Fluvastatin

HMG-CoA Reductase Inhibitor — CARDIOVASCULAR SYSTEM

Key facts

Fluvastatin is an ofp drug in the HMG-CoA Reductase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 1993. Its mechanism of action is classified as Hydroxymethylglutaryl-CoA Reductase Inhibitors. DrugCentral lists 8 molecular targets, including Hmgcr, HMGCR and CYP2C9. Recorded indications include Arteriosclerotic vascular disease, Familial hypercholesterolemia - heterozygous, Hypercholesterolemia and Mixed hyperlipidemia.

• Approval status: ofp (first approved 1993 by the FDA).
• Drug class: HMG-CoA Reductase Inhibitor.
• Mechanism of action: Hydroxymethylglutaryl-CoA Reductase Inhibitors.
• Molecular targets: Hmgcr, HMGCR, CYP2C9 and NR4A2 (8 listed in DrugCentral).
• Indications: Arteriosclerotic vascular disease, Familial hypercholesterolemia - heterozygous, Hypercholesterolemia, Mixed hyperlipidemia and Slow Progression of Coronary Artery Disease.
• ATC code: C10AA04 (HMG CoA reductase inhibitors).
• Molecular formula: C24H26FNO4; molecular weight 411.47 g/mol.

Indications & contraindications

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

Indications (5)

• Arteriosclerotic vascular disease
• Familial hypercholesterolemia - heterozygous
• Hypercholesterolemia
• Mixed hyperlipidemia
• Slow Progression of Coronary Artery Disease

Off-label uses (4)

• Cerebrovascular accident
• Myocardial Infarction Prevention
• Prevention of Transient Ischemic Attacks
• Primary Prevention of Coronary Heart Disease

Contraindications (13)

• Acute nephropathy
• Alcoholism
• Breastfeeding (mother)
• Disease of liver
• Disorder of muscle
• Hemorrhagic cerebral infarction
• Liver function tests abnormal
• Low blood pressure
• Pregnancy, function
• Rhabdomyolysis
• Surgical procedure
• Traumatic injury
• Uncontrolled Epilepsy

Mechanism & targets

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

Molecular targets (8)

Target	Gene	Action	Activity
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Hmgcr	unknown	IC50 8.60
3-hydroxy-3-methylglutaryl-coenzyme A reductase	HMGCR	inhibitor	IC50 7.55
Cytochrome P450 2C9	CYP2C9	unknown	IC50 6.40
Nuclear receptor subfamily 4 group A member 2	NR4A2	unknown	EC50 5.72
NAD-dependent protein deacetylase sirtuin-6	SIRT6	unknown	EC50 5.15
Retinoic acid receptor RXR-alpha	RXRA	unknown	Kd 4.96
Sodium/bile acid cotransporter	SLC10A1	unknown	IC50 4.40
Nuclear receptor subfamily 1 group I member 3	NR1I3	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1993-12-31	FDA	—	NOVARTIS

ATC classification

ATC code	Therapeutic hierarchy
C10AA04	CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, PLAIN › HMG CoA reductase inhibitors

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
Myalgia	845.8
Amaurosis fugax	657.5
Ocular discomfort	579.0
Haemorrhagic stroke	572.6
Urinary tract disorder	528.5
Head discomfort	491.2
Generalised oedema	449.9
Blindness	402.1
Presyncope	391.5
Haematemesis	368.5
Eye pain	366.1
Altered state of consciousness	355.3

Chemical structure

• Molecular formula: C₂₄H₂₆FNO₄
• Molecular weight: 411.47 g/mol
• CAS number: 93957-54-1
• InChIKey: FJLGEFLZQAZZCD-JUFISIKESA-N
• PubChem CID: 1548972

CC(C)N1C(\C=C\[C@H](O)C[C@H](O)CC(O)=O)=C(C2=C1C=CC=C2)C1=CC=C(F)C=C1

Frequently asked questions

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

What is Fluvastatin used for?

DrugCentral lists the following indications for Fluvastatin: Arteriosclerotic vascular disease, Familial hypercholesterolemia - heterozygous, Hypercholesterolemia, Mixed hyperlipidemia and Slow Progression of Coronary Artery Disease.

How does Fluvastatin work?

Fluvastatin is classified as Hydroxymethylglutaryl-CoA Reductase Inhibitors; its molecular targets in DrugCentral include Hmgcr, HMGCR (inhibitor), CYP2C9 and NR4A2.

When was Fluvastatin first approved?

Fluvastatin was first approved by the FDA in 1993.

What drug class does Fluvastatin belong to?

Fluvastatin is in the HMG-CoA Reductase Inhibitor class.

What is the chemical formula of Fluvastatin?

Fluvastatin has the molecular formula C24H26FNO4 and a molecular weight of 411.47 g/mol.

Sources

• DrugCentral drug card 1229 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2218894 — compound record and bioactivity
• PubChem CID 1548972 — chemical identifiers
• DrugBank DB01095 — drug record
• FDA UNII 4L066368AS — substance identity
• DailyMed: FDA labels for Fluvastatin — current prescribing information (label search)
• UniProt P04035 (HMGCR) — target protein
• UniProt P11712 (CYP2C9) — target protein
• UniProt P43354 (NR4A2) — target protein
• UniProt Q8N6T7 (SIRT6) — target protein
• UniProt P19793 (RXRA) — target protein
• UniProt Q14973 (SLC10A1) — 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.