Lovastatin

HMG-CoA Reductase Inhibitor — CARDIOVASCULAR SYSTEM

Key facts

Lovastatin is an ofp drug in the HMG-CoA Reductase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 1987. Its mechanism of action is classified as Hydroxymethylglutaryl-CoA Reductase Inhibitors. DrugCentral lists 18 molecular targets, including Hmgcr, HMGCR and Hmgcr. Recorded indications include Arteriosclerotic vascular disease, Familial hypercholesterolemia - heterozygous, Hypercholesterolemia and Hyperlipidemia.

• Approval status: ofp (first approved 1987 by the FDA).
• Drug class: HMG-CoA Reductase Inhibitor.
• Mechanism of action: Hydroxymethylglutaryl-CoA Reductase Inhibitors.
• Molecular targets: Hmgcr, HMGCR, Hmgcr and HCAR2 (18 listed in DrugCentral).
• Indications: Arteriosclerotic vascular disease, Familial hypercholesterolemia - heterozygous, Hypercholesterolemia, Hyperlipidemia and Hypertriglyceridemia and others.
• ATC code: C10AA02 (HMG CoA reductase inhibitors).
• Molecular formula: C24H36O5; molecular weight 404.55 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (11)

• Arteriosclerotic vascular disease
• Familial hypercholesterolemia - heterozygous
• Hypercholesterolemia
• Hyperlipidemia
• Hypertriglyceridemia
• Hypoalphalipoproteinemia
• Mixed hyperlipidemia
• Myocardial Infarction Prevention
• Myocardial Reinfarction Prevention
• Primary Prevention of Coronary Heart Disease
• Slow Progression of Coronary Artery Disease

Off-label uses (2)

• Cerebrovascular accident
• Prevention of Transient Ischemic Attacks

Contraindications (24)

• Acute coronary syndrome
• Acute nephropathy
• Alcoholism
• Arterial hemorrhage
• Blood coagulation disorder
• Breastfeeding (mother)
• Diabetes mellitus
• Disease of liver
• Disorder of coronary artery
• Disorder of muscle
• Gout
• Hemorrhagic cerebral infarction
• Hyperglycemia
• Hypophosphatemia
• Liver function tests abnormal
• Low blood pressure
• Myocardial infarction
• Peptic ulcer
• Pregnancy, function
• Rhabdomyolysis
• Surgical procedure
• Thrombocytopenic disorder
• Traumatic injury
• Uncontrolled Epilepsy

Mechanism & targets

• Mechanism of action (MoA): Hydroxymethylglutaryl-CoA Reductase Inhibitors
• Established pharmacologic class: HMG-CoA Reductase Inhibitor

Molecular targets (18)

Target	Gene	Action	Activity
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Hmgcr	unknown	IC50 8.52
3-hydroxy-3-methylglutaryl-coenzyme A reductase	HMGCR	inhibitor	IC50 7.67
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Hmgcr	unknown	IC50 7.57
Hydroxycarboxylic acid receptor 2	HCAR2	unknown	IC50 7.30
Hydroxycarboxylic acid receptor 3	HCAR3	unknown	IC50 6.53
Nuclear receptor subfamily 1 group I member 2	NR1I2	agonist	EC50 6.00
Cholinesterase	BCHE	unknown	Ki 5.96
Acetylcholinesterase	ache	unknown	Ki 5.57
Sodium-dependent dopamine transporter	SLC6A3	unknown	Ki 5.09
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Ki 5.06
Substance-K receptor	TACR2	unknown	Ki 5.03
Histone deacetylase 1	HDAC1	unknown	IC50 4.92
Leukocyte adhesion glycoprotein LFA-1 alpha	ITGAL	unknown	Kd 4.89
Adenosine receptor A1	ADORA1	unknown	Ki 4.81
Histone deacetylase 6	HDAC6	unknown	IC50 4.79
Acyl-CoA:cholesterol acyltransferase	ACAT	unknown	IC50 4.77
Androgen receptor	Ar	unknown	Ki 4.70
Histone deacetylase 2	HDAC2	unknown	IC50 4.59

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1987-08-31	FDA	—	MERCK

ATC classification

ATC code	Therapeutic hierarchy
C10AA02	CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, PLAIN › HMG CoA reductase inhibitors
C10BA01	CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, COMBINATIONS › Combinations of various lipid modifying agents

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Cardiac failure congestive	123.5
Rhabdomyolysis	116.1
Myalgia	116.0
Myocardial infarction	87.0
Synovitis	82.3
Infusion related reaction	80.3
Off label use	79.6
Cerebrovascular accident	79.5
Systemic lupus erythematosus	77.9
Pericarditis	72.2
Blood glucose increased	69.5
Atrial fibrillation	67.0

Chemical structure

• Molecular formula: C₂₄H₃₆O₅
• Molecular weight: 404.55 g/mol
• CAS number: —
• InChIKey: PCZOHLXUXFIOCF-BXMDZJJMSA-N
• PubChem CID: 53232

CC[C@H](C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@@H]12

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Lovastatin used for?

DrugCentral lists the following indications for Lovastatin: Arteriosclerotic vascular disease, Familial hypercholesterolemia - heterozygous, Hypercholesterolemia, Hyperlipidemia, Hypertriglyceridemia, Hypoalphalipoproteinemia, Mixed hyperlipidemia and Myocardial Infarction Prevention and others.

How does Lovastatin work?

Lovastatin is classified as Hydroxymethylglutaryl-CoA Reductase Inhibitors; its molecular targets in DrugCentral include Hmgcr, HMGCR (inhibitor), Hmgcr and HCAR2.

When was Lovastatin first approved?

Lovastatin was first approved by the FDA in 1987.

What drug class does Lovastatin belong to?

Lovastatin is in the HMG-CoA Reductase Inhibitor class.

What is the chemical formula of Lovastatin?

Lovastatin has the molecular formula C24H36O5 and a molecular weight of 404.55 g/mol.

Sources

• DrugCentral drug card 1612 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL503 — compound record and bioactivity
• PubChem CID 53232 — chemical identifiers
• DrugBank DB00227 — drug record
• FDA UNII 9LHU78OQFD — substance identity
• DailyMed: FDA labels for Lovastatin — current prescribing information (label search)
• UniProt P04035 (HMGCR) — target protein
• UniProt Q8TDS4 (HCAR2) — target protein
• UniProt P49019 (HCAR3) — target protein
• UniProt O75469 (NR1I2) — target protein
• UniProt Q01959 (SLC6A3) — target protein
• UniProt P23975 (SLC6A2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.