Eight faces of ezetimibe, that is a therapeutic signpost for practicing physician A.D. 2025 Review article
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Published:
Mar 31, 2025
Keywords:
ezetimibe, dyslipidemia, combination therapy
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Abstract
Hypercholesterolemia is the most common cardiovascular risk factor in Poland. According to experts, low effectiveness in achieving therapeutic goals in dyslipidemia is associated with: the use of too low doses of statins, the selection of drugs with weak hypolipidemic effects, short treatment period, unjustified discontinuation of therapy and too rare use of combination therapy. As shown in numerous studies, adding ezetimibe to any statin is associated with a significant reduction in LDL cholesterol concentration and more frequent achievement of target lipid values than in the case of statin monotherapy. Optimization of hypolipidemic therapy and persistence in its use results in reduction of circulatory complications risk, which should be particularly emphasized in patients with high and very high cardiovascular risk. The paper presents 8 advantages of ezetimibe, with particular emphasis on its efficacy and safety of use and its place in modern therapy for lipid disorders.
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Barylski, M. (2025). Eight faces of ezetimibe, that is a therapeutic signpost for practicing physician A.D. 2025. Medycyna Faktow (J EBM), 18(1(66), 67-71. https://doi.org/10.24292/01.MF.0125.10
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References
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11. Bardini G, Giorda CB, Pontiroli AE et al. Ezetimibe + simvastatin versus doubling the dose of simvastatin in high cardiovascular risk diabetics: a multicenter, randomized trial (the LEAD study). Cardiovasc Diabetol. 2010; 9: 20.
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13. Sharp Collaborative Group. Study of Heart and Renal Protection (SHARP): randomized trial to assess the effects of lowering low-density lipoprotein cholesterol among 9,438 patients with chronic kidney disease. Am Heart J. 2010; 160(5): 785-94.
14. van der Graaf A, Cuffie-Jackson C, Vissers MN et al. Efficacy and safety of coadministration of ezetimibe and simvastatin in adolescents with heterozygous familial hypercholesterolemia. J Am Coll Cardiol. 2008; 52(17): 1421-9.
15. Zieve F, Wenger NK, Ben-Yehuda O et al. Safety and efficacy of ezetimibe added to atorvastatin versus up titration of atorvastatin to 40 mg in Patients > or = 65 years of age (from the ZETia in the ELDerly [ZETELD] study). Am J Cardiol. 2010; 105(5): 656-63.
16. Ballantyne CM, Hoogeveen RC, Raya JL et al.; GRAVITY Study Investigators. Efficacy, safety and effect on biomarkers related to cholesterol and lipoprotein metabolism of rosuvastatin 10 or 20 mg plus ezetimibe 10 mg vs. simvastatin 40 or 80 mg plus ezetimibe 10 mg in high-risk patients: Results of the GRAVITY randomized study. Atherosclerosis. 2014; 232: 86-93.
17. Charakterystyka Produktu Leczniczego Ezen, 10 mg, tabletki, 09.2022.
18. Barylski M, Mamcarz A. Ezetimib. W: Mamcarz A, Barylski M, Wełnicki M (ed.). Lipidologia. Wydawnictwo Lekarskie PZWL, Warszawa 2021.
19. Barylski M. W parze skuteczniej i bezpieczniej, czyli kiedy ezetimib staje się nieocenionym partnerem w terapii dyslipidemii. Choroby Serca i Naczyń. 2018; 15(1): 1-9.
20. Averna M, Banach M, Bruckert E et al. Practical guidance for combination lipid-modifying therapy in high- and very-high-risk patients: A statement from a European Atherosclerosis Society Task Force. Atherosclerosis 2021; 325: 99-109.
21. Wełnicki M, Gorczyca-Głowacka I, Kapłon-Cieślicka A et al. Leczenie dyslipidemii w Polsce – powszechna diagnostyka, wczesna terapia skojarzona. Stanowisko grupy ekspertów wsparte przez Sekcję Farmakoterapii Sercowo-Naczyniowej Polskiego Towarzystwa Kardiologicznego. V Deklaracja Sopocka (w druku).
22. Crea F, Niccoli G. Ezetimibe and Plaque Regression. Cholesterol Lowering or Pleiotropic Effects? J Am Coll Cardiol. 2015; 66(5): 508-10.
23. Savarese G, De Ferrari GM, Rosano GM et al. Safety and efficacy of ezetimibe: A meta-analysis. Int J Cardiol. 2015; 201: 247-52.
24. Pearson TA, Denke MA, McBride PE et al. A community-based, randomized trial of ezetimibe added to statin therapy to attain NCEP ATP III goals for LDL cholesterol in hypercholesterolemic patients: the ezetimibe add-on to statin for effectiveness (EASE) trial. Mayo Clin Proc. 2005; 80: 587-95.
2. Broncel M. Miejsce ezetymibu we współczesnej terapii hipolipemizującej. KOF. 2010; 3: 211-8.
3. Sweeney ME, Johnson RR. Ezetimibe: an update on the mechanism of action, pharmacokinetics and recent clinical trials. Expert Opin Drug Metab Toxicol. 2007; 3(3): 441-50.
4. Pikto-Pietkiewicz W, Pasierski T. Ezetymib – inhibitor wchłaniania cholesterolu. Kardiol Pol. 2006; 64: 1434-41.
5. Knopp RH, Dujovne CA, Le Beaut A et al.; Ezetimbe Study Group. Evaluation of the efficacy, safety, and tolerability of ezetimibe in primary hypercholesterolaemia: a pooled analysis from two controlled phase III clinical studies. Int J Clin Pract. 2003; 57(5): 363-8.
6. Cagne C, Bays HE, Weiss SR et al. Efficacy and safety of ezetimibe added to ongoing statin therapy for treatment of patients with primary hypercholesterolemia. Am J Cardiol. 2002; 90: 1084-91.
7. Davidson MR, McGarry T, Bettis R et al. Ezetimibe coadministered with simvastatin in patients with primary hypercholesterolemia. Am J Coll Cardiol. 2002; 40: 2125-34.
8. Bays HE, Davidson MH, Massaad R et al. Safety and efficacy of ezetimibe added on to rosuvastatin 5 or 10 mg versus up-titration of rosuvastatin in patients with hypercholesterolemia (the ACTE Study). Am J Cardiol. 2011; 108(4): 523-30.
9. Mach F, Baigent C, Catapano AL et al.; ESC Scientific Document Group. 2019 ESC/EAS Guidelines for the management of dyslipidaemias: lipid modification to reduce cardiovascular risk. Eur Heart J. 2020; 41(1): 111-88.
10. Cannon CP, Blazing MA, Giugliano RP et al.; IMPROVE-IT Investigators. Ezetimibe added to statin therapy after acute coronary syndromes. N Engl J Med. 2015; 372(25): 2387-97.
11. Bardini G, Giorda CB, Pontiroli AE et al. Ezetimibe + simvastatin versus doubling the dose of simvastatin in high cardiovascular risk diabetics: a multicenter, randomized trial (the LEAD study). Cardiovasc Diabetol. 2010; 9: 20.
12. Ballantyne CM, Weiss R, Moccetti T et al.; EXPLORER Study Investigators. Efficacy and safety of rosuvastatin 40 mg alone or in combination with ezetimibe in patients at high risk of cardiovascular disease (results from the EXPLORER study). Am J Cardiol. 2007; 99(5): 673-80.
13. Sharp Collaborative Group. Study of Heart and Renal Protection (SHARP): randomized trial to assess the effects of lowering low-density lipoprotein cholesterol among 9,438 patients with chronic kidney disease. Am Heart J. 2010; 160(5): 785-94.
14. van der Graaf A, Cuffie-Jackson C, Vissers MN et al. Efficacy and safety of coadministration of ezetimibe and simvastatin in adolescents with heterozygous familial hypercholesterolemia. J Am Coll Cardiol. 2008; 52(17): 1421-9.
15. Zieve F, Wenger NK, Ben-Yehuda O et al. Safety and efficacy of ezetimibe added to atorvastatin versus up titration of atorvastatin to 40 mg in Patients > or = 65 years of age (from the ZETia in the ELDerly [ZETELD] study). Am J Cardiol. 2010; 105(5): 656-63.
16. Ballantyne CM, Hoogeveen RC, Raya JL et al.; GRAVITY Study Investigators. Efficacy, safety and effect on biomarkers related to cholesterol and lipoprotein metabolism of rosuvastatin 10 or 20 mg plus ezetimibe 10 mg vs. simvastatin 40 or 80 mg plus ezetimibe 10 mg in high-risk patients: Results of the GRAVITY randomized study. Atherosclerosis. 2014; 232: 86-93.
17. Charakterystyka Produktu Leczniczego Ezen, 10 mg, tabletki, 09.2022.
18. Barylski M, Mamcarz A. Ezetimib. W: Mamcarz A, Barylski M, Wełnicki M (ed.). Lipidologia. Wydawnictwo Lekarskie PZWL, Warszawa 2021.
19. Barylski M. W parze skuteczniej i bezpieczniej, czyli kiedy ezetimib staje się nieocenionym partnerem w terapii dyslipidemii. Choroby Serca i Naczyń. 2018; 15(1): 1-9.
20. Averna M, Banach M, Bruckert E et al. Practical guidance for combination lipid-modifying therapy in high- and very-high-risk patients: A statement from a European Atherosclerosis Society Task Force. Atherosclerosis 2021; 325: 99-109.
21. Wełnicki M, Gorczyca-Głowacka I, Kapłon-Cieślicka A et al. Leczenie dyslipidemii w Polsce – powszechna diagnostyka, wczesna terapia skojarzona. Stanowisko grupy ekspertów wsparte przez Sekcję Farmakoterapii Sercowo-Naczyniowej Polskiego Towarzystwa Kardiologicznego. V Deklaracja Sopocka (w druku).
22. Crea F, Niccoli G. Ezetimibe and Plaque Regression. Cholesterol Lowering or Pleiotropic Effects? J Am Coll Cardiol. 2015; 66(5): 508-10.
23. Savarese G, De Ferrari GM, Rosano GM et al. Safety and efficacy of ezetimibe: A meta-analysis. Int J Cardiol. 2015; 201: 247-52.
24. Pearson TA, Denke MA, McBride PE et al. A community-based, randomized trial of ezetimibe added to statin therapy to attain NCEP ATP III goals for LDL cholesterol in hypercholesterolemic patients: the ezetimibe add-on to statin for effectiveness (EASE) trial. Mayo Clin Proc. 2005; 80: 587-95.