Pravastatin

Summary

Pravastatin (CHEMBL1144) is an approved small-molecule anticholesteremic drug (ATC C10AA03) targeting SLCO1B1 and HMGCR; indicated across 32 conditions including cardiovascular disorder and hepatocellular carcinoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C10AA03
• Targets: 2 (SLCO1B1, HMGCR)
• Indications: 32 conditions
• Clinical trials: 140
• Chemistry: 424.5 Da · C23H36O7

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1144
Name	Pravastatin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	54687
ChEBI	CHEBI:63618
ATC	C10AA03
Molecular formula	C23H36O7
Molecular weight	424.5
InChIKey	TUZYXOIXSAXUGO-PZAWKZKUSA-N

SMILES: CC[C@H](C)C(=O)O[C@H]1C[C@@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@H](C[C@H](CC(=O)O)O)O)O

IUPAC name: (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6-hydroxy-2-methyl-8-[(2S)-2-methylbutanoyl]oxy-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid

ChEBI definition: A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.

Pharmacological roles (ChEBI): anticholesteremic drug.

Other ChEBI roles (chemical / environmental): metabolite, xenobiotic, environmental contaminant.

Also known as: C10AA03, Pravastatin, Pravastatina, Pravastatine, Pravator, pravastatin, Pravastatin (acid), PRAVASTATINE, PRAVASTATIN, PRAVASTATIN SODIUM

Parent form; salt/anhydrous children: CHEMBL690

Patent coverage: 18,730 distinct patent families (70,953 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
SLCO1B1	OATP1B1	Binding		0%	Q9Y6L6
HMGCR	hydroxymethylglutaryl-CoA reductase	Competitive	5.86	84.4%	P04035

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Organic anion transporter 3, Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, Solute carrier family 22 member 6, Organic anion transporter 3, 3-hydroxy-3-methylglutaryl-coenzyme A reductase, 3-hydroxy-3-methylglutaryl-coenzyme A reductase.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 12 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HMGCR	8.25	IC50	5.59	nM	CHEMBL_ACT_7719803
P51639	7.89	IC50	13	nM	CHEMBL_ACT_2064275
HMGCR	7.52	IC50	30	nM	CHEMBL_ACT_1127937
P51639	7.5	IC50	31.6	nM	CHEMBL_ACT_2218032
HMGCR	6.4	IC50	400	nM	CHEMBL_ACT_16667277
SLCO1B1	5.47	Ki	3400	nM	CHEMBL_ACT_12088885
SLCO1B1	5.44	IC50	3600	nM	CHEMBL_ACT_12088886

Target pathways

Aggregated over 2 target gene(s): SLCO1B1, HMGCR.

Top Reactome pathways

22 total, by targets touching each:

Pathway	Targets	Genes
Metabolism	1	SLCO1B1
Recycling of bile acids and salts	1	SLCO1B1
Disease	1	SLCO1B1
Metabolism of porphyrins	1	SLCO1B1
Heme degradation	1	SLCO1B1
Cholesterol biosynthesis	1	HMGCR
Bile acid and bile salt metabolism	1	SLCO1B1
PPARA activates gene expression	1	HMGCR
Activation of gene expression by SREBF (SREBP)	1	HMGCR
Transport of small molecules	1	SLCO1B1
Transport of vitamins, nucleosides, and related molecules	1	SLCO1B1
SLC-mediated transmembrane transport	1	SLCO1B1
Metabolism of lipids	1	SLCO1B1
SLC transporter disorders	1	SLCO1B1
Defective SLCO1B1 causes hyperbilirubinemia, Rotor type (HBLRR)	1	SLCO1B1
Disorders of transmembrane transporters	1	SLCO1B1
Organic anion transport by SLCO transporters	1	SLCO1B1
Metabolism of steroids	1	SLCO1B1
EGR2 and SOX10-mediated initiation of Schwann cell myelination	1	HMGCR
Drug ADME	1	SLCO1B1
Atorvastatin ADME	1	SLCO1B1
Lanosterol biosynthesis	1	HMGCR

Dominant GO biological processes

GO term	Targets
xenobiotic metabolic process	1
monoatomic ion transport	1
obsolete organic anion transport	1
bile acid and bile salt transport	1
heme catabolic process	1
sodium-independent organic anion transport	1
lipid transport	1
prostaglandin transport	1
transmembrane transport	1
thyroid hormone transport	1
cholesterol biosynthetic process	1
isoprenoid biosynthetic process	1
visual learning	1
coenzyme A metabolic process	1
sterol biosynthetic process	1

Indications & clinical

Indications

32 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
hepatocellular carcinoma	3	MONDO:0007256	EFO:0000182
hypertensive disorder	3	MONDO:0005044	EFO:0000537
preeclampsia	3	MONDO:0005081	EFO:0000668
chronic kidney disease	3	MONDO:0005300	EFO:0003884
relapsing-remitting multiple sclerosis	3	MONDO:0005314	EFO:0003929
myocardial ischemia	3	MONDO:0024644	EFO:1001375
autosomal dominant polycystic kidney disease	3	MONDO:0004691	EFO:1001496
diabetes mellitus	3	MONDO:0005015	EFO:0000400
myocardial infarction	3	MONDO:0005068	EFO:0000612
heart failure	3	MONDO:0005252	EFO:0003144
hyperlipidemia	3	MONDO:0021187	MONDO:0021187
carcinoma	2	MONDO:0004993	EFO:0000313
Kawasaki disease	2	MONDO:0012727	EFO:0004246
pulmonary tuberculosis	2	MONDO:0006052	EFO:1000049
breast neoplasm	2	MONDO:0021100	MONDO:0007254
progeroid syndrome	2	MONDO:0015333	MONDO:0020732
tuberculosis	2	MONDO:0018076	MONDO:0018076
cardiomyopathy	2	MONDO:0004994	EFO:0000318
systemic lupus erythematosus	2	MONDO:0007915	MONDO:0007915
leukemia	1	MONDO:0005059	EFO:0000565
rheumatoid arthritis	1	MONDO:0008383	EFO:0000685
HIV infectious disease	1	MONDO:0005109	EFO:0000764
acute kidney injury	1	MONDO:0002492	HP:0001919
pneumonia	0	MONDO:0005249	EFO:0003106

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

Clinical trials

Total trials: 140.

Phase distribution

Phase	Trials
PHASE4	37
PHASE1	34
PHASE2	27
PHASE3	23
Not specified	16
PHASE1/PHASE2	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03273413	PHASE4	ACTIVE_NOT_RECRUITING	Statin Therapy in Patients With Early Stage ADPKD
NCT06785727	PHASE4	NOT_YET_RECRUITING	StAtins in Frail OldEr Patients with Ischemic Stroke or Transient Ischemic Attack - the Randomized Controlled Trial
NCT00117494	PHASE4	COMPLETED	Rosuvastatin Versus Pravastatin in HIV Patients Treated With Boosted Protease Inhibitors (PI) (ANRS126)
NCT00177580	PHASE4	COMPLETED	Improving Symptoms of Schizophrenia and Schizoaffective Disorder by Supplementing Medications With Pravastatin
NCT00211705	PHASE4	COMPLETED	Management of Elevated Cholesterol in the Primary Prevention Group of Adult Japanese(MEGA Study)
NCT00227500	PHASE4	COMPLETED	Pravastatin for Hyperlipidaemia in HIV.
NCT00303277	PHASE4	COMPLETED	Do HMG CoA Reductase Inhibitors Affect Abeta Levels?
NCT00330980	PHASE4	COMPLETED	Effects of Statin Medications on Mental Processes, Behavior, and Serotonin Levels
NCT00380939	PHASE4	COMPLETED	This Study Uses Ultrasound to Determine Whether Atorvastatin or Pravastatin Effects the Progression of Coronary Plaque.
NCT00382460	PHASE4	COMPLETED	Pravastatin or Atorvastatin Evaluation and Infection Therapy (TIMI22)
NCT00384618	PHASE4	TERMINATED	Anti-Oxidant Therapy In Chronic Renal Insufficiency (ATIC) Study
NCT00402376	PHASE4	TERMINATED	Evaluation of Myocardial Improvement in Patients Supported by Ventricular Assist Device Under Optimal Pharmacological Therapy
NCT00405717	PHASE4	COMPLETED	Effects of Atorvastatin Versus Pravastatin on Platelet Inhibition by Clopidogrel
NCT00529178	PHASE4	COMPLETED	Pravastatin Efficacy and Safety Trial in Hypercholesterolemic Patients With Chronic Liver Disease
NCT00549926	PHASE4	COMPLETED	Yokohama Assessment of Fluvastatin, Pravastatin, Pitavastatin and Atorvastatin in Acute Coronary Syndrome (Yokohama-ACS)
NCT00630734	PHASE4	COMPLETED	Genetic Predictors of Variability in the Drug-drug Interaction Between Darunavir/Ritonavir and Pravastatin
NCT00631189	PHASE4	COMPLETED	Evaluation of the Efficacy and Safety of Rosuvastatin 5 mg Versus Pravastatin 40 mg and Atorvastatin 10 mg in Type IIa and IIb Hypercholesterolaemic Patients
NCT00688922	PHASE4	UNKNOWN	Pravastatin for Acute Myocardial Infarction With Minimally to Mildly Increased Levels of Serum Cholesterol Study
NCT00701285	PHASE4	COMPLETED	South Korean Pitavastatin Heart Failure Study
NCT00738296	PHASE4	COMPLETED	Vytorin on Carotid Intima-media Thickness and Overall Rigidity
NCT00755352	PHASE4	COMPLETED	A Study to Determine the Effect of WelChol Tablets on Cholesterol in Patients Who Have Been Taking Pravastatin for at Least 4 Weeks.
NCT00843661	PHASE4	UNKNOWN	Coadministration of Ezetimibe With Fenofibrate Versus Pravastatin Monotherapy for the Treatment of Hyperlipidaemia in HIV-infected Patients
NCT01038154	PHASE4	UNKNOWN	Study to Evaluate the Efficacy of Pravastatin on Survival and Recurrence of Advanced Gastroesophageal Cancer
NCT01082588	PHASE4	COMPLETED	Effects of Pravastatin on Cholesterol, Inflammation and Cognition in Schizophrenia
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
NCT01325818	PHASE4	UNKNOWN	The Effects of Pravastatin and Rosuvastatin on Coronary Plaques in Patients With Stable Angina Pectoris
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
NCT01816997	PHASE4	UNKNOWN	The Statins on Glucose Homeostasis in Subjects With Impaired Fasting Glucose
NCT01856374	PHASE4	COMPLETED	Serial EValuation of multiplE Coronary Artery Diseases by an Optical Coherence Tomography; Assessment of the Changes of de Novo Lesions and Comparisons of Neointimal Coverage Between Xience Prime® Versus Cypher SelectTM Stents; SEVEN-Xience Study
NCT01857843	PHASE4	COMPLETED	Early Effects of Intensive Lipid Lowering Treatment With Ezetimibe/ Simvastatin (Vytorin®) Assessed by Virtual Histology-Intravascular Ultrasound (VH-IVUS) and Optical Coherence Tomography (OCT) on Plaque Characteristics in Patients With Acute Coronary Syndrome
NCT02305355	PHASE4	COMPLETED	Efficacy and Safety of Prescription Omega-3 Fatty Acid Added to Stable Statin Therapy in Patients With Type 2 Diabetes and Hypertriglyceridemia
NCT02754739	PHASE4	COMPLETED	Effect of Pravastatin in the Subjects With Prediabetes or Early Diabetes
NCT02992548	PHASE4	COMPLETED	Effect of Pravastatin on Erythrocyte Membrane Fatty Acid Contents in Patients With Chronic Kidney Disease
NCT04640571	PHASE4	COMPLETED	Impact of Metformin and Polysorbate 80 on Drug Absorption and Disposition
NCT04719481	PHASE4	UNKNOWN	Pravastatin Reduces Acute Phase Response of Zoledronic Acid
NCT06357104	PHASE4	COMPLETED	Detoxification From the Lipid Tract
NCT00000539	PHASE3	COMPLETED	Arterial Disease Multifactorial Intervention Trial (ADMIT)
NCT00000542	PHASE3	COMPLETED	Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT)
NCT00005010	PHASE3	COMPLETED	Prevention of Kidney Transplant Rejection

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (4) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for pravastatin 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
Annotation of DPWG Guideline for pravastatin and SLCO1B1	DPWG	SLCO1B1

PharmGKB also curates 36 clinical and 177 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.

179 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
ATORVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR, SLCO1B1
LOVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR, SLCO1B1
SIMVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR, SLCO1B1
TANNIC ACID	ChEMBL + PubChem	Phase 4 (approved)	HMGCR, SLCO1B1
ATAZANAVIR	ChEMBL + PubChem	Phase 4 (approved)	SLCO1B1
ERLOTINIB	ChEMBL + PubChem	Phase 4 (approved)	SLCO1B1
OLMESARTAN MEDOXOMIL	ChEMBL + PubChem	Phase 4 (approved)	SLCO1B1
PITAVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR
RIFAMPIN	ChEMBL + PubChem	Phase 4 (approved)	SLCO1B1
ROSUVASTATIN	ChEMBL + PubChem	Phase 4 (approved)	HMGCR
VINBLASTINE	ChEMBL + PubChem	Phase 4 (approved)	SLCO1B1
BETA CAROTENE	ChEMBL	Phase 4 (approved)	SLCO1B1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	SLCO1B1
CARBENOXOLONE	ChEMBL	Phase 4 (approved)	SLCO1B1
CERIVASTATIN	ChEMBL	Phase 4 (approved)	HMGCR
CISAPRIDE	ChEMBL	Phase 4 (approved)	HMGCR
CLARITHROMYCIN	ChEMBL	Phase 4 (approved)	SLCO1B1
CYCLOSPORINE	ChEMBL	Phase 4 (approved)	SLCO1B1
DICLOXACILLIN	ChEMBL	Phase 4 (approved)	SLCO1B1
DIGOXIN	ChEMBL	Phase 4 (approved)	SLCO1B1
ELTROMBOPAG	ChEMBL	Phase 4 (approved)	SLCO1B1
ERYTHROMYCIN ESTOLATE	ChEMBL	Phase 4 (approved)	SLCO1B1
ERYTHROMYCIN ETHYLSUCCINATE	ChEMBL	Phase 4 (approved)	SLCO1B1
ESTRONE SULFURIC ACID	ChEMBL	Phase 4 (approved)	SLCO1B1
FLUVASTATIN	ChEMBL	Phase 4 (approved)	HMGCR
GEMFIBROZIL	ChEMBL	Phase 4 (approved)	SLCO1B1
GLYBURIDE	ChEMBL	Phase 4 (approved)	SLCO1B1
HYDROXYZINE PAMOATE	ChEMBL	Phase 4 (approved)	SLCO1B1
INDOMETHACIN	ChEMBL	Phase 4 (approved)	SLCO1B1
LOSARTAN	ChEMBL	Phase 4 (approved)	SLCO1B1
MOMETASONE FUROATE	ChEMBL	Phase 4 (approved)	SLCO1B1
NONOXYNOL 9	ChEMBL	Phase 4 (approved)	SLCO1B1
PACLITAXEL	ChEMBL	Phase 4 (approved)	SLCO1B1
RIFAMYCIN	ChEMBL	Phase 4 (approved)	SLCO1B1
RITONAVIR	ChEMBL	Phase 4 (approved)	SLCO1B1
SIROLIMUS	ChEMBL	Phase 4 (approved)	SLCO1B1
SULFASALAZINE	ChEMBL	Phase 4 (approved)	SLCO1B1
TACROLIMUS	ChEMBL	Phase 4 (approved)	SLCO1B1
TELITHROMYCIN	ChEMBL	Phase 4 (approved)	SLCO1B1
TELMISARTAN	ChEMBL	Phase 4 (approved)	SLCO1B1
VERAPAMIL	ChEMBL	Phase 4 (approved)	SLCO1B1
VINCRISTINE	ChEMBL	Phase 4 (approved)	SLCO1B1
ADMILPARANT	ChEMBL	Phase 3	SLCO1B1
ALISPORIVIR	ChEMBL	Phase 3	SLCO1B1
FASIGLIFAM	ChEMBL	Phase 3	SLCO1B1
GOSSYPOL	ChEMBL	Phase 3	SLCO1B1
PAMIPARIB	ChEMBL	Phase 3	SLCO1B1
SILIBININ	ChEMBL	Phase 3	SLCO1B1
SILYBIN A	ChEMBL	Phase 3	SLCO1B1
GLYCYRRHIZIN	ChEMBL + PubChem	Phase 2 (approved)	SLCO1B1
BMS-986020	ChEMBL	Phase 2	SLCO1B1
CLESACOSTAT	ChEMBL	Phase 2	SLCO1B1
ENOXOLONE	ChEMBL	Phase 2	SLCO1B1
GENISTEIN	ChEMBL	Phase 2	SLCO1B1
GLENVASTATIN	ChEMBL	Phase 2	HMGCR
MEGLUTOL	ChEMBL	Phase 2	HMGCR
MEVASTATIN	ChEMBL	Phase 2	HMGCR
MOLIBRESIB	ChEMBL	Phase 2	SLCO1B1
SILICRISTIN	ChEMBL	Phase 2	SLCO1B1
TENIVASTATIN	ChEMBL	Phase 2	SLCO1B1