CAS number：163222-33-1
molecular formula：C24H21F2NO3
molecular weight：409.43
EINECS number：682-606-0

English synonyms

(3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one;Ezetimibe-001;Ticagrelor and its interMediate;Ezetimibe 1-(4-Fluorophenyl)-3-[3-(4-fluorophenyl)-3-hydroxy-propyl]-4-(4-hydroxyphenyl)-azetidin-2-one;Ezatimibe;zetia/vytorin;SCH 60969;Ezetimibe, >=99%

Related categories

Pharmaceutical raw materials; compounds; pharmaceutical categories; raw materials; medical cardiovascular system; ezetimibe; pharmaceutical intermediates; small molecule inhibitors; active drug intermediates; new selective cholesterol absorption inhibitors; blood lipid lowering; medicine Raw materials; intermediates; cholesterol-lowering drugs; spot; ezetimibe API; reference substance-impurity reference substance; Intermediates;Raw Materials;Medicine, Pesticide and Dye Intermediates;All Inhibitors;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Final material;API;Isotope;CEDAX;Cardiovascular APIs;Ezetimibe;
Standard products; impurity reference substances; technical intermediates; chemical intermediates; chemical raw materials; scientific research raw materials; chemical reagents

Introduction

Ezetimibe is a white crystalline powder, easily soluble in ethanol, methanol and acetone, insoluble in water, with a melting point of about 163°C and stable at room temperature. Ezetimibe only acts on the small intestine, and reduces the transport of intestinal cholesterol to the liver by inhibiting the absorption of cholesterol, reducing its storage; it can strengthen the removal of cholesterol in the blood, thereby reducing the level of plasma cholesterol.

Chemical properties

Use

●  Ezetimibe is a new class of selective cholesterol absorption inhibitors. It binds to the membrane protein (relative molecular weight 145X103) on the small intestinal brush border membrane vesicles to inhibit the small intestine from feeding and transporting to the intestinal tract through bile. Absorption of cholesterol, lower serum and liver cholesterol levels.

●  Hyperlipidemia is one of the high-risk factors for coronary heart disease. The drugs for clinical treatment of hyperlipidemia mainly include cholesterol synthesis inhibitors (such as statins), phenoxy acids (such as fibrates), bile acid sequestrants (such as cholestyramine) and others (such as niacin analogs), etc.

●  After oral absorption, ezetimibe combines with glucuronide to form the active substance, ezetimibe‑glucuronide, which is excreted by bile and kidney. After oral administration, the peak plasma concentration is reached within 4 to 12 hours, the Cmax is 3.4 to 5.5 mg/mL, the bioavailability is between 35% and 60%, and the t1/2 is about 22 hours. Ezetimibe mainly acts on exogenous cholesterol, while the main effect of statins is to reduce the synthesis of cholesterol in the liver, so the two drugs have a synergistic effect. The combined application of ezetimibe and statins has 8 times the cholesterol-lowering effect of statins alone.

API Active Pharmaceutical Ingredients

Obtained from natural medicine. Natural medicine is an important part of medicine. For example, artemisinin, an effective antimalarial ingredient isolated from the traditional Chinese medicine Artemisia annua.
Take existing drugs as first-comers.
1) Discover the active ingredients of the drug from the side effects of the drug. For example, the phenothiazine antipsychotic chlorpromazine and its analogs are developed from the sedative side effects of the similarly structured antihistamine promethazine.
2) Obtained through drug metabolism research. For example, the metabolites of antidepressants imipramine and amitriptyline, norimipramine and noramitriptyline, have stronger antidepressant effects than the original drug; oxazepam is the active metabolite of diazepam.
3) Leading with existing breakthrough drugs. For example, the research on lansoprazole and other prazols is based on omeprazole, which is more active than omeprazole.
Obtained by screening with pharmacological model. Through combinatorial chemistry, a large number of chemical libraries with different structures are constructed without separation of mixtures. Through high-throughput screening, the components are found to have pharmaceutical activity and then separated, and the structure of the active compound is determined.
Designed according to physiological and pathological mechanisms. For example: the study of fluorouracil takes the nucleotide uracil synthesized from DNA or RNA as the lead compound, and replaces the hydrogen at position 5 with fluorine, making it a metabolic antagonist of the normal metabolites of the organism, and is used as an antitumor drug

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