Scroll

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
Myalgia	47.23	12.57	122	17644	124197	50463161
Cardiac failure congestive	46.62	12.57	96	17670	84286	50503072
Rhabdomyolysis	45.37	12.57	62	17704	38965	50548393
Drug hypersensitivity	42.10	12.57	187	17579	250823	50336535
Blood glucose increased	38.05	12.57	80	17686	71244	50516114
Atrial fibrillation	30.85	12.57	92	17674	101653	50485705
Synovitis	29.99	12.57	4	17762	123861	50463497
Exposure during pregnancy	29.08	12.57	4	17762	121011	50466347
Muscle spasms	28.60	12.57	103	17663	125450	50461908
Infusion related reaction	28.37	12.57	12	17754	169545	50417813
Treatment failure	27.85	12.57	7	17759	137630	50449728
Systemic lupus erythematosus	26.86	12.57	8	17758	140614	50446744
Glossodynia	25.14	12.57	5	17761	115564	50471794
Rheumatoid arthritis	24.57	12.57	21	17745	202529	50384829
Myocardial infarction	22.84	12.57	76	17690	88951	50498407
Wound	22.14	12.57	5	17761	105789	50481569
Asthenia	22.06	12.57	189	17577	318853	50268505
Off label use	21.95	12.57	89	17677	474337	50113021
Retroperitoneal oedema	20.50	12.57	4	17762	21	50587337
Myopathy	19.82	12.57	20	17746	9119	50578239
General physical health deterioration	19.53	12.57	13	17753	142421	50444937
Dehydration	19.35	12.57	105	17661	152344	50435014
Cerebrovascular accident	19.32	12.57	75	17691	94605	50492753
Coronary artery disease	19.03	12.57	36	17730	29690	50557668
Chronic obstructive pulmonary disease	18.80	12.57	51	17715	53384	50533974
Febrile neutropenia	17.85	12.57	6	17760	97661	50489697
Lower respiratory tract infection	17.14	12.57	6	17760	95195	50492163
Alopecia	17.04	12.57	38	17728	245009	50342349
Amyotrophic lateral sclerosis	16.87	12.57	8	17758	1059	50586299
Pyrexia	16.53	12.57	73	17693	380130	50207228
Drug intolerance	16.05	12.57	33	17733	219071	50368287
Dizziness	15.64	12.57	188	17578	346181	50241177
Psoriasis	15.18	12.57	56	17710	68944	50518414
Feeling abnormal	14.96	12.57	85	17681	125407	50461951
Product dose omission issue	14.90	12.57	113	17653	183725	50403633
Product quality issue	14.61	12.57	33	17733	30825	50556533
Product use issue	14.21	12.57	19	17747	149456	50437902
C-reactive protein increased	14.19	12.57	3	17763	66471	50520887
Hepatic enzyme increased	13.53	12.57	17	17749	137363	50449995
Nausea	13.47	12.57	333	17433	705065	49882293
Product use in unapproved indication	12.86	12.57	13	17753	115806	50471552
Chest pain	12.83	12.57	106	17660	176776	50410582
Gait disturbance	12.60	12.57	93	17673	149912	50437446
Pulmonary arterial pressure increased	12.59	12.57	10	17756	3338	50584020

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	38.26	13.51	12	13427	395	29560693
Rhabdomyolysis	36.04	13.51	83	13356	60725	29500363
Cardiac failure congestive	31.39	13.51	91	13348	76490	29484598
Neck mass	29.17	13.51	14	13425	1467	29559621
Drug abuse	23.52	13.51	4	13435	79879	29481209
Myalgia	23.03	13.51	80	13359	73939	29487149
Back disorder	22.67	13.51	20	13419	5953	29555135
Diverticulum	21.67	13.51	20	13419	6312	29554776
Cerebrovascular accident	21.28	13.51	80	13359	76831	29484257
Sleep inertia	20.36	13.51	4	13435	16	29561072
Hand deformity	19.18	13.51	12	13427	2118	29558970
Febrile neutropenia	18.96	13.51	14	13425	112226	29448862
Thrombocytosis	18.58	13.51	14	13425	3339	29557749
Blood creatine phosphokinase increased	18.30	13.51	50	13389	40594	29520494
Anxiety	18.24	13.51	82	13357	85283	29475805
Injury	17.23	13.51	31	13408	19015	29542073
Asthenia	16.70	13.51	160	13279	215090	29345998
Myopathy	16.35	13.51	22	13417	10511	29550577
Pyrexia	15.31	13.51	73	13366	287549	29273539
Off label use	15.06	13.51	78	13361	300722	29260366
Pinguecula	14.41	13.51	3	13436	17	29561071
Atrial fibrillation	14.01	13.51	89	13350	105557	29455531
Acquired haemophilia	13.72	13.51	7	13432	836	29560252
Gross motor delay	13.59	13.51	5	13434	269	29560819

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	84.74	11.96	134	23595	91592	64383411
Cardiac failure congestive	73.67	11.96	154	23575	130426	64344577
Myalgia	46.41	11.96	146	23583	158471	64316532
Blood glucose increased	41.22	11.96	103	23626	97970	64377033
Myocardial infarction	37.43	11.96	140	23589	165681	64309322
Drug abuse	37.38	11.96	3	23726	132371	64342632
Asthenia	36.08	11.96	275	23454	427769	64047234
Myopathy	35.60	11.96	38	23691	17642	64457361
Myasthenic syndrome	35.32	11.96	12	23717	633	64474370
Drug hypersensitivity	32.59	11.96	173	23556	237642	64237361
Atrial fibrillation	31.83	11.96	136	23593	170953	64304050
Cerebrovascular accident	30.08	11.96	115	23614	137468	64337535
Infusion related reaction	29.14	11.96	12	23717	164455	64310548
Febrile neutropenia	28.27	11.96	17	23712	187640	64287363
Contraindicated product administered	26.52	11.96	4	23725	107825	64367178
Off label use	25.00	11.96	134	23595	632672	63842331
Coronary artery disease	24.89	11.96	63	23666	60370	64414633
Treatment failure	23.30	11.96	7	23722	116809	64358194
Pyrexia	21.66	11.96	119	23610	558525	63916478
General physical health deterioration	21.64	11.96	26	23703	204399	64270604
Back disorder	21.05	11.96	22	23707	9968	64465035
Intentional overdose	20.66	11.96	4	23725	89940	64385063
Sleep inertia	20.64	11.96	4	23725	19	64474984
Retroperitoneal oedema	20.31	11.96	4	23725	21	64474982
Product use in unapproved indication	20.30	11.96	21	23708	176597	64298406
Neck mass	18.88	11.96	14	23715	4030	64470973
Interstitial lung disease	17.52	11.96	7	23722	97725	64377278
Myositis	16.61	11.96	25	23704	16352	64458651
Dehydration	16.41	11.96	136	23593	216627	64258376
Muscle spasms	16.25	11.96	98	23631	140925	64334078
Mental status changes	15.79	11.96	54	23675	61108	64413895
Cardiovascular disorder	15.76	11.96	24	23705	15857	64459146
Product quality issue	15.46	11.96	34	23695	29765	64445238
Blood creatine phosphokinase increased	15.38	11.96	52	23677	58506	64416497
Lower respiratory tract infection	15.06	11.96	8	23721	94606	64380397
Diverticulum	14.61	11.96	21	23708	13177	64461826
Chronic obstructive pulmonary disease	14.39	11.96	58	23671	70990	64404013
Product dose omission issue	14.11	11.96	121	23608	194626	64280377
Pericarditis	13.90	11.96	3	23726	62513	64412490
Pain in extremity	13.70	11.96	171	23558	302914	64172089
Feeling abnormal	13.63	11.96	90	23639	133512	64341491
Rheumatoid arthritis	13.40	11.96	25	23704	164269	64310734
Amyotrophic lateral sclerosis	13.24	11.96	8	23721	1642	64473361
Fatigue	12.52	11.96	362	23367	748368	63726635
International normalised ratio increased	12.51	11.96	60	23669	79107	64395896
Chronic kidney disease	12.30	11.96	48	23681	57871	64417132
Plasma cell myeloma	12.18	11.96	41	23688	46034	64428969

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	0615-8152	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	43063-548	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
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43063-939	TABLET	40 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43063-983	TABLET	20 mg	ORAL	ANDA	22 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43353-763	TABLET	40 mg	ORAL	ANDA	21 sections
Lovastatin	HUMAN PRESCRIPTION DRUG LABEL	1	43353-995	TABLET	40 mg	ORAL	ANDA	22 sections