Aprepitant
CAS_1: 170729-80-3
Specification: USP /EP /BP 99.5%
Active_ingredients: 
Content

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-1, Product Name: Aprepitant
-2, Specification & Standard: USP /EP /BP 99.5%
 
-3, CAS #: 170729-80-3
-4, Description: White crystalline powder
 
-5, Function of Aprepitant :

Aprepitant is for prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) and for prevention of postoperative nausea and vomiting. It was approved by the FDA in 2003.
 
Aprepitant may also be useful in the treatment of cyclic vomiting syndrome but there are few studies to date.
Aprepitant is taken orally in the form of a capsule. Before clinical testing, a new class of therapeutic agent has to be characterized in terms of preclinical metabolism and excretion studies. Average bioavailability is found to be around 60-65%. Aprepitant is metabolized primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19. Seven metabolites of aprepitant, which are only weakly active, have been identified in human plasma. As a moderate inhibitor of CYP3A4, aprepitant can increase plasma concentrations of coadministered medicinal products that are metabolized through CYP3A4. Following IV administration of a 14C-labelled prodrug of aprepitant (L-758298), which is converted rapidly and completely to aprepitant, approximately 57% of the total radioactivity is excreted in the urine and 45% in faeces. No unchanged substance is excreted in urine.
  
One of the fundamental features of aprepitant, and a major advantage it has over other chemotherapy induced side effect treatments, is it that while it successfully antagonises the NK1 receptors it has very little affinity over other receptors such as serotonin, dopamine and corticosteroid. It is estimated that aprepitant is at least 3000 times more selective of NK1 receptors compared to these other enzyme transporter, ion channels.


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