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Medical Application of Aprepitant

  • Author:Ray Dean
  • Source:www.oceanchinachem.com
  • Release on :2016-09-14
Aprepitant by binding to the NK-1 receptor (mainly in the central nervous system and peripheral) to block the action of Substance P. It can be used to pass the blood-brain occupied in the NK-1 receptor with high affinity and selectivity, while NK-2 and NK-3 receptor affinity is very low. At the same time the product of the other targets for the treatment of chemotherapy-induced nausea and vomiting drugs (such as dopamine receptors, 5-HT receptors) affinity interaction is very low, which reduces nausea and vomiting than other drugs .

This product can be extensively metabolized in the body, mainly through CPY3A4, a small part by CPY1 A2 and CPY2C9 conduct; its metabolites are mainly structural parts of the morpholine ring and side chains. Healthy subjects administered a single dose of 300 mg of the product ¨C mark after 72 h, the plasma can be detected in 24% of the radioactivity, indicating that the product does exist in plasma metabolites, and at least seven species, but the basic no pharmacological effect. In the standard method of severe emetic symptoms and serotonin 3 (5-HT) receptor antagonist and dexamethasone combination treatment of chemotherapy-induced, it is possible to improve the acute and delayed nausea and vomiting induced by chemotherapy complete response rate .

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