akynzeo
akynzeo Uses, Dosage, Side Effects, Food Interaction and all others data.
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 | akynzeo |
Generic | Netupitant + Palonosetron Hydrochloride |
Weight | 300, 0.5mg, , 300mg + 0.5mg |
Type | Capsule, Oral Capsule, Intravenous |
Therapeutic Class | |
Manufacturer | Helsinn Birex Pharmaceuticals Ltd, Chugai Pharma Uk Limited, Glenmark Pharmaceuticals |
Available Country | Saudi Arabia, Canada, United Kingdom, India, United States, |
Last Updated: | September 19, 2023 at 7:00 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 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.
akynzeo is also used to associated treatment for these conditions: Acute caused and vomiting caused by Chemotherapy, Delayed Nausea and Vomiting caused by Chemotherapy
How akynzeo 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.
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.
Half Life
96 hours with CV% of 61.
Clearance
Estimated systemic clearance of 20.3 ± 9.2 L/h (mean ± SD).
Elimination Route
Primarily fecal.
Innovators Monograph
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