4895	399998	410288	78929207
Blood creatine phosphokinase increased	1285.47	9.72	1631	403262	64459	79275036
Drug ineffective	1169.30	9.72	2336	402557	1078577	78260918
Myopathy	1012.40	9.72	838	404055	19725	79319770
Acute kidney injury	977.23	9.72	5202	399691	514202	78825293
Off label use	938.65	9.72	2009	402884	905206	78434289
Myocardial infarction	700.52	9.72	2292	402601	181837	79157658
Maternal exposure during pregnancy	514.94	9.72	49	404844	136489	79203006

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A10BH51	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Dipeptidyl peptidase 4 (DPP-4) inhibitors
ATC	C10AA01	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN HMG CoA reductase inhibitors
ATC	C10BA02	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BA04	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BX01	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
ATC	C10BX04	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Lipid modifying agents in combination with other drugs
CHEBI has role	CHEBI:35664	hydroxymethylglutaryl-CoA reductase inhibitors
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:77255	lethal toxin inhibitors
CHEBI has role	CHEBI:173085	ferroptosis inducers

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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
Hypoalphalipoproteinemia	indication	190785000
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

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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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 100MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	JUVISYNC	MERCK SHARP DOHME	N202343	Oct. 7, 2011	DISCN	TABLET	ORAL	7326708	April 11, 2026	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN PATIENTS FOR WHOM TREATMENT WITH BOTH SITAGLIPTIN AND SIMVASTATIN IS APPROPRIATE
10MG;EQ 50MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	JUVISYNC	MERCK SHARP DOHME	N202343	Sept. 18, 2012	DISCN	TABLET	ORAL	7326708	April 11, 2026	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN PATIENTS FOR WHOM TREATMENT WITH BOTH SITAGLIPTIN AND SIMVASTATIN IS APPROPRIATE
20MG;EQ 100MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	JUVISYNC	MERCK SHARP DOHME	N202343	Oct. 7, 2011	DISCN	TABLET	ORAL	7326708	April 11, 2026	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN PATIENTS FOR WHOM TREATMENT WITH BOTH SITAGLIPTIN AND SIMVASTATIN IS APPROPRIATE
20MG;EQ 50MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	JUVISYNC	MERCK SHARP DOHME	N202343	Sept. 18, 2012	DISCN	TABLET	ORAL	7326708	April 11, 2026	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN PATIENTS FOR WHOM TREATMENT WITH BOTH SITAGLIPTIN AND SIMVASTATIN IS APPROPRIATE
40MG;EQ 100MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	JUVISYNC	MERCK SHARP DOHME	N202343	Oct. 7, 2011	DISCN	TABLET	ORAL	7326708	April 11, 2026	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN PATIENTS FOR WHOM TREATMENT WITH BOTH SITAGLIPTIN AND SIMVASTATIN IS APPROPRIATE
40MG;EQ 50MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	JUVISYNC	MERCK SHARP DOHME	N202343	Sept. 18, 2012	DISCN	TABLET	ORAL	7326708	April 11, 2026	METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN PATIENTS FOR WHOM TREATMENT WITH BOTH SITAGLIPTIN AND SIMVASTATIN IS APPROPRIATE

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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	7.77	WOMBAT-PK	CHEMBL
Nuclear receptor subfamily 1 group I member 3	Nuclear hormone receptor	Q14994	NR1I3_HUMAN				WOMBAT-PK
Nuclear receptor subfamily 4 group A member 2	Nuclear other	P43354	NR4A2_HUMAN		EC50	5.29	CHEMBL
Acetylcholinesterase	Enzyme		ACES_ELEEL		Ki	5.74	CHEMBL
Cholinesterase	Enzyme		CHLE_HORSE		Ki	6.12	CHEMBL
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme		HMDH_SCHPO		IC50	4.02	CHEMBL
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme		HMDH_RAT		IC50	8.37	CHEMBL

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External reference:

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ID	Source
003621	NDDF
2955	IUPHAR_LIGAND_ID
36567	RXNORM
387584000	SNOMEDCT_US
4020400	VUID
4020400	VANDF
54454	PUBCHEM_CID
5465	MMSL
6147	INN_ID
82969	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
SIMVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7992	TABLET, FILM COATED	10 mg	ORAL	ANDA	27 sections
SIMVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7992	TABLET, FILM COATED	10 mg	ORAL	ANDA	27 sections
SIMVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7992	TABLET, FILM COATED	10 mg	ORAL	ANDA	27 sections
SIMVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7993	TABLET, FILM COATED	20 mg	ORAL	ANDA	27 sections
SIMVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7993	TABLET, FILM COATED	20 mg	ORAL	ANDA	27 sections
SIMVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7993	TABLET, FILM COATED	20 mg	ORAL	ANDA	27 sections
SIMVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8056	TABLET, FILM COATED	40 mg	ORAL	ANDA	26 sections
SIMVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8056	TABLET, FILM COATED	40 mg	ORAL	ANDA	26 sections
Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-486	TABLET, FILM COATED	20 mg	ORAL	ANDA	25 sections
Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-487	TABLET, FILM COATED	40 mg	ORAL	ANDA	25 sections

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