Rosuvastatin

Rosuvastatin
Clinical data
Pronunciation/rˈsvəstætɪn/ roh-SOO-və-stat-in
Trade namesCrestor, others
Other namesRosuvastatin calcium (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa603033
License data
Pregnancy
category
  • AU: D
Routes of
administration
Oral (by mouth)
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • CA: ℞-only
  • UK: POM (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability20%
Protein binding88%
MetabolismLiver: CYP2C9 (major) and CYP2C19-mediated; ~10% metabolized
MetabolitesN-desmethyl rosuvastatin (major; 1/6–1/9 of rosuvastatin activity)
Elimination half-life19 hours
ExcretionFeces (90%)
Identifiers
  • (3R,5S,6E)-7-[4-(4-Fluorophenyl)-2-(N-methylmethanesulfonamido)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.216.011
Chemical and physical data
FormulaC22H28FN3O6S
Molar mass481.54 g·mol−1
3D model (JSmol)
  • OC(=O)C[C@H](O)C[C@H](O)\C=C\c1c(C(C)C)nc(N(C)S(=O)(=O)C)nc1c2ccc(F)cc2
  • InChI=1S/C22H28FN3O6S/c1-13(2)20-18(10-9-16(27)11-17(28)12-19(29)30)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)33(4,31)32/h5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30)/b10-9+/t16-,17-/m1/s1 N
  • Key:BPRHUIZQVSMCRT-VEUZHWNKSA-N N
 NY (what is this?)  (verify)

Rosuvastatin, sold under the brand name Crestor among others, is a statin medication, used to prevent cardiovascular disease in those at high risk and treat abnormal lipids. It is recommended to be used with dietary changes, exercise, and weight loss. It is taken orally (by mouth).

Common side effects include abdominal pain, nausea, headaches, and muscle pains. Serious side effects may include rhabdomyolysis, liver problems, and diabetes. Use during pregnancy may harm the baby. Like all statins, rosuvastatin works by inhibiting HMG-CoA reductase, an enzyme found in the liver that plays a role in producing cholesterol.

Rosuvastatin was patented in 1991 and approved for medical use in the United States in 2003. It is available as a generic medication. In 2022, it was the thirteenth most commonly prescribed medication in the United States, with more than 37 million prescriptions. In Australia, it was one of the top 10 most prescribed medications between 2017 and 2023.