Fluvastatin

Summary

Fluvastatin (CHEMBL2220442) is an approved small molecule (ATC C10AA04) targeting HMGCR; indicated across 12 conditions including cardiovascular disorder and erectile dysfunction.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C10AA04
• Targets: 1 (HMGCR)
• Indications: 12 conditions
• Clinical trials: 42
• Chemistry: 411.5 Da · C24H26FNO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2220442
Name	Fluvastatin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5353627
ChEBI	CHEBI:38562
ATC	C10AA04
Molecular formula	C24H26FNO4
Molecular weight	411.5
InChIKey	FJLGEFLZQAZZCD-VAWYXSNFSA-N

SMILES: CC(C)N1C2=CC=CC=C2C(=C1/C=C/C(CC(CC(=O)O)O)O)C3=CC=C(C=C3)F

IUPAC name: (E)-7-[3-(4-fluorophenyl)-1-propan-2-ylindol-2-yl]-3,5-dihydroxyhept-6-enoic acid

ChEBI definition: A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers.

Also known as: Fluvas, Fluvastatin, Fluvastatina, Fluvastatine, NSC-758896, fluvastatin, rel-Fluvastatin, FLUVASTATINE, SID144213082, Rel-Fluvastatin, rel-fluvastatin, FLUVASTATIN

Parent form; salt/anhydrous children: CHEMBL2218894

Patent coverage: 13,248 distinct patent families (53,699 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
HMGCR	hydroxymethylglutaryl-CoA reductase	Competitive	6.56	84.4%	P04035

Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: Cholecystokinin receptor type A, Retinoic acid receptor RXR-alpha, Thromboxane A2 receptor, Progesterone receptor, NAD-dependent protein deacylase sirtuin-6, Alpha-1A adrenergic receptor, Prostaglandin G/H synthase 2, Adenosine receptor A3, 3’,5’-cyclic-AMP phosphodiesterase 4D, 3-hydroxy-3-methylglutaryl-coenzyme A reductase.

Bioactivity

ChEMBL activities: 9 potent at pChembl ≥ 5 of 23 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HMGCR	9.45	IC50	0.35	nM	CHEMBL_ACT_7650959
P51639	8.52	IC50	3	nM	CHEMBL_ACT_2689638
HMGCR	7.55	IC50	28	nM	CHEMBL_ACT_1439882
CYP2C9	6.4	IC50	400	nM	CHEMBL_ACT_7650913
NR4A2	5.72	EC50	1900	nM	CHEMBL_ACT_24824513
NR4A2	5.72	EC50	1900	nM	CHEMBL_ACT_25540417
NR4A2	5.72	EC50	1900	nM	CHEMBL_ACT_25647234
SIRT6	5.15	EC50	7100	nM	CHEMBL_ACT_22901058
ADRA1A	5.15	AC50	7098	nM	CHEMBL_ACT_25137802

Target pathways

Aggregated over 1 target gene(s): HMGCR.

Top Reactome pathways

5 total, by targets touching each:

Pathway	Targets	Genes
Cholesterol biosynthesis	1	HMGCR
PPARA activates gene expression	1	HMGCR
Activation of gene expression by SREBF (SREBP)	1	HMGCR
EGR2 and SOX10-mediated initiation of Schwann cell myelination	1	HMGCR
Lanosterol biosynthesis	1	HMGCR

Dominant GO biological processes

GO term	Targets
cholesterol biosynthetic process	1
isoprenoid biosynthetic process	1
visual learning	1
coenzyme A metabolic process	1
sterol biosynthetic process	1
negative regulation of protein catabolic process	1
negative regulation of protein secretion	1
long-term synaptic potentiation	1
regulation of ERK1 and ERK2 cascade	1
negative regulation of amyloid-beta clearance	1
lipid metabolic process	1
steroid biosynthetic process	1
steroid metabolic process	1
cholesterol metabolic process	1

Indications & clinical

Indications

12 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
erectile dysfunction	3	MONDO:0005362	HP:0000802
aortic valve stenosis	2	MONDO:0042981	EFO:0000266
hepatitis C virus infection	2	MONDO:0005231	EFO:0003047
chronic hepatitis C virus infection	2	MONDO:0005354	EFO:0004220
hereditary nephritis	2	MONDO:0005334	MONDO:0018965
paraganglioma	1	MONDO:0000448	EFO:1000453
melanoma	0	MONDO:0005105	EFO:0000756

4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 42.

Phase distribution

Phase	Trials
PHASE4	19
PHASE3	8
PHASE2	7
Not specified	4
PHASE1	2
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06785727	PHASE4	NOT_YET_RECRUITING	StAtins in Frail OldEr Patients with Ischemic Stroke or Transient Ischemic Attack - the Randomized Controlled Trial
NCT00125125	PHASE4	COMPLETED	Fluvastatin in Adults With Dislipidemia With History of Muscle Problems
NCT00138528	PHASE4	COMPLETED	Other Effects of Fluvastatin Are Investigated in Patients With Metabolic Syndrome
NCT00171262	PHASE4	COMPLETED	Trial to Evaluate the Efficacy of Fluvastatin on Certain Markers
NCT00171275	PHASE4	COMPLETED	Fluvastatin in the Therapy of Acute Coronary Syndrome
NCT00171327	PHASE4	COMPLETED	Efficacy and Safety of Fluvastatin or Valsartan and Their Combination in Dyslipidemic Patients With Hypertension and Endothelial Dysfunction
NCT00223015	PHASE4	COMPLETED	Investigation of the Steady State Pharmacokinetics of Tacrolimus, Mycophenolate Mofetil and Fluvastatin After Renal Transplantation
NCT00223028	PHASE4	COMPLETED	Investigation of the Steady State Pharmacokinetics of Sirolimus, Mycophenolat Mofetil and Fluvastatin After Renal Transplantation
NCT00404287	PHASE4	TERMINATED	Randomized Study to Evaluate the Efficacy of Fluvastatin on Inflammatory Markers in Patients With Aortic Stenosis.
NCT00407680	PHASE4	UNKNOWN	Intensive Medical Treatment for Nephropathy Caused by Type 2 Diabetes With Hypertension
NCT00421005	PHASE4	UNKNOWN	Fluvastatin After Heart Transplantation
NCT00489424	PHASE4	COMPLETED	Acetaminophen or Fluvastatin Compared to Placebo on the Transient Post-Dose Symptoms (PDS) Following an Intravenous (i.v.) Infusion of a Single Dose of Zoledronic Acid 5mg, in Post-menopausal Women With Low Bone Mass
NCT00549926	PHASE4	COMPLETED	Yokohama Assessment of Fluvastatin, Pravastatin, Pitavastatin and Atorvastatin in Acute Coronary Syndrome (Yokohama-ACS)
NCT00565474	PHASE4	COMPLETED	Evaluation of the Effect of Fluvastatin 40 mg (b.i.d.) in the Prevention of the Development of Vasculopathy of the Graft in de Novo Renal Transplant Patients Transplant
NCT00664742	PHASE4	COMPLETED	The Effect of Fluvastatin XL® Treatment in Patients With Metabolic Syndrome
NCT00814723	PHASE4	COMPLETED	Fluvastatin 80 mg Ret. vs Combination With Ezetimibe 10 mg in Patients With High Cardiovascular Risk
NCT00821574	PHASE4	COMPLETED	Reducing the Overall Risk Level in Patients Suffering From Metabolic Syndrome
NCT03189511	PHASE4	COMPLETED	Effect of Fluvastatin on Brown Fat Activity
NCT04029584	PHASE4	COMPLETED	Drug-Drug Interaction Between Rifampin and Fluvastatin
NCT00132717	PHASE3	COMPLETED	A 12 Week Study of MK0653A in Patients Who Have Been Hospitalized for a Possible Heart Problem (0653A-808)
NCT00136799	PHASE3	COMPLETED	Efficacy and Safety of Fluvastatin in Different Doses in Adults With Mixed Dyslipidemia or Primary Hypercholesterolemia
NCT00171236	PHASE3	COMPLETED	Efficacy and Safety of Fluvastatin in Children With Heterozygous Familial Hypercholesterolemia
NCT00171288	PHASE3	COMPLETED	Efficacy and Safety Study of Fluvastatin and Ezetimibe Combined Versus Fluvastatin Alone
NCT00199927	PHASE3	COMPLETED	Statins in Proteinuric Nephropathies
NCT00223041	PHASE2/PHASE3	TERMINATED	Cranoc Lipid Study in Renal Transplantation
NCT00718796	PHASE3	COMPLETED	Naturopathic Treatment for the Prevention of Cardiovascular Disease
NCT03510715	PHASE3	COMPLETED	An Efficacy and Safety Study of Alirocumab in Children and Adolescents With Homozygous Familial Hypercholesterolemia
NCT03510884	PHASE3	COMPLETED	An Efficacy and Safety Study of Alirocumab in Children and Adolescents With Heterozygous Familial Hypercholesterolemia
NCT00176410	PHASE2	UNKNOWN	Statin Therapy in Asymptomatic Aortic Stenosis
NCT00309257	PHASE2	COMPLETED	Effects of an Intensified Treatment With ACE-I,ATA II and Statins in Alport Syndrome
NCT00487318	PHASE2	COMPLETED	Fluvastatin, Rosuvastatin Added to Pegylated Interferon and Ribavirin
NCT00674297	PHASE2	COMPLETED	Effects of Fluvastatin on Proinflammatory and Prothrombotic Markers in Antiphospholipid Syndrome Patients
NCT00814606	PHASE2	WITHDRAWN	A Pilot Trial to Determine the Safety and Efficacy of Fluvastatin in Previous Partial Responders to Pegylated Interferon and Ribivirin in Patients With Genotype 1 Hepatitis C
NCT01045512	PHASE2	TERMINATED	The Role of the Inflammatory/ Pathogen Burden for Cardiac Ageing
NCT01992042	PHASE2	COMPLETED	Novel Window of Opportunity Trial to Evaluate the Impact of Statins to Oppose Prostate Cancer
NCT00752843	PHASE1	COMPLETED	A Phase I Study to Determine the Effect of Mifepristone on the Pharmacokinetics of Fluvastatin in Healthy Volunteers
NCT02115074	PHASE1	COMPLETED	Safety of Fluvastatin-Celebrex Association in Low-grade and High Grade Optico-chiasmatic Gliomas
NCT04285749	EARLY_PHASE1	WITHDRAWN	Prevention of Recurrence and Metastasis in Genetically High-Risk Melanomas
NCT00441493	Not specified	COMPLETED	Fluvastatin Versus Hepatitis C Virus
NCT00465322	Not specified	COMPLETED	Effect of Fluvastatin on Top of Clopidogrel and Aspirin in Patients After DES Implantation on Platelet Aggregation

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
ATORVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR
LOVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR
PITAVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR
PRAVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR
ROSUVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR
SIMVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR
CERIVASTATIN	ChEMBL	Phase 4 (approved)	HMGCR
CISAPRIDE	ChEMBL	Phase 4 (approved)	HMGCR
TANNIC ACID	ChEMBL	Phase 4 (approved)	HMGCR
GLENVASTATIN	ChEMBL	Phase 2	HMGCR
MEGLUTOL	ChEMBL	Phase 2	HMGCR
MEVASTATIN	ChEMBL	Phase 2	HMGCR
Vorinostat	PubChem	Approved	HMGCR