Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. It has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonists, such as ondansetron, and the corticosteroids, e.g. dexamethasone, and inhibits both the acute and delayed phases of cisplatin- induced emesis. Furthermore, studies show that aprepitant has a long duration of central activity and inhibits both the acute and delayed phases of cisplatin-induced emesis.
Storage conditions: Room temperature
Packaging: polyethylene nylon plastic bag