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Indication
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AKYNZEO is indicated 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 is an oral fixed combination of palonosetron and netupitant: palonosetron prevents nausea and vomiting during the acute phase and netupitant prevents nausea and vomiting during both the acute and delayed phase after cancer chemotherapy.
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Important Safety Information
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Warnings and Precautions
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Hypersensitivity reactions, including anaphylaxis, have been reported with or without known hypersensitivity to other 5‑HT3 receptor antagonists |
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Please see below for additional Important Safety Information.
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The first and only oral fixed combination for CINV1
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The correlation between these pharmacological data and clinical efficacy has not been established.
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AKYNZEO® is the first and only oral fixed combination of palonosetron and netupitant: palonosetron prevents nausea and vomiting during the acute phase of CINV and netupitant prevents nausea and vomiting during both the acute and delayed phase after cancer chemotherapy.
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Netupitant is a selective antagonist of substance P/NK1 receptors. As shown in in vitro and in vivo studies, netupitant inhibits substance P‑mediated response.
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Netupitant has a mean plasma half‑life of approximately 80 hours |
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Netupitant demonstrated 92.5% NK1 receptor occupancy at 6 hours, with 76% occupancy at 96 hours |
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Palonosetron is a 5‑HT3 receptor antagonist with a strong binding affinity for this receptor.
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Oral palonosetron has a mean plasma half‑life of approximately 48 hours |
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CINV=chemotherapy‑induced nausea and vomiting.
MOA=mechanism of action.
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Important Safety Information (continued)
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Warnings and Precautions (continued)
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Serotonin syndrome has been reported with 5‑HT3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs. Serotonin syndrome can be life threatening. Symptoms associated with serotonin syndrome may include the following combination of signs and symptoms: mental status changes, autonomic instability, neuromuscular symptoms, seizures, and gastrointestinal symptoms. Patients should be monitored for the emergence of serotonin syndrome, and if symptoms occur, discontinue AKYNZEO and initiate supportive treatment. Patients should be informed of the increased risk of serotonin syndrome, especially if AKYNZEO is used concomitantly with other serotonergic drugs
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Adverse Reactions
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Most common adverse reactions: headache, asthenia, dyspepsia, fatigue, constipation and erythema
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Drug Interactions
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Use with caution in patients receiving concomitant medications primarily metabolized by CYP3A4. The plasma concentrations of CYP3A4 substrates can increase when co‑administered with AKYNZEO. The inhibitory effect on CYP3A4 can last for multiple days
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Dexamethasone doses should be reduced when given with AKYNZEO. A two-fold increase in the systemic exposure of dexamethasone was observed 4 days after single dose of netupitant
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Consider the potential effects of increased plasma concentrations of midazolam or other benzodiazepines metabolized via CYP3A4 (alprazolam, triazolam) when administering with AKYNZEO. When administered with netupitant, the systemic exposure to midazolam was significantly increased
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Avoid concomitant use of AKYNZEO in patients on chronic use of a strong CYP3A4 inducer such as rifampin as this may decrease the efficacy of AKYNZEO
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Use in Specific Populations
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Avoid use of AKYNZEO in patients with severe hepatic impairment, severe renal impairment, or end-stage renal disease
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For more information about AKYNZEO, please see Full Prescribing Information.
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Reference: 1. AKYNZEO® (netupitant/palonosetron) capsules. Full Prescribing Information.
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