Rosuvastatin

Rosuvastatin
Clinical data
Pronunciation/roʊˈsuːvəstætɪn/ roh-SOO-və-stat-in
Trade namesCrestor, others
Other namesRosuvastatin calcium (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa603033
License data
Pregnancy
category
Routes of
administration		Oral (by mouth)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability20%[5][6]
Protein binding88%[5][6]
MetabolismLiver: CYP2C9 (major) and CYP2C19-mediated; ~10% metabolized[5][6]
MetabolitesN-desmethyl rosuvastatin (major; 1/6–1/9 of rosuvastatin activity)[4]
Elimination half-life19 hours[5][6]
ExcretionFeces (90%)[5][6]
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 Edit this at Wikidata
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
 ☒NcheckY (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.[6] It is recommended to be used together with dietary changes, exercise, and weight loss.[6] It is taken orally (by mouth).[6]

Common side effects include abdominal pain, nausea, headaches, and muscle pains.[6] Serious side effects may include rhabdomyolysis, liver problems, and diabetes.[6] Use during pregnancy may harm the baby.[6] Like all statins, rosuvastatin works by inhibiting HMG-CoA reductase, an enzyme found in the liver that plays a role in producing cholesterol.[6]

Rosuvastatin was patented in 1991, and approved for medical use in the United States in 2003.[6][7] It is available as a generic medication.[6] In 2022, it was the thirteenth most commonly prescribed medication in the United States, with more than 37 million prescriptions.[8][9] In Australia, it was one of the top 10 most prescribed medications between 2017 and 2023.[10]

  1. ^ "Rosuvastatin Use During Pregnancy". Drugs.com. 27 September 2019. Archived from the original on 30 November 2020. Retrieved 14 March 2020.
  2. ^ "Crestor Product information". Health Canada. 25 April 2012. Archived from the original on 9 July 2021. Retrieved 9 July 2021.
  3. ^ "Crestor 10mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 29 September 2020. Archived from the original on 9 July 2021. Retrieved 9 July 2021.
  4. ^ a b Cite error: The named reference Crestor FDA label was invoked but never defined (see the help page).
  5. ^ a b c d e Aggarwal RK, Showkathali R (June 2013). "Rosuvastatin calcium in acute coronary syndromes". Expert Opinion on Pharmacotherapy. 14 (9): 1215–27. doi:10.1517/14656566.2013.789860. PMID 23574635. S2CID 20221457.
  6. ^ a b c d e f g h i j k l m n "Rosuvastatin Calcium Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists (AHFS). Archived from the original on 24 December 2018. Retrieved 24 December 2018.
  7. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 473. ISBN 9783527607495. Archived from the original on 12 January 2023. Retrieved 27 August 2020.
  8. ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
  9. ^ "Rosuvastatin Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.
  10. ^ "Medicines in the health system". Australian Institute of Health and Welfare. 2 July 2024. Retrieved 30 September 2024.