CAS · 163222-33-1
Product Overview
Ezetimibe is a high-purity pharmaceutical-intermediates supplied for industrial and specialty chemical applications. Contact our team for specifications, packaging options and lead times.
Product Specifications
| Appearance: | White crystalline powder |
|---|---|
| Content: | 98.0%~102.0% (calculated on the anhydrous substance) |
| Solubility: | Soluble in methanol or ethanol, soluble in acetonitrile, almost insoluble in water or n-hexane |
| Melting point: | 161~166 °C |
| Water content: | 0.6% max |
| Specific rotation: | -25° ~ -29° |
| Identification: | IR: spectrum should concord with spectrum of standard; Retention time of sample matches standard in assay |
| Maximum single impurity: | 0.5% max |
| Total impurities: | 0.9% max |
| Impurity A: | 0.15% max |
| Sum of impurities C and D: | 0.15% max |
| Impurity G: | 0.2% max |
| Impurity F: | 0.10% max |
| Unspecified impurity: | 0.10% max |
| Sum of achiral impurities: | 0.6% max |
| Impurity SSS: | 0.2% max |
| Impurity RRR: | 0.1% max |
| Impurity E: | 0.4% max |
| Impurity SSR: | 0.10% max |
| Impurity RSR: | 0.10% max |
| Sum of chiral impurities: | 0.5% max |
| 4-fluorine aniline: | 0.15% max |
| 4-hydroxybenzaldehyde: | 0.15% max |
| 4-dimethylaminopyridine: | 0.15% max |
| Isopropyl alcohol: | 0.5% max |
| Dichloromethane: | 0.06% max |
| Methyl tert-butyl ether: | 0.5% max |
| N-hexane: | 0.029% max |
| Ethyl acetate: | 0.5% max |
| Methanol: | 0.3% max |
| N,N-dimethylformamide: | 0.088% max |
| Acetic acid: | 0.5% max |
| Sulfate: | 0.04% max |
| Heavy metals: | 20 ppm max |
| Fluorine: | 8.2% - 9.3% |
Applications
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
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.
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Conclusion
A concise summary and suitability assessment for this product is available on request. Contact our team to discuss whether it fits your process and quality requirements.