netupitant

Netupitant is a pharmaceutical agent classified as an NK1 receptor antagonist used in the prevention of chemotherapy-induced nausea and vomiting. It is most commonly used in the fixed-dose combination with palonosetron, sold under the brand name Akynzeo, to prevent emesis in adults receiving moderately or highly emetogenic chemotherapy. The combination is indicated for prevention of both acute and delayed chemotherapy-induced nausea and vomiting. The mechanism combines blocking substance P at the neurokinin-1 receptor with antagonism of 5-HT3 receptors by palonosetron.

Netupitant is a long-acting antagonist with a relatively extended half-life, allowing a single pre-chemotherapy dose. In fixed-dose products, a single capsule containing netupitant 300 mg and palonosetron 0.5 mg is taken about one hour before chemotherapy. Netupitant is predominantly metabolized by CYP3A4 and also inhibits CYP3A4, leading to potential drug interactions; co-administered dexamethasone dose is often reduced due to this interaction.

Adverse effects are generally mild to moderate and include fatigue, constipation, headache, and hiccups in some cases; serious adverse events are uncommon. As with other NK1 antagonists, liver function should be monitored in patients with hepatic impairment or on hepatically metabolized drugs.

Netupitant was developed by Helsinn and is approved in several countries for prevention of CINV in adults. The approval status and dosing recommendations may vary by regulatory authority, and clinicians should consult current labeling for detailed guidance about dosing adjustments and contraindications.