These highlights do not include all the information needed to use AKYNZEO® safely and effectively. See full prescribing information for AKYNZEO®.
AKYNZEO® (netupitant and palonosetron) capsules, for oral use
Initial U.S. Approval: 2014
AKYNZEO® (fosnetupitant and palonosetron) for injection, for intravenous use
Initial U.S. Approval: 2018
RECENT MAJOR CHANGES
Indication and Usage (1) 04/2018
Dosage and Administration, Recommended Dosage (2.1) 04/2018
Dosage and Administration, Preparation (2.2) 04/2018
Dosage and Administration, Incompatibility (2.3) 04/2018
INDICATIONS AND USAGE
AKYNZEO capsules is indicated in combination with dexamethasone in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.
AKYNZEO for injection is indicated in combination with dexamethasone in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy.
Limitations of Use
AKYNZEO for injection has not been studied for the prevention of nausea and vomiting associated with anthracycline plus cyclophosphamide chemotherapy.
AKYNZEO is a combination of palonosetron, a serotonin-3 (5-HT3) receptor antagonist, and netupitant or fosnetupitant, substance P/neurokinin-1 (NK-1) receptor antagonists: palonosetron prevents nausea and vomiting during the acute phase and netupitant/fosnetupitant prevents nausea and vomiting during both the acute and delayed phase after cancer chemotherapy. (1)
DOSAGE AND ADMINISTRATION
One AKYNZEO capsule administered approximately 1 hour prior to the start of chemotherapy, with or without food. (2.1)
One vial of AKYNZEO for injection; reconstituted in 50 ml of 5% Dextrose Injection, USP or 0.9% Sodium Chloride Injection, USP and administered as 30-minute infusion starting approximately 30 minutes prior to the start of chemotherapy. (2.1, 2.2, 2.3)
DOSAGE FORMS AND STRENGTHS
Capsules: 300 mg netupitant/0.5 mg palonosetron
For Injection: 235 mg fosnetupitant/0.25 mg palonosetron lyophilized powder in a single-dose vial for reconstitution (3)
WARNINGS AND PRECAUTIONS
Hypersensitivity reactions, including anaphylaxis, have been reported in patients receiving palonosetron, one of the components of AKYNZEO, with or without known hypersensitivity to other 5-HT3 receptor antagonists. (5.1)
Serotonin syndrome has been reported with 5-HT3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs. If such symptoms occur, discontinue AKYNZEO and initiate supportive treatment. If concomitant use of AKYNZEO with other serotonergic drugs is clinically warranted, patients should be made aware of a potential increased risk for serotonin syndrome. (5.2,7.3)
Most common adverse reactions (?3%) for AKYNZEO capsules are headache, asthenia, dyspepsia, fatigue, constipation and erythema (6.1)
The safety profile of AKYNZEO for injection was generally similar to that seen with AKYNZEO capsules. (6.1)
To report SUSPECTED ADVERSE REACTIONS, contact HELSINN at 1-844-357-4668 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
CYP3A4 Substrates: inhibition of CYP3A4 by netupitant can result in increased plasma concentrations of the concomitant drug for 6 days after single dosage administration of AKYNZEO; avoid concomitant CYP3A4 substrates for one week, if feasible. If not avoidable, consider dose reduction of the CYP3A4 substrate (7.1)
CYP3A4 Inducers (e.g., rifampin): decreased plasma concentrations of netupitant; avoid use (7.2)
USE IN SPECIFIC POPULATIONS
Pregnancy: May cause fetal harm (8.1).
Hepatic Impairment: Avoid use in patients with severe hepatic impairment (8.6)
Renal Impairment: Avoid use in patients with severe renal impairment or end-stage renal disease (8.7)
See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.