Modern views on the evolution of the ketoprofen molecule. Clinical progress in efficacy and safety of use

May 12, 2026
66
УДК:  615.06
Resume

The aim of this article is to review current perspectives on the evolution of ketoprofen and to evaluate clinical advances in its efficacy and safety, particularly with the development of ketoprofen lysine salt (KLS). Ketoprofen is a widely used nonsteroidal anti-inflammatory drug with proven analgesic and anti-inflammatory effects, but its use is limited by gastrointestinal adverse events. The development of KLS has improved the pharmacokinetic profile of the molecule, provided faster absorption, a more rapid onset of action, and enhanced gastrointestinal tolerability while maintaining clinical efficacy. Available evidence suggests that KLS allows for effective pain and inflammation control at lower doses, with improved safety and good tolerability in both adult and pediatric populations.

References

  • 1. Neha K., Wakode S. (2021) Contemporary advances of cyclic molecules proposed for inflammation. Eur. J. Med. Chem., 221: 113493.
  • 2. Meyer-Kirchrath J., Schror K. (2000) Cyclooxygenase-2 inhibition and side-effects of non-steroidal antiinflammatory drugs in the gastrointestinal tract. Curr. Med. Chem., 7: 1121–1129.
  • 3. Graziosi A., Senatore M., Gazzaniga G. et al. (2025) Ketoprofen Lysine Salt vs. Ketoprofen Acid: Assessing the Evidence for Enhanced Safety and Efficacy. Life (Basel), 15(4): 659.
  • 4. D’angelo M., Brandolini L., Catanesi M. et al. (2023) Differential Effects of Nonsteroidal Anti-Inflammatory Drugs in an In Vitro Model of Human Leaky Gut. Cells, 12: 728.
  • 5. Carbone C., Rende P., Comberiati P. et al. (2013) The safety of ketoprofen in different ages. J. Pharmacol. Pharmacother., 4: S99–S103.
  • 6. Castellsague J., Riera-Guardia N., Calingaert B. et al. (2012) Individual NSAIDs and upper gastrointestinal complications: A systematic review and meta-analysis of observational studies (the SOS project). Drug Saf., 35: 1127–1146.
  • 7. Kuczyńska J., Nieradko-Iwanicka B. (2021) Future prospects of ketoprofen in improving the safety of the gastric mucosa. Biomed. Pharmacother., 139: 111608.
  • 8. Hayamizu K., Oshima I., Nakano M. (2020) Comprehensive Safety Assessment of l-Lysine Supplementation from Clinical Studies: A Systematic Review. J. Nutr., 150: 2561S–2569S.
  • 9. Marseglia G.L. (2023) Clinical use of ketoprofen lysine salt: a reappraisal in adolescents with acute respiratory infections. Allergol. Immunopathol., 51(6): 76–82.
  • 10. Kalinski P. (2012) Regulation of Immune Responses by Prostaglandin E2. J. Immunol., 188: 21–28.
  • 11. Mannila A., Kokki H., Heikkinen M. (2006) Cerebrospinal fluid distribution of ketoprofen after intravenous administration in young children. Clin. Pharmacokinet., 45(7): 737–743.
  • 12. Bjarnason I., Scarpignato C., Takeuchi K., Rainsford K.D. (2007) Determinants of the short-term gastric damage caused by NSAIDs in man. Aliment. Pharmacol. Ther., 26(1): 95–106.
  • 13. Panerai A.E. (2011) The management of pain-inflammatory conditions. Trends Med., 11(4): 163–177.
  • 14. Brandolini L., d’Angelo M., Antonosante A. et al. (2018) Differential protein modulation by ketoprofen and ibuprofen underlines different cellular response by gastric epithelium. J. Cell Physiol., 233(3): 2304–2312.
  • 15. Novelli R., Aramini A., Boccella S. et al. (2022) Ketoprofen lysine salt has a better gastrointestinal and renal tolerability than ketoprofen acid: A comparative tolerability study in the Beagle dog. Biomed. Pharmacother., 153: 113336.
  • 16. Panerai A.E., Lanata L., Ferrari M., Bagnasco M. (2012) A new ketoprofen lysine salt formulation: 40 mg orodispersible granules. Trends Med., 12: 159–167.
  • 17. Marseglia G., Miraglia Del Giudice M., Scaglione F. (2025) An Italian multidisciplinary Delphi Consensus on managing children and adolescents with acute fever using ketoprofen lysine salt. Minerva Pediatr. (Torino). doi: 10.23736/S2724-5276.25.07830-9.
  • 18. Mariniello D.F., Pagliaro R., D’Agnano V. et al. (2025) Ketoprofen Lysine Salt Versus Corticosteroids in Early Outpatient Management of Mild and Moderate COVID-19: A Retrospective Study. Pharmacy (Basel), 13(3): 65. doi: 10.3390/pharmacy13030065.
  • 19. Kokki H. (2010) Ketoprofen pharmacokinetics, efficacy, and tolerability in pediatric patients. Pediatr. Drugs, 12(5): 313–329.
  • 20. Cooney M.F. (2021) Pain management in children: NSAID use in the perioperative and emergency department settings. Pediatr. Drugs, 23: 361–372.
  • 21. Sarzi-Puttini P., Atzeni F., Lanata L., Bagnasco M. (2013) Efficay of ketoprofen vs. ibuprofen and diclofenac: a systematic review of the literature and meta-analysis. Clin. Exp. Rheumatol., 31(5): 731–738.
  • 22. Brewer E.J., Giannini E.H., Baum J. et al. (1982) Ketoprofen (Orudis) in the treatment of juvenile rheumatoid arthritis: a segment I study. J. Rheumatol., 9(1): 144–148.
  • 23. Kokki H., Kokki M. (2010) Dose-finding studies of ketoprofen in the management of fever in children. Clin. Drug Invest., 30: 251–258.