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Specifications of Ezetimibe丨163222-33-1
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Appearance: |
White crystalline powder |
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Content: |
98.0%~102.0% (calculated on the anhydrous substance) |
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Solubility: |
Soluble in methanol or ethanol, soluble in acetonitrile, almost insoluble in water or n-hexane |
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Melting point: |
161~166 °C |
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Water content: |
0.6% max |
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Specific rotation: |
-25° ~ -29° |
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Identification: |
IR: spectrum should concord with spectrum of standard; Retention time of sample matches standard in assay |
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Maximum single impurity: |
0.5% max |
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Total impurities: |
0.9% max |
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Impurity A: |
0.15% max |
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Sum of impurities C and D: |
0.15% max |
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Impurity G: |
0.2% max |
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Impurity F: |
0.10% max |
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Unspecified impurity: |
0.10% max |
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Sum of achiral impurities: |
0.6% max |
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Impurity SSS: |
0.2% max |
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Impurity RRR: |
0.1% max |
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Impurity E: |
0.4% max |
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Impurity SSR: |
0.10% max |
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Impurity RSR: |
0.10% max |
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Sum of chiral impurities: |
0.5% max |
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4-fluorine aniline: |
0.15% max |
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4-hydroxybenzaldehyde: |
0.15% max |
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4-dimethylaminopyridine: |
0.15% max |
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Isopropyl alcohol: |
0.5% max |
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Dichloromethane: |
0.06% max |
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Methyl tert-butyl ether: |
0.5% max |
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N-hexane: |
0.029% max |
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Ethyl acetate: |
0.5% max |
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Methanol: |
0.3% max |
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N,N-dimethylformamide: |
0.088% max |
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Acetic acid: |
0.5% max |
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Sulfate: |
0.04% max |
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Heavy metals: |
20 ppm max |
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Fluorine: |
8.2% - 9.3% |
Transport Information of Ezetimibe丨163222-33-1
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Parameter |
Specification |
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UN Number |
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Class |
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Packing Group |
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H.S. Code |
2934999099305 |
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Stability & Reactivity |
Stable under recommended storage conditions. |
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Storage |
Tightly closed. Store in a closed, dry, ventilated place. 0-8℃ |
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Condition to Avoid |
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Package |
Manufacturing Information of Ezetimibe丨163222-33-1
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Parameter |
Specification |
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Capacity |
500MT/month |
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Frequency |
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Main Export Countries |
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Capacity/Batch |
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Experience |
Production since 2010 |
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Stock |
Overview
Ezetimibe丨163222-33-1 is a lipid-lowering agent that works by selectively inhibiting intestinal absorption of cholesterol. It is most commonly used in the treatment of hypercholesterolemia and other lipid disorders, either as monotherapy or in combination with statins.
Applications of Ezetimibe丨163222-33-1
1. Treatment of Hypercholesterolemia
● Primarily indicated for primary (heterozygous familial and nonfamilial) hypercholesterolemia.
● Reduces low-density lipoprotein cholesterol (LDL-C) levels by 18–25% when used alone.
● Can be used in combination with statins (e.g., simvastatin, atorvastatin) for enhanced LDL-lowering effect (up to 50–60%).
2. Homozygous Familial Hypercholesterolemia (HoFH)
● Used in combination with statins and other lipid-lowering therapies in patients with HoFH to achieve target cholesterol levels.
3. Homozygous Sitosterolemia (Phytosterolemia)
● Rare genetic disorder in which plant sterols are absorbed excessively.
● Ezetimibe reduces plasma plant sterol levels by 35–45% by blocking their absorption.
4. Cardiovascular Risk Reduction
● When added to statin therapy, ezetimibe further reduces cardiovascular event risk, as demonstrated in clinical trials like IMPROVE-IT, particularly in patients post-acute coronary syndrome.
Mechanism of Action
Ezetimibe acts at the brush border of the small intestine to inhibit the Niemann-Pick C1-like 1 (NPC1L1) protein, a transporter critical for the uptake of cholesterol and plant sterols.
● Reduces the amount of cholesterol delivered to the liver.
● Leads to upregulation of LDL receptors in the liver, enhancing clearance of LDL-C from blood.
Importantly, ezetimibe does not affect triglycerides or HDL cholesterol significantly and does not inhibit cholesterol synthesis, making it complementary to statins.
Benefits of Ezetimibe丨163222-33-1
1. Potent LDL Cholesterol Reduction
● When statins are not sufficient or not tolerated, ezetimibe is a valuable add-on or alternative.
● Enables more patients to reach target LDL-C goals, especially those at high or very high cardiovascular risk.
2. Well Tolerated and Few Systemic Side Effects
● Minimal systemic absorption - most of the drug acts locally in the intestines.
● Side effects are generally mild and infrequent, such as diarrhea, fatigue, or abdominal pain.
● Lower risk of muscle toxicity compared to statins, making it suitable for patients with statin intolerance.
3. No Impact on Liver Enzymes or Glucose Metabolism
● Unlike statins, Ezetimibe丨163222-33-1 does not increase liver enzymes or blood sugar levels.
● Safer option for patients with diabetes or liver conditions (with monitoring).
4. Convenient Dosing
● Once-daily oral tablet (usually 10 mg), with or without food.
● Can be easily co-administered or co-formulated with statins (e.g., ezetimibe + simvastatin = Vytorin®).
Additional Research and Emerging Uses
● Being investigated in combination with PCSK9 inhibitors, bempedoic acid, and fibrates for comprehensive lipid management.
● Studied for potential anti-inflammatory and anti-atherosclerotic effects beyond LDL-C lowering.
Conclusion
Ezetimibe丨163222-33-1 is a well-established, highly effective cholesterol absorption inhibitor that plays a vital role in managing hyperlipidemia and cardiovascular risk, especially in patients who require additional LDL-C lowering beyond statins. With minimal systemic exposure, a favorable safety profile, and proven clinical benefit in atherosclerotic cardiovascular disease, ezetimibe is a key component of modern lipid-lowering strategies.
