Netupitant Uses, Dosage, Side Effects and more

Netupitant is an antiemitic drug approved by the FDA in October 2014 for use in combination with palonosetron for the prevention of acute and delayed vomiting and nausea associated with cancer chemotherapy including highly emetogenic chemotherapy. Netupitant is a neurokinin 1 receptor antagonist. The combination drug is marketed by Eisai Inc. and Helsinn Therapeutics (U.S.) Inc. under the brand Akynzeo.

Trade Name	Netupitant
Generic	Netupitant
Netupitant Other Names	Netupitant
Type
Formula	C₃₀H₃₂F₆N₄O
Weight	Average: 578.603 Monoisotopic: 578.248030644
Protein binding	> 99.5% at drug concentrations ranging from 10-1300 ng/mL.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	January 7, 2025 at 1:49 am

Uses

Netupitant is an antiemetic agent used in combination with palonosetron to prevent acute and delayed vomiting and nausea caused by chemotherapy.

Netupitant is also used to associated treatment for these conditions: Acute caused and vomiting caused by Chemotherapy, Delayed Nausea and Vomiting caused by Chemotherapy

How Netupitant works

Delayed emesis (vomiting) has been largely associated with the activation of tachykinin family neurokinin 1 (NK1) receptors (broadly distributed in the central and peripheral nervous systems) by substance P. As shown in in vitro and in vivo studies, netupitant inhibits substance P mediated responses.

Toxicity

Daily oral administration of netupitant in rats at doses up to 30 mg/kg (1.9 times the human AUC in male rats and 3.7 times the human AUC in female rats at the recommended human dose) had no effects on fertility or reproductive performance.

Food Interaction

Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of netupitant, which may increase its serum concentration.
Avoid St. John's Wort. This herb induces the CYP3A metabolism of netupitant and may reduce its serum concentration.
Take with or without food.

Volume of Distribution

In cancer patients, Vz/F: 1982 ± 906 L (mean ± SD).

Elimination Route

Upon oral administration of a single dose of netupitant, netupitant started to be measurable in plasma between 15 minutes and 3 hours after dosing. Plasma concentrations reached Cmax in approximately 5 hours. There was a greater than dose-proportional increase in the systemic exposure with the dose increase from 10 mg to 300 mg and a dose-proportional increase in systemic exposure with a dose increase from 300 mg to 450 mg.