FDA Approves an Oral Combination of Netupitant and Palonosetron for Nausea and Vomiting Associated With Cancer Chemotherapy

A novel oral combination of a new highly selective NK1 receptor antagonist and a 5-HT3 receptor antagonist

The USA Food and Drug Administration (FDA) approved on 10 October, 2014 Akynzeo (netupitant and palonosetron) to treat nausea and vomiting in patients undergoing cancer chemotherapy. Akynzeo is a fixed combination capsule comprised of two drugs (netupitant and palonosetron).

Oral palonosetron, approved in 2008, prevents nausea and vomiting during the acute phase (within the first 24 hours) after the start of cancer chemotherapy. Netupitant, a new drug, prevents nausea and vomiting during both the acute phase and delayed phase (from 25 to 120 hours) after the start of cancer chemotherapy.

It is a novel oral fixed-dose combination of netupitant, a new highly selective NK1 receptor antagonist and palonosetron, a pharmacologically and clinically distinct 5-HT3 receptor antagonist.

Akynzeo’s effectiveness was established in two clinical trials

The new drug's effectiveness was established in two clinical trials of 1,720 participants receiving cancer chemotherapy. Participants were randomly assigned to receive Akynzeo or oral palonosetron. The trials were designed to measure whether the study drugs prevented any vomiting episodes in the acute, delayed and overall phases after the start of cancer chemotherapy.

Results of the first trial showed that 98.5%, 90.4% and 89.6% of Akynzeo-treated participants did not experience any vomiting or require rescue medication for nausea during the acute, delayed and overall phases, respectively. In contrast, 89.7%, 80.1% and 76.5% of participants treated with oral palonosetron did not experience any vomiting or require rescue medication for nausea during the acute, delayed and overall phases, respectively. The second trial showed similar results.

Common side effects of Akynzeo in the clinical trials were headache, asthenia, fatigue, dyspepsia and constipation.

Akynzeo is distributed and marketed by Eisai Inc. of Woodcliff Lake, New Jersey, under license from Lugano, Switzerland-based Helsinn Healthcare S.A.