Compendium of the most significant studies with reference to properties, intake, effects.

Sjuls S, Jensen U, Littmann K, Bruchfeld A, Brinck J. Effective cholesterol lowering after myocardial infarction in patients with nephrotic syndrome may require a multi-pharmacological approach: a case report. Eur Heart J Case Rep. 2021 May 13;5(5):ytab151. doi: 10.1093/ehjcr/ytab151.

Boutari C, Karagiannis A, Athyros VG. Rosuvastatin and ezetimibe for the treatment of dyslipidemia and hypercholesterolemia. Expert Rev Cardiovasc Ther. 2021 Jun 15:1-6. doi: 10.1080/14779072.2021.1940959. 

Salgado MM, Manchado A, Nieto CT, Díez D, Garrido NM. Synthesis and Modeling of Ezetimibe Analogues. Molecules. 2021 May 22;26(11):3107. doi: 10.3390/molecules26113107.

Reynolds TM, Pottle A, Quoraishi SH. Current Perspectives on the Attainment of Lipid Modification Goals Relating to the Use of Statins and Ezetimibe for the Prevention of Cardiovascular Disease in the United Kingdom. Vasc Health Risk Manag. 2021 May 21;17:227-237. doi: 10.2147/VHRM.S269879.

Lowenstern A, Li S, Navar AM, Virani SS, Roger VL, Robinson JG, Goldberg AC, Kampman W, Peterson ED, Wang TY. Patient perceptions and use of non-statin lipid lowering therapy among patients with or at risk for atherosclerotic cardiovascular disease: Insights from the PALM registry. Clin Cardiol. 2021 Jun;44(6):863-870. doi: 10.1002/clc.23625.

Yamashita S, Masuda D, Harada-Shiba M, Arai H, Bujo H, Ishibashi S, Daida H, Koga N, Oikawa S; FAME Study Group. Effectiveness and Safety of Lipid-Lowering Drug Treatments in Japanese Patients with Familial Hypercholesterolemia: Familial Hypercholesterolemia Expert Forum (FAME) Study. J Atheroscler Thromb. 2021 May 13. doi: 10.5551/jat.62764. 

Barrios V, Escobar C. Fixed-dose combination of rosuvastatin and ezetimibe: treating hypercholesteremia according to cardiovascular risk. Expert Rev Clin Pharmacol. 2021 May 24:1-14. doi: 10.1080/17512433.2021.1925539.

Diaconu CC, Iorga RA, Furtunescu F, Katsiki N, Stoian AP, Rizzo M. Statin intolerance: new data and further options for treatment. Curr Opin Cardiol. 2021 Jul 1;36(4):487-493. doi: 10.1097/HCO.0000000000000874.

Lui DTW, Lee ACH, Tan KCB. Management of Familial Hypercholesterolemia: Current Status and Future Perspectives. J Endocr Soc. 2020 Aug 21;5(1):bvaa122. doi: 10.1210/jendso/bvaa122.

Ezetimibe is a chemical compound, a derivative of azetidinone (azetidin-2-one).

Take only under medical supervision

It comes as white fine powder.

What it is used for and where

It is a cholesterol absorption inhibitor with lipid-lowering activity. 

Ezetimibe significantly reduces the risk of myocardial infarction and stroke without any effect on all-cause and cardiovascular mortality and risk of cancer (1).

The bempedoic acid and ezetimibe fixed-dose combination significantly lowered low-density lipoprotein cholesterol versus placebo or other oral monotherapies and had a favourable safety profile when added to maximally tolerated statin therapy in patients with hypercholesterolemia and high cardiovascular disease risk (2).

Coronary heart disease (CHD) is the main cause of death and morbidity in the world. There is a strong evidence that the atherosclerotic process begins in childhood and that hypercholesterolaemia is a CHD major risk factor. Statins are the cornerstone of the drug therapy approved in USA and in Europe for use in children. Ezetimibe or bile acid sequestrants may be required to attain LDL-C goal in some patients. Early identification of children with severe hypercholesterolaemia or with FH is important to prevent atherosclerosis at the earliest stage of development, when maximum benefit can still be obtained via lifestyle adaptations and therapy. The purpose of our review is to highlight the importance of prevention and treatment of hypercholesterolaemia starting from the earliest stages of life (3).

Like all drugs it can cause side effects. Always ask the physician.

Ezetimibe studies

Typical optimal characteristics of the commercial product Ezetimibe

• Molecular Formula: C₂₄H₂₁F₂NO₃
• Molecular Weight: 409.4 g/mol
• CAS: 163222-33-1
• UNII EOR26LQQ24
• EC Number: 682-606-0
• PubChem Substance ID 329749824
• InChI=1S/C24H21F2NO3/c25-17-5-1-15(2-6-17)22(29)14-13-21-23(16-3-11-20(28)12-4-16)27(24(21)30)19-9-7-18(26)8-10-19/h1-12,21-23,28-29H,13-14H2/t21-,22+,23-/m1/s1 
• InChl Key      OLNTVTPDXPETLC-XPWALMASSA-N
• SMILES    C1=CC(=CC=C1C2C(C(=O)N2C3=CC=C(C=C3)F)CCC(C4=CC=C(C=C4)F)O)O
• IUPAC   (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
• ChEBI
• DSSTox Substance ID: DTXSID1044223
• MDL number  MFCD00937872
• NACRES: NA.24

Synonyms: 

• (3R,4S)-1-(4-Fluorophenyl)-3-[(S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
• ezetimib
• Ezetrol
• 2-Azetidinone, 1-(4-fluorophenyl)-3-((3S)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)-, (3R,4S)-

References____________________________________________________________________

(1) Savarese G, De Ferrari GM, Rosano GM, Perrone-Filardi P. Safety and efficacy of ezetimibe: A meta-analysis. Int J Cardiol. 2015 Dec 15;201:247-52. doi: 10.1016/j.ijcard.2015.08.103.

(2) Ballantyne CM, Laufs U, Ray KK, Leiter LA, Bays HE, Goldberg AC, Stroes ES, MacDougall D, Zhao X, Catapano AL. Bempedoic acid plus ezetimibe fixed-dose combination in patients with hypercholesterolemia and high CVD risk treated with maximally tolerated statin therapy. Eur J Prev Cardiol. 2020 Apr;27(6):593-603. doi: 10.1177/2047487319864671.

(3) Pederiva C, Capra ME, Viggiano C, Rovelli V, Banderali G, Biasucci G. Early Prevention of Atherosclerosis: Detection and Management of Hypercholesterolaemia in Children and Adolescents. Life (Basel). 2021 Apr 14;11(4):345. doi: 10.3390/life11040345.