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

Stem definition	Drug id	CAS RN
antihyperlipidaemic substances, HMG CoA reductase inhibitors	1612	75330-75-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lovastatin lostatin mevacor	A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver. Molecular weight: 404.55 Formula: C24H36O5 CLOGP: 4.08 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 72.83 ALOGS: -4.22 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lovastatin
lostatin
mevacor

A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.

Molecular weight: 404.55
Formula: C24H36O5
CLOGP: 4.08
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 72.83
ALOGS: -4.22
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
45	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.00 mg/mL	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)	3.29 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	5 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Aug. 31, 1987	FDA	MERCK

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
Rheumatoid arthritis	65.36	12.55	21	18109	382583	55891354
Myalgia	50.35	12.55	123	18007	131902	56142035
Cardiac failure congestive	49.81	12.55	96	18034	87624	56186313
Contraindicated product administered	48.10	12.55	3	18127	186283	56087654
Rhabdomyolysis	47.57	12.55	62	18068	40596	56233341
Drug hypersensitivity	42.27	12.55	188	17942	275017	55998920
Blood glucose increased	41.14	12.55	81	18049	75070	56198867
Synovitis	37.76	12.55	4	18126	161301	56112636
Systemic lupus erythematosus	34.22	12.55	8	18122	180070	56093867
Atrial fibrillation	33.84	12.55	94	18036	108803	56165134
Treatment failure	33.53	12.55	7	18123	170385	56103552
Infusion related reaction	33.00	12.55	13	18117	208918	56065019
Glossodynia	32.73	12.55	5	18125	152453	56121484
Exposure during pregnancy	30.37	12.55	4	18126	136338	56137599
Muscle spasms	30.09	12.55	105	18025	137266	56136671
Wound	28.80	12.55	5	18125	138799	56135138
Dehydration	25.47	12.55	110	18020	158715	56115222
Myocardial infarction	24.84	12.55	76	18054	92794	56181143
Off label use	24.72	12.55	94	18036	556086	55717851
Asthenia	23.69	12.55	190	17940	342783	55931154
General physical health deterioration	23.11	12.55	13	18117	169997	56103940
Alopecia	21.08	12.55	39	18091	293419	55980518
Drug intolerance	21.03	12.55	33	18097	264785	56009152
Cerebrovascular accident	20.97	12.55	75	18055	99195	56174742
Retroperitoneal oedema	20.84	12.55	4	18126	21	56273916
Coronary artery disease	20.35	12.55	36	18094	30760	56243177
Lower respiratory tract infection	20.09	12.55	6	18124	114788	56159149
Myopathy	20.07	12.55	20	18110	9792	56264145
Chronic obstructive pulmonary disease	19.26	12.55	51	18079	57364	56216573
Product use issue	19.14	12.55	19	18111	186022	56087915
Hepatic enzyme increased	18.22	12.55	17	18113	171367	56102570
Febrile neutropenia	17.61	12.55	6	18124	105539	56168398
Dizziness	17.24	12.55	191	17939	375949	55897988
Pyrexia	17.17	12.55	73	18057	418700	55855237
Product quality issue	17.10	12.55	34	18096	31702	56242235
Amyotrophic lateral sclerosis	17.10	12.55	8	18122	1120	56272817
Feeling abnormal	16.63	12.55	86	18044	133516	56140421
Fall	16.13	12.55	181	17949	357329	55916608
Product dose omission issue	16.10	12.55	117	18013	204636	56069301
C-reactive protein increased	15.95	12.55	3	18127	78681	56195256
Nausea	14.63	12.55	335	17795	763843	55510094
Therapeutic product effect decreased	14.53	12.55	20	18110	169432	56104505
Chronic kidney disease	13.74	12.55	37	18093	42019	56231918
Chest pain	13.53	12.55	106	18024	189691	56084246
Gait disturbance	13.22	12.55	94	18036	163227	56110710
Cardiomegaly	13.21	12.55	21	18109	16446	56257491
Pulmonary arterial pressure increased	13.20	12.55	10	18120	3395	56270542
Discomfort	12.90	12.55	16	18114	141745	56132192
Abdominal discomfort	12.84	12.55	46	18084	277228	55996709
Drug ineffective	12.76	12.55	214	17916	918775	55355162

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
Type IIa hyperlipidaemia	39.35	13.58	11	13613	255	31683465
Myasthenic syndrome	38.55	13.58	12	13612	408	31683312
Rhabdomyolysis	36.65	13.58	83	13541	63498	31620222
Cardiac failure congestive	32.51	13.58	91	13533	79296	31604424
Neck mass	29.19	13.58	14	13610	1550	31682170
Cerebrovascular accident	24.93	13.58	83	13541	79401	31604319
Drug abuse	24.79	13.58	4	13620	87754	31595966
Myalgia	24.52	13.58	81	13543	77177	31606543
Back disorder	23.29	13.58	20	13604	6073	31677647
Diverticulum	22.19	13.58	20	13604	6474	31677246
Sleep inertia	20.58	13.58	4	13620	16	31683704
Febrile neutropenia	19.96	13.58	14	13610	121835	31561885
Asthenia	19.57	13.58	164	13460	224591	31459129
Blood creatine phosphokinase increased	19.05	13.58	50	13574	41924	31641796
Thrombocytosis	17.97	13.58	14	13610	3709	31680011
Anxiety	17.87	13.58	82	13542	90951	31592769
Injury	17.71	13.58	31	13593	19678	31664042
Myocardial infarction	17.20	13.58	95	13529	113359	31570361
Myopathy	16.80	13.58	22	13602	10830	31672890
Off label use	16.56	13.58	85	13539	347189	31336531
Hand deformity	15.90	13.58	12	13612	3035	31680685
International normalised ratio increased	15.78	13.58	49	13575	45174	31638546
Pyrexia	15.26	13.58	73	13551	303767	31379953
Pinguecula	14.57	13.58	3	13621	17	31683703

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
Rhabdomyolysis	87.97	12.06	134	24074	95626	70808610
Cardiac failure congestive	77.78	12.06	154	24054	135303	70768933
Myalgia	48.96	12.06	147	24061	167745	70736491
Blood glucose increased	45.16	12.06	105	24103	102877	70801359
Myocardial infarction	44.24	12.06	144	24064	171501	70732735
Type IIa hyperlipidaemia	43.24	12.06	12	24196	344	70903892
Rheumatoid arthritis	40.15	12.06	25	24183	291780	70612456
Asthenia	39.94	12.06	280	23928	457386	70446850
Drug abuse	38.85	12.06	3	24205	147253	70756983
Myopathy	36.35	12.06	38	24170	18574	70885662
Myasthenic syndrome	34.94	12.06	12	24196	706	70903530
Cerebrovascular accident	34.85	12.06	118	24090	143352	70760884
Atrial fibrillation	33.42	12.06	138	24070	184210	70720026
Infusion related reaction	33.08	12.06	13	24195	197521	70706715
Drug hypersensitivity	31.92	12.06	175	24033	262284	70641952
Febrile neutropenia	28.80	12.06	17	24191	204301	70699935
Treatment failure	28.58	12.06	7	24201	144135	70760101
Off label use	28.36	12.06	144	24064	742916	70161320
Coronary artery disease	27.53	12.06	64	24144	62672	70841564
General physical health deterioration	24.10	12.06	27	24181	236004	70668232
Contraindicated product administered	23.99	12.06	8	24200	134604	70769632
Pyrexia	22.35	12.06	119	24089	606833	70297403
Dehydration	21.84	12.06	142	24066	226000	70678236
Back disorder	21.40	12.06	22	24186	10542	70893694
Intentional overdose	21.10	12.06	4	24204	98431	70805805
Sleep inertia	20.94	12.06	4	24204	19	70904217
Retroperitoneal oedema	20.61	12.06	4	24204	21	70904215
Blood creatine phosphokinase increased	20.10	12.06	56	24152	61207	70843029
Product use in unapproved indication	19.83	12.06	25	24183	207453	70696783
Neck mass	19.38	12.06	14	24194	4172	70900064
Pericarditis	19.13	12.06	3	24205	84702	70819534
Product quality issue	17.81	12.06	35	24173	30526	70873710
Lower respiratory tract infection	17.71	12.06	8	24200	111905	70792331
Mental status changes	17.20	12.06	54	24154	63047	70841189
Myositis	16.78	12.06	25	24183	17464	70886772
Systemic lupus erythematosus	16.57	12.06	7	24201	101895	70802341
Muscle spasms	16.27	12.06	99	24109	153947	70750289
Cardiovascular disorder	16.24	12.06	24	24184	16646	70887590
International normalised ratio increased	15.86	12.06	62	24146	80664	70823572
Interstitial lung disease	15.77	12.06	8	24200	104677	70799559
Diverticulum	15.23	12.06	21	24187	13672	70890564
Pain in extremity	14.75	12.06	174	24034	327908	70576328
Feeling abnormal	14.74	12.06	91	24117	142228	70762008
Wound	14.21	12.06	8	24200	98724	70805512
Glossodynia	13.97	12.06	6	24202	86481	70817755
Chronic obstructive pulmonary disease	13.95	12.06	58	24150	77583	70826653
Product dose omission issue	13.91	12.06	124	24084	217344	70686892
Renal failure	13.78	12.06	111	24097	188959	70715277
Chronic kidney disease	13.75	12.06	49	24159	61008	70843228
Fall	13.64	12.06	220	23988	443876	70460360
Amyotrophic lateral sclerosis	13.26	12.06	8	24200	1766	70902470
Hyperlipidaemia	12.33	12.06	26	24182	23837	70880399
Fatigue	12.31	12.06	368	23840	823951	70080285
Blood urea increased	12.24	12.06	39	24169	45870	70858366

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C10AA02	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN HMG CoA reductase inhibitors
ATC	C10BA01	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
FDA MoA	N0000000121	Hydroxymethylglutaryl-CoA Reductase Inhibitors
FDA EPC	N0000175589	HMG-CoA Reductase Inhibitor
MeSH PA	D000924	Anticholesteremic Agents
MeSH PA	D000963	Antimetabolites
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D019161	Hydroxymethylglutaryl-CoA Reductase Inhibitors
MeSH PA	D000960	Hypolipidemic Agents
MeSH PA	D057847	Lipid Regulating Agents
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:35821	anticholesteremic drugs
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:76956	Aspergillus metabolites

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

Disease	Relation	SNOMED_ID	DOID
Hypercholesterolemia	indication	13644009
Hyperlipidemia	indication	55822004	DOID:1168
Arteriosclerotic vascular disease	indication	72092001
Hypoalphalipoproteinemia	indication	190785000
Familial hypercholesterolemia - heterozygous	indication	238079002
Mixed hyperlipidemia	indication	267434003
Hypertriglyceridemia	indication	302870006
Myocardial Reinfarction Prevention	indication
Slow Progression of Coronary Artery Disease	indication
Primary Prevention of Coronary Heart Disease	indication
Myocardial Infarction Prevention	indication
Cerebrovascular accident	off-label use	230690007
Prevention of Transient Ischemic Attacks	off-label use
Hypophosphatemia	contraindication	4996001
Alcoholism	contraindication	7200002
Peptic ulcer	contraindication	13200003	DOID:750
Myocardial infarction	contraindication	22298006	DOID:5844
Low blood pressure	contraindication	45007003
Acute nephropathy	contraindication	58574008
Blood coagulation disorder	contraindication	64779008	DOID:1247
Diabetes mellitus	contraindication	73211009	DOID:9351
Hyperglycemia	contraindication	80394007	DOID:4195
Gout	contraindication	90560007	DOID:13189
Disorder of muscle	contraindication	129565002	DOID:423
Liver function tests abnormal	contraindication	166603001
Hemorrhagic cerebral infarction	contraindication	230706003
Arterial hemorrhage	contraindication	234003006
Disease of liver	contraindication	235856003	DOID:409
Rhabdomyolysis	contraindication	240131006
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Surgical procedure	contraindication	387713003
Acute coronary syndrome	contraindication	394659003
Breastfeeding (mother)	contraindication	413712001
Disorder of coronary artery	contraindication	414024009
Traumatic injury	contraindication	417746004
Uncontrolled Epilepsy	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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	7.67	WOMBAT-PK	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.06	DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	5.10	DRUG MATRIX
Adenosine receptor A1	GPCR	P30542	AA1R_HUMAN		Ki	4.81	DRUG MATRIX
Nuclear receptor subfamily 1 group I member 2	Nuclear hormone receptor	O75469	NR1I2_HUMAN	AGONIST	EC50	6	IUPHAR
Hydroxycarboxylic acid receptor 2	GPCR	Q8TDS4	HCAR2_HUMAN		IC50	7.30	WOMBAT-PK
Hydroxycarboxylic acid receptor 3	GPCR	P49019	HCAR3_HUMAN		IC50	6.53	WOMBAT-PK
Histone deacetylase 2	Enzyme	Q92769	HDAC2_HUMAN		IC50	4.59	CHEMBL
Histone deacetylase 1	Enzyme	Q13547	HDAC1_HUMAN		IC50	4.92	CHEMBL
Substance-K receptor	GPCR	P21452	NK2R_HUMAN		Ki	5.03	DRUG MATRIX
Leukocyte adhesion glycoprotein LFA-1 alpha	Adhesion	P20701	ITAL_HUMAN		Kd	4.89	CHEMBL
Histone deacetylase 6	Enzyme	Q9UBN7	HDAC6_HUMAN		IC50	4.79	CHEMBL
Androgen receptor	Transcription factor		ANDR_RAT		Ki	4.70	DRUG MATRIX
Acetylcholinesterase	Enzyme		ACES_ELEEL		Ki	5.57	CHEMBL
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme		HMDH_RAT		IC50	8.52	CHEMBL
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme		HMDH_MOUSE		IC50	7.57	CHEMBL
Cholinesterase	Enzyme		CHLE_HORSE		Ki	5.96	CHEMBL
Acyl-CoA:cholesterol acyltransferase	Enzyme		Q95214_RABIT		IC50	4.77	CHEMBL

External reference:

ID	Source
4019482	VUID
N0000147602	NUI
D00359	KEGG_DRUG
4019482	VANDF
C0024027	UMLSCUI
CHEBI:40303	CHEBI
803	PDB_CHEM_ID
CHEMBL503	ChEMBL_ID
D008148	MESH_DESCRIPTOR_UI
DB00227	DRUGBANK_ID
53232	PUBCHEM_CID
2739	IUPHAR_LIGAND_ID
6074	INN_ID
9LHU78OQFD	UNII
224938	RXNORM
1105	MMSL
42628	MMSL
4998	MMSL
d00280	MMSL
002063	NDDF
386024001	SNOMEDCT_US
96303004	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0576	TABLET	20 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0926	TABLET	10 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0928	TABLET	40 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0070	TABLET	10 mg	ORAL	ANDA	18 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0072	TABLET	20 mg	ORAL	ANDA	18 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0074	TABLET	40 mg	ORAL	ANDA	18 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8151	TABLET	20 mg	ORAL	ANDA	12 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8151	TABLET	20 mg	ORAL	ANDA	12 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8152	TABLET	40 mg	ORAL	ANDA	12 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8152	TABLET	40 mg	ORAL	ANDA	12 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-235	TABLET	10 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-241	TABLET	20 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	10544-242	TABLET	40 mg	ORAL	ANDA	22 sections
Lovastatin	Human Prescription Drug Label	1	10544-246	TABLET	20 mg	ORAL	ANDA	19 sections
LOVASTATIN	HUMAN PRESCRIPTION DRUG LABEL	1	16590-311	TABLET	10 mg	ORAL	ANDA	12 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	21695-534	TABLET	10 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	21695-535	TABLET	20 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	21695-536	TABLET	40 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	33261-547	TABLET	10 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	33261-548	TABLET	20 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	33261-549	TABLET	40 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	42254-025	TABLET	40 mg	ORAL	ANDA	21 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	42254-028	TABLET	20 mg	ORAL	ANDA	21 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	42254-106	TABLET	10 mg	ORAL	ANDA	21 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43063-493	TABLET	10 mg	ORAL	ANDA	12 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43063-493	TABLET	10 mg	ORAL	ANDA	12 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43063-548	TABLET	40 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43063-548	TABLET	40 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43063-548	TABLET	40 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43063-692	TABLET	20 mg	ORAL	ANDA	22 sections