Aprepitant is a potent neurokinin-1 (NK₁) receptor antagonist that crosses the blood-brain barrier and occupies brain NK₁ receptors, preventing substance P from binding and triggering emesis. As an antiemetic agent, Aprepitant is administered orally as part of a triple-therapy regimen with a corticosteroid and a 5-HT₃ antagonist for chemotherapy-induced nausea and vomiting. The unique pharmacokinetic profile of Aprepitant includes a long half-life and the ability to block both acute and delayed phases of emesis—a significant advantage over traditional antiemetics. Aprepitant and its related impurities serve as critical reference standards for analytical method development, quality control, and ANDA filings.
|
Parameter |
Specification |
|
Product Name |
Aprepitant |
|
CAS Number |
170729-80-3 |
|
Molecular Formula |
C₂₃H₂₁F₇N₄O₃ |
|
Molecular Weight |
534.43 g/mol |
|
Appearance |
White to off-white solid |
|
Melting Point |
244–246°C |
|
Density |
1.51 ± 0.1 g/cm³ (Predicted) |
|
pKa |
8.06 ± 0.20 (Predicted) |
|
Storage Condition |
Sealed in dry, 2–8°C |
Aprepitant was granted marketing authorization in both the United States and the European Union in 2003 for use in combination with other antiemetic agents to prevent acute or delayed nausea and vomiting occurring during the initial or repeated treatment of patients with highly or moderately vomiting-related malignancies undergoing chemotherapy.
2-(R)-[1-(R)-[3,5-bis(tetrafluoromethyl)phenyl]ethoxy]-3-(S)-(4-fluorophenyl)morpholine (R) camphorsulfonate and potassium carbonate are dissolved in dimethylformamide Chemicalbook. At 22°C, a dimethylformamide solution of 3-chloromethyl-1,2,4-triazolin-5-one is added, stirred, water is added, and the mixture is cooled in an ice bath. The crystals are collected by filtration, washed with water, and dried to obtain Aprepitant.
It exerts a blocking effect on substance P by binding to NK-1 receptors, which are mainly present in the central nervous system and its periphery. This product can cross the blood-brain barrier and occupy NK-1 receptors in the brain, with high selectivity and affinity, while its affinity for NK-2 and NK-3 receptors is very low. Meanwhile, this product also has very low affinity for the targets of other drugs used to treat chemotherapy-induced nausea and vomiting, such as dopamine receptors and 5-HT3 receptors, and its effect of reducing nausea and vomiting is superior to that of other drugs. When this product is used in combination with 5-hydroxytryptamine 3 (5-HT3) receptor blockers and dexamethasone as part of the standard regimen for treating severe emetogenic symptoms caused by chemotherapy, it can improve the complete response rate of chemotherapy-induced acute and delayed nausea and vomiting. In animal models, this product can inhibit acute and delayed vomiting induced by cisplatin. When administered as a single dose before cisplatin intake or concurrently with cisplatin, this product can reduce vomiting symptoms within the following 72 hours; meanwhile, this product can also enhance its antiemetic effect when used in combination with dexamethasone or the 5-HT receptor blocker ondansetron.
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