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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:

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Property	Value	Reference
BA (Bioavailability)	5 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	3.29 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
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
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Aug. 31, 1987	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
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

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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
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

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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	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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
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
FDA EPC	N0000175589	HMG-CoA Reductase Inhibitor
FDA MoA	N0000000121	Hydroxymethylglutaryl-CoA Reductase Inhibitors
MeSH PA	D000924	Anticholesteremic Agents
MeSH PA	D000963	Antimetabolites

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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
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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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:

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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	7.67	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

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External reference:

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ID	Source
803	PDB_CHEM_ID
002063	NDDF
1105	MMSL
224938	RXNORM
2739	IUPHAR_LIGAND_ID
386024001	SNOMEDCT_US
4019482	VUID
4019482	VANDF
42628	MMSL
4998	MMSL

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Pharmaceutical products:

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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

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