Rosuvastatin
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2003
- First approval year
- 2003
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Rosuvastatin
- Molecular weight
- 481.55
- Structure (SMILES)
- CC(C)c1nc(N(C)S(C)(=O)=O)nc(-c2ccc(F)cc2)c1/C=C/[C@@H](O)C[C@@H](O)CC(=O)O
- 6 heptenoic acid 7 4 4 fluorophenyl 6 1 methylethyl 2 methyl methylsulfonyl amino 5 pyrimidinyl 3 5 dihydroxy 3r 5s 6e
- 6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, (3R,5S,6E)-
- creston
- Creston
- rosuvastatin
- Rosuvastatin
- Rosuvastatin [HSDB]
- rosuvastatin [INN]
- Rosuvastatin [MI]
- Rosuvastatin [VANDF]
- Rosuvastatin [WHO-DD]
- rosuvastatin hsdb
- rosuvastatin inn
- rosuvastatin mi
- rosuvastatin vandf
- rosuvastatin who dd
- rosuvastatina
- Rosuvastatina
- rosuvastatine
- Rosuvastatine
- x plended
- X-plended
- zd 4522
- ZD-4522
- zd4522
And 1 more, listed on the interactive page.
- ATC classification codes
- C10AA07
Sources for recorded values
- CAS registry numbers
- 287714-41-4
- ChEMBL ID
- CHEMBL1496
- InChIKey
- BPRHUIZQVSMCRT-VEUZHWNKSA-N
- PubChem compound IDs
- 446157
- RxNorm IDs (RxCUI)
- 301542
- FDA ingredient codes (UNII)
- 413KH5ZJ73
- Applicant
- ASTRAZENECA
- Approval date
- 12 Aug 2003
- Application number
- NDA021366
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- rosuvastatin
- Type
- Synthetic organic
- Drug name stem
- -stat-
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Competitive
- Action type
- COMPETITIVE
- Target
- hydroxymethylglutaryl-CoA reductase
- Gene symbol
- HMGCR
- Protein identifier
- P04035
- Median affinity
- 8.27
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Competitive
- Action type
- COMPETITIVE
- Target
- hydroxymethylglutaryl-CoA reductase
- Gene symbol
- HMGCR
- Protein identifier
- P04035
- Median affinity
- 8.3
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Competitive
- Action type
- COMPETITIVE
- Target
- hydroxymethylglutaryl-CoA reductase
- Gene symbol
- HMGCR
- Protein identifier
- P04035
- Median affinity
- 8.51
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Competitive
- Action type
- COMPETITIVE
- Target
- hydroxymethylglutaryl-CoA reductase
- Gene symbol
- HMGCR
- Protein identifier
- P04035
- Median affinity
- 8.64
- Affinity units
- pKi
- Primary target
- Yes
Open Targets mechanisms
- Mechanism
- HMG-CoA reductase inhibitor
- Action type
- Inhibitor
- Target
- 3-hydroxy-3-methylglutaryl-coenzyme A reductase
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- HMGCR
- Protein identifier
- P04035
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- HIV Infections
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000180
- Subject identifier
- D015658
- Condition
- Metabolic Syndrome
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000195
- Subject identifier
- D024821
- Condition
- Aortic Valve Stenosis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000266
- Subject identifier
- D001024
- Condition
- Cardiovascular Diseases
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000319
- Subject identifier
- D002318
- Condition
- Pulmonary Disease, Chronic Obstructive
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000341
- Subject identifier
- D029424
- Condition
- Heart Failure
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000373
- Subject identifier
- D006333
- Condition
- Crohn Disease
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000384
- Subject identifier
- D003424
- Condition
- Diabetes Mellitus
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000400
- Subject identifier
- D003920
- Condition
- Cardiomyopathy, Dilated
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000407
- Subject identifier
- D002311
- Condition
- Hypertension
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000537
- Subject identifier
- D006973
- Condition
- Immune System Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000540
- Subject identifier
- D007154
- Condition
- Ischemia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000556
- Subject identifier
- D007511
- Condition
- Metabolic Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000589
- Subject identifier
- D008659
- Condition
- Myocardial Infarction
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000612
- Subject identifier
- D009203
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Periodontitis
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000649
- Subject identifier
- D010518
- Condition
- Pre-Eclampsia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000668
- Subject identifier
- D011225
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Arthritis, Rheumatoid
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000685
- Subject identifier
- D001172
- Condition
- Skin Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000701
- Subject identifier
- D012871
- Condition
- Stroke
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000712
- Subject identifier
- D020521
- Condition
- Scleroderma, Systemic
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000717
- Subject identifier
- D012595
- Condition
- Colitis, Ulcerative
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000729
- Subject identifier
- D003093
- Condition
- HIV Infections
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000764
- Subject identifier
- D015658
- Condition
- Malaria
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001068
- Subject identifier
- D008288
And 54 more, listed on the interactive page.
- Condition identifier
- EFO_0000180
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000195
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000266
- Condition identifier
- EFO_0000266
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000319
- Condition identifier
- EFO_0000341
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000373
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000400
- Condition identifier
- EFO_0000407
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000537
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000540
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000556
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000589
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000612
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000649
- Condition identifier
- EFO_0000668
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000685
- Condition identifier
- EFO_0000712
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000717
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000729
- Condition identifier
- EFO_0000764
- Highest recorded phase
- 3
- Condition identifier
- EFO_0001068
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001073
- Highest recorded phase
- 3
- Condition identifier
- EFO_0001645
- Highest recorded phase
- 3
And 122 more, listed on the interactive page.
- Event
- blood creatine phosphokinase increased
- Reports
- 3,155
- Reporting signal score
- 5,866.28
- Event
- blood triglycerides increased
- Reports
- 272
- Reporting signal score
- 426.62
- Event
- drug interaction
- Reports
- 3,621
- Reporting signal score
- 2,589.05
- Event
- high density lipoprotein decreased
- Reports
- 220
- Reporting signal score
- 621.08
- Event
- immune-mediated myositis
- Reports
- 474
- Reporting signal score
- 1,511.58
- Event
- immune-mediated necrotising myopathy
- Reports
- 367
- Reporting signal score
- 1,189.74
- Event
- liver function test abnormal
- Reports
- 997
- Reporting signal score
- 890.243
- Event
- low density lipoprotein increased
- Reports
- 241
- Reporting signal score
- 502.385
- Event
- muscle spasms
- Reports
- 530
- Reporting signal score
- 264.011
- Event
- muscular weakness
- Reports
- 2,041
- Reporting signal score
- 1,792.04
- Event
- myalgia
- Reports
- 6,976
- Reporting signal score
- 10,840.7
- Event
- myopathy
- Reports
- 1,546
- Reporting signal score
- 3,847.82
- Event
- myositis
- Reports
- 734
- Reporting signal score
- 1,327.11
- Event
- renal failure acute
- Reports
- 1,476
- Reporting signal score
- 1,206.36
- Event
- rhabdomyolysis
- Reports
- 6,575
- Reporting signal score
- 15,588.2
- NCT00090298
- NCT00132717
- NCT00160745
- NCT00240279
- NCT00241488
- NCT00249899
- NCT00249912
- NCT00379249
- NCT00462748
- NCT00654173
- NCT00654407
- NCT00654537
- NCT00664469
- NCT00683618
- NCT00783263
- NCT01154036
- NCT01730040
- NCT01730053
- NCT02251847
- NCT02390375
- NCT02445352
- NCT02476006
- NCT02715726
- NCT02741245
- NCT02749994
And 160 more, listed on the interactive page.
- Dose
- 5-40 mg
- Route
- Oral
- How often
- Once daily
- If a dose is missed, do not double next dose
- Swallow tablets whole
- Take with or without food
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 3
- Polar surface area
- 140.92
- Calculated partition coefficient (ALogP)
- 2.4
- Calculated partition coefficient (XLogP)
- 1.6
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 10
- Heavy atoms
- 33
- Molecular formula
- C22H28FN3O6S
- Monoisotopic mass
- 481.16828496
- Natural product
- No
- 50228-116
- 50228-117
- 50228-118
- 50228-119
- 51407-848
- 51407-849
- 51407-850
- 51407-851
- 71610-796
- 71610-797
- 71610-798
- 71610-922
- 50090-7240
- 50090-7241
- 50090-7430
- 50090-7431
- 50090-7482
- 50090-7483
- 50090-7730
- 50090-7793
- 67046-1627
- 68071-3847
- 68788-4057
- 68788-4161
- 68788-8698
And 8 more, listed on the interactive page.
- Recorded assays
- 550
- Active assays
- 54
- Confirmatory
- Other
- Summary
- Anticholesteremic Agents
- Hydroxymethylglutaryl-CoA Reductase Inhibitors
These details could not be displayed.
Related records
Trials (626)
- "Efficacy Of 1.2% Rosuvastatin Gel In The Management Of Infrabony Defects"
- [Effects of Selected Statins on Cardiovascular Parameters in Healthy Volunteers]
- 1.2% Rosuvastatin Gel As A Local Agent In Smokers With Chronic Periodontitis
- 1.2% Rosuvastatin Subgingivally Delivered In Chronic Periodontitis With Type 2 Diabetes Mellitus
- 12-week Open-label, Phase IIIb Comparing Efficacy and Safety of Rosuvastatin (CRESTOR™) in Combination With Ezetimibe
- 30 Week Study of the Combination of ABT-335 and Rosuvastatin Compared to Rosuvastatin Monotherapy for Subjects With Dyslipidemia and Stage 3 Chronic Kidney Disease
- 48-wk Open Label Phase IIIb to Evaluate Efficacy and Safety
- A 2-part Study to Investigate the Effect of Macitentan in Healthy Male Participants
- A Clinical Drug-Drug Interaction (DDI) Study With Omaveloxolone
- A Clinical Study of Calderasib (MK-1084) With Rosuvastatin and Metformin in Healthy People (MK-1084-016)
- A Clinical Study of Enlicitide in Participants With High Cholesterol (MK-0616-037)
- A Clinical Study of the Effect of MK-2828 on Rosuvastatin or Furosemide in Healthy People (MK-2828-005)
- A Clinical Study to Evaluate PK, PD, and PG of Rosuvastatin in the Elderly
- A Clinical Study to Evaluate the Pharmacokinetics of Microdose Midazolam, Dabigatran, Pitavastatin, Atorvastatin and Rosuvastatin in Healthy Volunteers and Renal Impairment Patients
- A Clinical Trial of Enlicitide and Rosuvastatin in Healthy Adults (MK-0616-039)
- A Clinical Trial of YMC017 in Hypertensive and Hypercholesterolemic Patients With Metabolic Syndrome
- A Clinical Trial to Assess the Long Term Safety and Tolerability of MK-0653H in Japanese Participants With Hypercholesterolemia (MK-0653H-833)
- A Clinical Trial to Compare the Efficacy and Safety of a Combination Therapy of Ezetimibe and Rosuvastatin Versus Monotherapy of Rosuvastatin in Hypercholesterolemia Patients (I-ROSETTE Study)
- A Clinical Trial to Evaluate the Effects of MK-4646 on Rosuvastatin in Healthy Participants (MK-4646-007)
- A Clinical Trial to Evaluate the Efficacy and Safety of Olmesartan/Amlodipine/Rosuvastatin Combination Treatment in Patients With Concomitant Hypertension and Hyperlipidemia
Approved for (1)
In development for (71)
- Acute coronary syndrome Phase 3
- Acute myocardial infarction Phase 2
- Anemia Phase 1
- Anti-neutrophil antibody associated vasculitis Phase 3
- Aortic valve stenosis Phase 3
- Asthma Phase 1
- Atherosclerosis Phase 3
- Breast cancer Phase 2
- Burn Phase 2
- Cancer Phase 1
- Chronic obstructive pulmonary disease Phase 2
- Colorectal cancer Phase 3
- Congestive heart failure Phase 3
- Coronary artery disorder Phase 3
- Coronary atherosclerosis Phase 3
- COVID-19 Phase 3
- Crohn disease Phase 1
- Depressive disorder Phase 2
- Diabetes mellitus Phase 2
- Diabetic polyneuropathy Phase 2
Other linked conditions (3)
- Behcet disease
- Intracranial arterial disease
- Severe pre-eclampsia
Targets (1)
- HMGCR HMG-CoA reductase inhibitor