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
Cardiac failure congestive	53.52	12.71	97	18625	92336	63377964
Myalgia	52.24	12.71	126	18596	146403	63323897
Rhabdomyolysis	48.07	12.71	62	18660	43889	63426411
Contraindicated product administered	46.51	12.71	5	18717	217643	63252657
Drug hypersensitivity	41.94	12.71	192	18530	310495	63159805
Synovitis	40.70	12.71	4	18718	186914	63283386
Blood glucose increased	39.99	12.71	81	18641	83675	63386625
Infusion related reaction	37.17	12.71	13	18709	245508	63224792
Atrial fibrillation	36.01	12.71	95	18627	116541	63353759
Systemic lupus erythematosus	35.37	12.71	9	18713	208909	63261391
Glossodynia	33.76	12.71	6	18716	178870	63291430
Treatment failure	32.89	12.71	9	18713	199034	63271266
Exposure during pregnancy	32.16	12.71	4	18718	155543	63314757
Muscle spasms	29.37	12.71	107	18615	156043	63314257
Dehydration	28.66	12.71	114	18608	173240	63297060
Off label use	26.42	12.71	106	18616	674356	62795944
Rheumatoid arthritis	25.99	12.71	22	18700	253797	63216503
Wound	25.83	12.71	8	18714	163255	63307045
Myocardial infarction	25.55	12.71	76	18646	99817	63370483
General physical health deterioration	25.22	12.71	14	18708	201388	63268912
Asthenia	25.04	12.71	196	18526	383408	63086892
Drug intolerance	23.63	12.71	34	18688	308627	63161673
Alopecia	23.17	12.71	40	18682	337496	63132804
Coronary artery disease	21.35	12.71	36	18686	32341	63437959
Retroperitoneal oedema	21.19	12.71	4	18718	21	63470279
Cerebrovascular accident	21.13	12.71	75	18647	107949	63362351
Product use issue	20.34	12.71	21	18701	220499	63249801
Chronic obstructive pulmonary disease	20.30	12.71	52	18670	62634	63407666
Hepatic enzyme increased	20.14	12.71	18	18704	202310	63267990
Lower respiratory tract infection	20.02	12.71	7	18715	132300	63338000
Myopathy	19.34	12.71	20	18702	11171	63459129
Febrile neutropenia	18.38	12.71	6	18716	118443	63351857
C-reactive protein increased	18.25	12.71	3	18719	94704	63375596
Feeling abnormal	18.00	12.71	89	18633	148303	63321997
Fall	17.66	12.71	185	18537	392149	63078151
Amyotrophic lateral sclerosis	17.54	12.71	8	18714	1155	63469145
Product dose omission issue	17.11	12.71	123	18599	234190	63236110
Pyrexia	17.10	12.71	76	18646	470402	62999898
Product quality issue	16.30	12.71	34	18688	35831	63434469
Nausea	15.94	12.71	346	18376	854125	62616175
Therapeutic product effect decreased	15.05	12.71	21	18701	193166	63277134
Arthropathy	15.04	12.71	29	18693	234763	63235537
Dizziness	15.00	12.71	193	18529	429732	63040568
Abdominal discomfort	14.80	12.71	47	18675	320838	63149462
Discomfort	14.27	12.71	17	18705	167357	63302943
Chronic kidney disease	14.02	12.71	37	18685	45361	63424939
Gait disturbance	13.85	12.71	97	18625	183081	63287219
Cardiomegaly	13.54	12.71	21	18701	17593	63452707
Pulmonary arterial pressure increased	13.50	12.71	10	18712	3585	63466715
Psoriasis	13.41	12.71	56	18666	86901	63383399
Chest pain	13.32	12.71	109	18613	215850	63254450
Swelling	12.93	12.71	40	18682	275338	63194962
Gallbladder oedema	12.79	12.71	4	18718	203	63470097

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
Myasthenic syndrome	49.08	13.48	15	13972	516	34942428
Rhabdomyolysis	42.49	13.48	88	13899	68075	34874869
Cardiac failure congestive	33.87	13.48	91	13896	83179	34859765
Neck mass	29.73	13.48	14	13973	1599	34941345
Myalgia	29.39	13.48	87	13900	84023	34858921
Drug abuse	26.52	13.48	4	13983	99092	34843852
Cerebrovascular accident	25.26	13.48	83	13904	84728	34858216
Off label use	23.92	13.48	87	13900	419437	34523507
Back disorder	23.01	13.48	20	13967	6631	34936313
Myopathy	21.83	13.48	25	13962	11529	34931415
Diverticulum	21.74	13.48	20	13967	7139	34935805
Febrile neutropenia	21.72	13.48	14	13973	136835	34806109
Blood creatine phosphokinase increased	21.31	13.48	52	13935	44805	34898139
Asthenia	20.10	13.48	167	13820	245084	34697860
Sleep inertia	19.67	13.48	4	13983	23	34942921
Injury	18.23	13.48	31	13956	20656	34922288
Cardiovascular disorder	17.73	13.48	21	13966	10035	34932909
Thrombocytosis	17.63	13.48	14	13973	4098	34938846
Myocardial infarction	17.50	13.48	95	13892	120990	34821954
Anxiety	17.16	13.48	82	13905	99346	34843598
International normalised ratio increased	16.56	13.48	49	13938	47278	34895666
Potentiating drug interaction	15.30	13.48	14	13973	4963	34937981
Pinguecula	14.64	13.48	3	13984	18	34942926
Hand deformity	14.52	13.48	12	13975	3713	34939231
Blood glucose increased	14.52	13.48	59	13928	66659	34876285
Atrial fibrillation	13.80	13.48	90	13897	122303	34820641

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	96.33	12.24	139	24849	102992	79616408
Cardiac failure congestive	82.87	12.24	155	24833	142247	79577153
Myalgia	55.27	12.24	155	24833	185486	79533914
Myasthenic syndrome	45.88	12.24	15	24973	827	79718573
Myocardial infarction	45.55	12.24	144	24844	183985	79535415
Blood glucose increased	44.52	12.24	106	24882	114869	79604531
Myopathy	41.34	12.24	41	24947	20522	79698878
Asthenia	40.75	12.24	287	24701	511402	79207998
Drug abuse	39.53	12.24	3	24985	162688	79556712
Atrial fibrillation	36.14	12.24	140	24848	197746	79521654
Cerebrovascular accident	35.28	12.24	118	24870	155174	79564226
Infusion related reaction	35.26	12.24	14	24974	230223	79489177
Off label use	35.00	12.24	156	24832	907059	78812341
Drug hypersensitivity	31.40	12.24	180	24808	298736	79420664
Febrile neutropenia	30.82	12.24	17	24971	230982	79488418
Coronary artery disease	29.37	12.24	64	24924	65410	79653990
Treatment failure	26.70	12.24	10	24978	170476	79548924
General physical health deterioration	25.71	12.24	29	24959	275209	79444191
Blood creatine phosphokinase increased	24.57	12.24	60	24928	66030	79653370
Dehydration	23.82	12.24	146	24842	248041	79471359
Pericarditis	22.52	12.24	3	24985	104233	79615167
Back disorder	21.29	12.24	22	24966	11556	79707844
Myositis	21.12	12.24	28	24960	19140	79700260
Retroperitoneal oedema	20.95	12.24	4	24984	21	79719379
Cardiovascular disorder	20.90	12.24	27	24961	17998	79701402
Sleep inertia	20.50	12.24	4	24984	24	79719376
Contraindicated product administered	20.42	12.24	12	24976	157526	79561874
Pyrexia	19.83	12.24	128	24860	678581	79040819
Neck mass	19.82	12.24	14	24974	4390	79715010
Lower respiratory tract infection	19.54	12.24	8	24980	129212	79590188
Intentional overdose	18.75	12.24	5	24983	105955	79613445
Product use in unapproved indication	18.71	12.24	31	24957	250328	79469072
Mental status changes	18.05	12.24	54	24934	66905	79652495
Systemic lupus erythematosus	17.52	12.24	8	24980	121141	79598259
Product quality issue	17.34	12.24	35	24953	33905	79685495
Renal failure	17.28	12.24	115	24873	200853	79518547
International normalised ratio increased	17.16	12.24	62	24926	84659	79634741
Pain in extremity	15.72	12.24	179	24809	364359	79355041
Feeling abnormal	15.48	12.24	94	24894	159105	79560295
Interstitial lung disease	15.43	12.24	8	24980	112592	79606808
Rheumatoid arthritis	15.40	12.24	26	24962	208444	79510956
Death	15.37	12.24	256	24732	566258	79153142
Plasma cell myeloma	15.36	12.24	44	24944	53215	79666185
Diverticulum	15.25	12.24	21	24967	14875	79704525
Muscle spasms	15.03	12.24	100	24888	174630	79544770
Fall	14.97	12.24	225	24763	487404	79231996
Wound	14.84	12.24	9	24979	116170	79603230
Chronic kidney disease	14.77	12.24	50	24938	66104	79653296
Product dose omission issue	14.75	12.24	130	24858	247407	79471993
Blood urea increased	14.75	12.24	41	24947	48749	79670651
Glossodynia	14.67	12.24	7	24981	103330	79616070
Chronic obstructive pulmonary disease	14.42	12.24	59	24929	85360	79634040
Amyotrophic lateral sclerosis	13.72	12.24	8	24980	1807	79717593
Potentiating drug interaction	13.14	12.24	15	24973	8804	79710596
Gastrointestinal haemorrhage	12.98	12.24	85	24903	147634	79571766
Right ventricular failure	12.93	12.24	25	24963	23472	79695928
Hypersensitivity	12.70	12.24	41	24947	262198	79457202

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 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
Histone deacetylase 6	Enzyme	Q9UBN7	HDAC6_HUMAN		IC50	4.79	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
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.06	DRUG MATRIX
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