Pitavastatin

Summary

Pitavastatin (CHEMBL1201753) is an approved small-molecule antioxidant (ATC C10AA08) targeting HMGCR; indicated across 11 conditions including cardiovascular disorder and coronary artery disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C10AA08
• Targets: 1 (HMGCR)
• Indications: 11 conditions
• Clinical trials: 70
• Chemistry: 421.5 Da · C25H24FNO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201753
Name	Pitavastatin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5282452
ChEBI	CHEBI:32020
ATC	C10AA08
Molecular formula	C25H24FNO4
Molecular weight	421.5
InChIKey	VGYFMXBACGZSIL-MCBHFWOFSA-N

SMILES: C1CC1C2=NC3=CC=CC=C3C(=C2/C=C/[C@H](C[C@H](CC(=O)O)O)O)C4=CC=C(C=C4)F

IUPAC name: (E,3R,5S)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid

ChEBI definition: A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise.

Pharmacological roles (ChEBI): antioxidant.

Also known as: NSC-760423, Pitavastatin, Pitavastatina, Pitavastatine, PITAVASTATINE, PITAVASTATIN, pitavastatin

Parent form; salt/anhydrous children: CHEMBL1237061, CHEMBL3989920, CHEMBL3989923

Patent coverage: 6,195 distinct patent families (24,149 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 24,025 (99%) of the total. 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	Inhibition	5.05	84.4%	P04035

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: 3’,5’-cyclic-AMP phosphodiesterase 4D, 3-hydroxy-3-methylglutaryl-coenzyme A reductase, Nuclear receptor subfamily 1 group I member 2, Nuclear receptor subfamily 4 group A member 2.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
P51639	8.39	IC50	4.1	nM	CHEMBL_ACT_16742548
NR4A2	6.92	EC50	120	nM	CHEMBL_ACT_24824514
NR4A2	6.92	EC50	120	nM	CHEMBL_ACT_25647235
PDE4D	6.17	AC50	670	nM	CHEMBL_ACT_25185712
PDE4D	6.03	AC50	930	nM	CHEMBL_ACT_25185707

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

11 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
coronary artery disorder	3	MONDO:0005010	EFO:0001645
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148
hyperlipidemia	3	MONDO:0021187	MONDO:0021187
breast neoplasm	2	MONDO:0021100	MONDO:0007254
metabolic syndrome X	1	MONDO:0011565	EFO:0000195
influenza	1	MONDO:0005812	EFO:0007328
kidney failure	1	MONDO:0001106	HP:0000083

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

Clinical trials

Total trials: 70.

Phase distribution

Phase	Trials
PHASE4	29
PHASE1	16
PHASE3	15
Not specified	9
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05537948	PHASE4	ACTIVE_NOT_RECRUITING	Efficacy and Safety of Pitavastatin and PCSK9 Inhibitors in Liver Transplant Patients
NCT07442630	PHASE4	ACTIVE_NOT_RECRUITING	Long-term Comparison of Pitavastatin/Ezetimibe and Pitavastatin in Patients With Hypercholesterolemia and Elevated Triglycerides
NCT00242944	PHASE4	COMPLETED	Japan Assessment of Pitavastatin and Atorvastatin in Acute Coronary Syndrome (JAPAN-ACS)
NCT00444717	PHASE4	COMPLETED	Impact of Pitavastatin in Hypercholesterolemic Patients With Metabolic Syndrome
NCT00549926	PHASE4	COMPLETED	Yokohama Assessment of Fluvastatin, Pravastatin, Pitavastatin and Atorvastatin in Acute Coronary Syndrome (Yokohama-ACS)
NCT00640276	PHASE4	COMPLETED	Safety and Efficacy Study of Pitavastatin in Patient With a Metabolic Syndrome
NCT00701285	PHASE4	COMPLETED	South Korean Pitavastatin Heart Failure Study
NCT00786734	PHASE4	WITHDRAWN	Pitavastatin Pre-Treatment Study in Patient With Elective PCI for Stable Angina Pectoris (PIPA)
NCT00861861	PHASE4	COMPLETED	Comparison of Pitavastatin With Atorvastatin in Increasing High Density Lipoprotein - Cholesterol (HDL-C) and Adiponectin in Patients With Dyslipidemia and Coronary Artery Disease (CAD)
NCT00889226	PHASE4	COMPLETED	Efficacy and Safety Study of Pitavastatin Compared to atoRvastatin in Type 2 dIabeTes Mellitus With Hypercholesterolemia
NCT01043094	PHASE4	COMPLETED	Safety, Tolerability, and Pharmacokinetic of Single Dose of Pitavastatin 4 mg in Severe Renal Patients Versus Healthy Adult Volunteers
NCT01057433	PHASE4	COMPLETED	Drug-Drug Interaction of Lopinavir/Ritonavir on Pitavastatin
NCT01166633	PHASE4	COMPLETED	Efficacy and Safety Study of Pitavastatin Versus Atorvastatin to Treat Hypercholesterolemia
NCT01256476	PHASE4	COMPLETED	Prevail-Us: A Study Of Pitavastatin 4 mg Vs. Pravastatin 40 mg In Patients With Primary Hyperlipidemia Or Mixed Dyslipidemia
NCT01301066	PHASE4	COMPLETED	A 12-Week Study Comparing Pitavastatin 4 mg vs. Pravastatin 40 mg in HIV-Infected Subjects
NCT01422369	PHASE4	COMPLETED	Drug-Drug Interaction of Darunavir/Ritonavir on Pitavastatin
NCT01422382	PHASE4	COMPLETED	Drug-Drug Interaction of Cardizem LA (Diltiazem Hydrochloride) on Pitavastatin
NCT01502904	PHASE4	COMPLETED	Neointimal Coverage After Implantation of Biolimus Eluting Stent With Biodegradable Polymer: Optical Coherence Tomographic Assessment According to the Treatment of Dyslipidemia and Hypertension and the Types of Implanted Drug-eluting Stents
NCT01648829	PHASE4	UNKNOWN	PharmacOdynamic compaRison of piTavastatin Versus atOrvastatin on Platelet Reactivity
NCT01871792	PHASE4	UNKNOWN	Preventive Effect of Pitavastatin on Contrast-Induced Nephropathy in Patients With Renal Dysfunction
NCT02056847	PHASE4	COMPLETED	to Evaluate the Safety and Efficacy of Pitavastatin in Patients With IFG and Hyperlipidemia
NCT02144922	PHASE4	COMPLETED	Effect of Pitavastatin on Coronary Flow Reserve in Hypertensive Patients
NCT02442700	PHASE4	COMPLETED	Effects of Pitavastatin on Lipid Profiles in HIV-infected Patients With Dyslipidemia and Receiving Atazanavir/Ritonavir
NCT02545231	PHASE4	COMPLETED	Effect of Low-dose vs. High-dose Pitavastatin on In-stent Restenosis
NCT02743260	PHASE4	COMPLETED	Drug Transporter Interaction Study PHENTRA_2015_KPUK
NCT02863185	PHASE4	COMPLETED	Effect of Pitavastatin on Erythrocyte Membrane Fatty Acid Contents in Patients With Chronic Kidney Disease
NCT03418974	PHASE4	UNKNOWN	Safety and Efficacy of Statins for Chinese Patients With Dyslipidemia
NCT04945122	PHASE4	UNKNOWN	Comparison of Atorvastatin and Pitavastatin on the Effect of HbA1c in AMI Patients With Abnormal Glucose Metabolism
NCT06359353	PHASE4	COMPLETED	Effect of Pitavastatin on Bone
NCT00249249	PHASE3	COMPLETED	Study to Compare the Efficacy of Pitavastatin With That of Atorvastatin in Lowering Cholesterol Levels
NCT00257686	PHASE3	COMPLETED	Study to Compare the Efficacy and Safety of Pitavastatin and Pravastatin in Elderly Patients
NCT00309738	PHASE3	COMPLETED	Study to Compare the Efficacy and Safety of Pitavastatin and Simvastatin
NCT00309751	PHASE3	COMPLETED	Study Comparing Pitavastatin and Atorvastatin in Patients With Type II Diabetes Mellitus and Combined Dyslipidemia
NCT00309777	PHASE3	COMPLETED	Study to Compare the Efficacy and Safety of Pitavastatin and Simvastatin
NCT00325780	PHASE3	COMPLETED	Long-Term Extension Study of Pitavastatin in Patients With Primary Hypercholesterolemia or Combined Dyslipidemia
NCT00330876	PHASE3	COMPLETED	Study of Pitavastatin in Elderly Patients With Primary Hypercholesterolemia or Combined Dyslipidemia
NCT00344175	PHASE3	COMPLETED	Follow-on Protocol of Pitavastatin Versus Simvastatin in Patients With Hypercholesterolemia or Dyslipidemia and Coronary Heart Disease Risk Factors
NCT00344370	PHASE3	COMPLETED	Follow-On Study of Pitavastatin Versus Atorvastatin in Patients With Type II Diabetes Mellitus and Combined Dyslipidemia
NCT01386853	PHASE3	UNKNOWN	Efficacy and Safety Study of Pitavastatin and Atorvastatin in High Risk Hypercholesterolemic Patients
NCT01402843	PHASE3	COMPLETED	Efficacy, Safety of Coadministered Pitavastatin and Valsartan in Patients With Hypertension and Dyslipidemia

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (3) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for pitavastatin and SLCO1B1	CPIC	SLCO1B1	yes	yes
Annotation of CPIC Guideline for atorvastatin, fluvastatin, lovastatin	CPIC	ABCG2
Annotation of CPIC Guideline for atorvastatin, fluvastatin, lovastatin	CPIC	CYP3A4;CYP3A5;HMGCR

PharmGKB also curates 4 clinical and 26 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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
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
FLUVASTATIN	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