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Rosuvastatin

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Also known as CrestonRosuvastatinaRosuvastatineX-plendedZD-4522ZD4522[3H]-RosuvastatinROSUVASTATIN CALCIUM

Summary

Rosuvastatin (CHEMBL1496) is an approved small-molecule antilipemic drug (ATC C10AA07) targeting HMGCR; indicated across 79 conditions including cardiovascular disorder and hiv infectious disease.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C10AA07
  • Targets: 1 (HMGCR)
  • Indications: 79 conditions
  • Clinical trials: 592
  • Chemistry: 481.5 Da · C22H28FN3O6S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1496
NameRosuvastatin
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID446157
ChEBICHEBI:38545
ATCC10AA07
Molecular formulaC22H28FN3O6S
Molecular weight481.5
InChIKeyBPRHUIZQVSMCRT-VEUZHWNKSA-N

SMILES: CC(C)C1=NC(=NC(=C1/C=C/[C@H](C[C@H](CC(=O)O)O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C

IUPAC name: (E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid

ChEBI definition: A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer).

Pharmacological roles (ChEBI): antilipemic drug, anti-inflammatory agent, CETP inhibitor, cardioprotective agent.

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

Also known as: Creston, Rosuvastatin, Rosuvastatina, Rosuvastatine, X-plended, ZD-4522, ZD4522, rosuvastatin, ROSUVASTATINE, [3H]-Rosuvastatin, ROSUVASTATIN, ROSUVASTATIN CALCIUM

Parent form; salt/anhydrous children: CHEMBL1744447

Patent coverage: 10,555 distinct patent families (41,471 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 41,457 (100%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
HMGCRhydroxymethylglutaryl-CoA reductaseCompetitive8.2784.4%P04035

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

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 17 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
HMGCR9.05Ki0.9nMCHEMBL_ACT_1436566
P516398.68IC502.1nMCHEMBL_ACT_2042755
HMGCR8.51IC503.1nMCHEMBL_ACT_2036447
P516398.51IC503.1nMCHEMBL_ACT_2064274
P516398.51IC503.1nMCHEMBL_ACT_2218035
P516398.51IC503.1nMCHEMBL_ACT_6231546
P516398.44IC503.6nMCHEMBL_ACT_1974260
P516398.43IC503.7nMCHEMBL_ACT_2075561
P516398.4IC504nMCHEMBL_ACT_17678545
HMGCR8.4IC504nMCHEMBL_ACT_17699513
HMGCR8.3IC505nMCHEMBL_ACT_1439885
HMGCR8.27IC505.4nMCHEMBL_ACT_1436567
HMGCR7.77Kd17nMCHEMBL_ACT_2445502
PDE6D5.9Kd1250nMCHEMBL_ACT_14727871
NR1I25.44AC503600nMCHEMBL_ACT_25188260
PDE4D5.38AC504157nMCHEMBL_ACT_25185454

Target pathways

Aggregated over 1 target gene(s): HMGCR.

Top Reactome pathways

5 total, by targets touching each:

PathwayTargetsGenes
Cholesterol biosynthesis1HMGCR
PPARA activates gene expression1HMGCR
Activation of gene expression by SREBF (SREBP)1HMGCR
EGR2 and SOX10-mediated initiation of Schwann cell myelination1HMGCR
Lanosterol biosynthesis1HMGCR

Dominant GO biological processes

GO termTargets
cholesterol biosynthetic process1
isoprenoid biosynthetic process1
visual learning1
coenzyme A metabolic process1
sterol biosynthetic process1
negative regulation of protein catabolic process1
negative regulation of protein secretion1
long-term synaptic potentiation1
regulation of ERK1 and ERK2 cascade1
negative regulation of amyloid-beta clearance1
lipid metabolic process1
steroid biosynthetic process1
steroid metabolic process1
cholesterol metabolic process1

Indications & clinical

Indications

79 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).

IndicationTrial phaseMONDOEFO
cardiovascular disorder4MONDO:0004995EFO:0000319
HIV infectious disease3MONDO:0005109EFO:0000180
metabolic syndrome X3MONDO:0011565EFO:0000195
aortic valve stenosis3MONDO:0042981EFO:0000266
congestive heart failure3MONDO:0005009EFO:0000373
dilated cardiomyopathy3MONDO:0005021EFO:0000407
hypertensive disorder3MONDO:0005044EFO:0000537
stroke disorder3MONDO:0005098EFO:0000712
systemic sclerosis3MONDO:0005100EFO:0000717
obesity disorder3MONDO:0011122EFO:0001073
coronary artery disorder3MONDO:0005010EFO:0001645
heart failure3MONDO:0005252EFO:0003144
atherosclerosis3MONDO:0005311EFO:0003914
hip fracture3MONDO:0005327EFO:0003964
anti-neutrophil antibody associated vasculitis3MONDO:0005435EFO:0004826
familial hypercholesterolemia3MONDO:0005439EFO:0004911
acute coronary syndrome3MONDO:0005542EFO:0005672
metabolic dysfunction-associated steatohepatitis3MONDO:0007027EFO:1001249
kidney failure3MONDO:0001106EFO:1002048
severe acute respiratory syndrome3MONDO:0005091MONDO:0100096
hyperlipidemia3MONDO:0021187MONDO:0021187
metabolic dysfunction-associated steatotic liver disease3MONDO:0013209EFO:0003095
colorectal neoplasm3MONDO:0005335MONDO:0005575
chronic obstructive pulmonary disease2MONDO:0005002EFO:0000341
diabetes mellitus2MONDO:0005015EFO:0000400
ischemic disease2MONDO:0005053EFO:0000556
periodontitis2MONDO:0005076EFO:0000649
preeclampsia2MONDO:0005081EFO:0000668
rheumatoid arthritis2MONDO:0008383EFO:0000685
hepatitis C virus infection2MONDO:0005231EFO:0003047
venous thromboembolism2MONDO:0005399EFO:0004286
swine influenza2MONDO:0005460EFO:0005226
intracerebral hemorrhage2MONDO:0013792EFO:0005669
rectal cancer2MONDO:0006519EFO:1000657
burn2MONDO:0043519EFO:0009516
renal artery obstruction2MONDO:0006945EFO:1001150
diabetic neuropathy2MONDO:0006626MONDO:0001583
breast neoplasm2MONDO:0021100MONDO:0007254
ovarian cancer2MONDO:0008170MONDO:0008170
pulmonary tuberculosis2MONDO:0006052EFO:1000049
endometrial carcinoma2MONDO:0002447EFO:1001512
depressive disorder2MONDO:0002050MONDO:0002050
ulcerative colitis2MONDO:0005101EFO:0000729
acute myocardial infarction2MONDO:0004781EFO:0008583
myocardial infarction2MONDO:0005068EFO:0000612
Crohn disease1MONDO:0005011EFO:0000384
immune system disorder1MONDO:0005046EFO:0000540
metabolic disease1MONDO:0005066EFO:0000589
neoplasm1MONDO:0005070EFO:0000616
prostate adenocarcinoma1MONDO:0005082EFO:0000673
skin disorder1MONDO:0005093EFO:0000701
malaria1MONDO:0005136EFO:0001068
non-small cell lung carcinoma1MONDO:0005233EFO:0003060
hypertriglyceridemia1MONDO:0005347EFO:0004211
anemia1MONDO:0002280EFO:0004272
metastatic melanoma1MONDO:0005191EFO:0002617
respiratory syncytial virus infectious disease1MONDO:0001577EFO:1001413
asthma1MONDO:0004979MONDO:0004979
type 2 diabetes mellitus1MONDO:0005148MONDO:0005148
Parkinson disease1MONDO:0005180MONDO:0005180
hereditary angioedema1MONDO:0019623MONDO:0019623
systemic lupus erythematosus1MONDO:0007915MONDO:0007915
sickle cell disease1MONDO:0011382MONDO:0011382
Friedreich ataxia0MONDO:0100339MONDO:0100339

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

Clinical trials

Total trials: 592.

Phase distribution

PhaseTrials
PHASE1215
PHASE4128
PHASE3126
Not specified50
PHASE248
PHASE2/PHASE313
EARLY_PHASE17
PHASE1/PHASE25

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04098003PHASE4ACTIVE_NOT_RECRUITINGInvestigation of the Gut Microbiome and Statin Response
NCT04499859PHASE4RECRUITINGLow Dose Rosuvastatin Plus Ezetimibe Versus High-dose Rosuvastatin in AMI
NCT05850091PHASE4RECRUITINGPolygenic Risk-based Detection of Subclinical Coronary Atherosclerosis and Intervention With Statin and Colchicine
NCT06186037PHASE4RECRUITINGClinical Comparison of Low-dose Rosuvastatin Plus Ezetimibe Combination Therapy and High-dose Rosuvastatin Monotherapy in Patients With Minimal to Intermediate Coronary Artery Disease Without Percutaneous Coronary Intervention
NCT06338293PHASE4RECRUITINGEffects of Inclisiran Combined With Statins on the Morphology of Coronary Vulnerable Plaques
NCT06765265PHASE4RECRUITINGImpact of Atorvastatin Versus Rosuvastatin on 25 Hydroxy Vitamin D Levels in Patients With Acute Coronary Syndrome
NCT06804980PHASE4RECRUITINGDESIFOR-EXPAND (MHIF)
NCT06820086PHASE4ACTIVE_NOT_RECRUITINGPolygenic Risk Driven Pragmatic Statin Trial for Heart Disease Prevention
NCT06856772PHASE4NOT_YET_RECRUITINGRandomized Comparison of Morning Versus Bedtime Administration of Statins: A Cardiovascular Circadian Chronotherapy (C3) Trial
NCT07036991PHASE4NOT_YET_RECRUITINGClinical Trial of PCSK9 Inhibitor and Statin Treatment for Carotid Artery Stenosis
NCT07254221PHASE4NOT_YET_RECRUITINGRosuvastatin for Prevention of Anthracycline-induced Cardiac Dysfunction in Breast Cancer Patients
NCT07255820PHASE4NOT_YET_RECRUITINGDual vs Triple Lipid-Lowering Therapy in Type 2 Diabetes Mellitus Patients With Elevated LDL Cholesterol
NCT07303816PHASE4NOT_YET_RECRUITINGStatins to Prevent Cancer Associated Blood Clots
NCT07605130PHASE4NOT_YET_RECRUITINGEfficacy and Safety Study of Digital Cognitive Training and PCSK9 Inhibitor-Enhanced Lipid-lowering Strategy in Patients With Intracranial Atherosclerotic Stenosis: A 2×2 Randomized Controlled Trial
NCT00079638PHASE4COMPLETEDComparative Efficacy Evaluation of Lipids When Treated With Niaspan & Statin or Other Lipid-Modifying Therapies-COMPELL
NCT00117494PHASE4COMPLETEDRosuvastatin Versus Pravastatin in HIV Patients Treated With Boosted Protease Inhibitors (PI) (ANRS126)
NCT00295373PHASE4UNKNOWNExercise And Rosuvastatin Treatment: Is There an Anti-Inflammatory Synergy?
NCT00329160PHASE4COMPLETEDRosuvastatin in the Long-term Treatment of Hypercholesterolaemic Subjects With Coronary Heart Disease
NCT00335699PHASE4COMPLETEDKorean Rosuvastatin Effectiveness Study in Nondiabetic Metabolic Syndrome
NCT00371501PHASE4COMPLETEDAspirin and Statins for Prevention of Atherosclerosis and Arterial Thromboembolism in Systemic Lupus Erythematosus
NCT00395486PHASE4COMPLETEDROMEO (Rosuvastatin in Metabolic syndrOme)
NCT00396240PHASE4WITHDRAWNORBITAL: Open-Label Primary Care Study: Rosuvastatin Based Compliance Initiatives Linked To Achievement Of LDL Goals
NCT00427960PHASE4TERMINATEDStudy of Asian Patients With Hypercholesterolaemia in the UK - Rosuvastatin 5mg Versus Atorvastatin 10mg
NCT00457652PHASE4COMPLETEDDoes Caffeine Reduce Rosuvastatin-Induced Protection Against Ischemia-Reperfusion Injury?
NCT00468923PHASE4COMPLETEDHeart Outcomes Prevention Evaluation-3
NCT00473655PHASE4COMPLETEDEffect of Rosuvastatin on Triglyceride Levels in Mexican Hypertriglyceridemic Patients
NCT00506961PHASE4COMPLETEDEvaluate the Efficacy and Safety of Rosuvastatin Versus Simvastatin in Type 2 Diabetic Patients With Dyslipidemia
NCT00631189PHASE4COMPLETEDEvaluation of the Efficacy and Safety of Rosuvastatin 5 mg Versus Pravastatin 40 mg and Atorvastatin 10 mg in Type IIa and IIb Hypercholesterolaemic Patients
NCT00651378PHASE4TERMINATEDSwitching to Rosuvastatin Versus Adding Ezetimibe to Atorvastatin Versus Doubling the Dose of Atorvastatin in Patients With Hypercholesterolemia and Risk Factors (P03708)
NCT00658463PHASE4COMPLETEDEffects of Rosuvastatin on the, in Vivo, Kinetic of apoB and apoA1, Using Stable Isotopes, in Type 2 Diabetic Patients
NCT00665834PHASE4COMPLETEDComparison of Rosuvastatin and Atorvastatin in Patients With Acute Coronary Syndrome
NCT00673582PHASE4TERMINATEDEffectiveness of Rosuvastatin at Preventing the Progression of Atherosclerosis in HIV Positive Patients
NCT00747149PHASE4COMPLETEDA Diabetes Study to Treat A Population Previously Not at Target
NCT00786136PHASE4COMPLETEDRosuvastatin Prevent Contrast Induced Acute Kidney Injury in Patients With Diabetes
NCT00815659PHASE4COMPLETEDEffect of Crestor (Rosuvastatin) on Lipid Levels in Patients With Metabolic Syndrome
NCT00851175PHASE4COMPLETEDIs Augmentation of PORH by Rosuvastatin Adenosine-receptor Mediated?
NCT00866229PHASE4UNKNOWNEfficacy and Adverse Effect of Simvastatin Compare to Rosuvastatin in Systemic Lupus Erythematosus (SLE) Patients With Corticosteroid Therapy and High Low-Density Lipoprotein (LDL) Cholesterol Level
NCT00871351PHASE4COMPLETEDEvaluation of Ezetimibe and Atorvastatin Coadministration Versus Atorvastatin or Rosuvastatin Monotherapy in Japanese Patients With Hypercholesterolemia (Study P06027)(COMPLETED)
NCT00885872PHASE4UNKNOWNRosuvastatin Evaluation of Atherosclerotic Chinese Patients (REACH)
NCT00913562PHASE4WITHDRAWNEffect of Rosuvastatin on Endothelial Function in Patients With Diabetes and Glaucoma

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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:

MoleculeSourceStatusShared targets
ATORVASTATINChEMBL + PubChemPhase 4 (approved)HMGCR
LOVASTATINChEMBL + PubChemPhase 4 (approved)HMGCR
PITAVASTATINChEMBL + PubChemPhase 4 (approved)HMGCR
PRAVASTATINChEMBL + PubChemPhase 4 (approved)HMGCR
SIMVASTATINChEMBL + PubChemPhase 4 (approved)HMGCR
CERIVASTATINChEMBLPhase 4 (approved)HMGCR
CISAPRIDEChEMBLPhase 4 (approved)HMGCR
FLUVASTATINChEMBLPhase 4 (approved)HMGCR
TANNIC ACIDChEMBLPhase 4 (approved)HMGCR
GLENVASTATINChEMBLPhase 2HMGCR
MEGLUTOLChEMBLPhase 2HMGCR
MEVASTATINChEMBLPhase 2HMGCR
VorinostatPubChemApprovedHMGCR

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot