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Netopitant is a highly selective, long-acting neurokinin-1 (NK1) receptor antagonist. It works by blocking the binding of substance P, a neuropeptide involved in the emetic reflex, to NK1 receptors in both the central and peripheral nervous systems. Originally discovered by Roche and developed by Helsinn Healthcare, netopitant is primarily indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV). It is most commonly administered as a fixed-dose oral combination with the 5-HT3 receptor antagonist palonosetron (marketed as Akynzeo). Beyond CINV, netopitant is being investigated for other indications, including opioid-induced nausea and vomiting (OINV) in patients with cancer pain.
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