Netupitant/Palonosetron

DEA Class; Rx

Common Brand Names; Akynzeo, fosnetupitant

  • Antiemetic Agents; 
  • Antiemetics, Selective 5-HT3 Antagonist; 
  • NK1 Receptor Antagonists

Combination of a selective substance P neurokinin 1 (NK1) receptor antagonist and highly selective 5-HT3 receptor antagonist
Used with dexamethasone for prevention of CINV due to chemotherapy, including, but not limited to, highly emetogenic chemotherapy
Palonosetron prevents nausea and vomiting during the acute phase and netupitant/fosnetupitant prevents nausea and vomiting during both the acute and delayed phase after chemotherapy

Indicated for acute and delayed chemotherapy-induced nausea/vomiting prophylaxis (CINV prophylaxis) associated with initial and repeat courses of cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.

  • Headache (9%)
  • Asthenia (8%)
  • Fatigue (4-7%)
  • Dyspepsia (4%)
  • Constipation (3%)
  • Erythema (3%)

Hypersensitivity reactions (eg, anaphylaxis) reported in patients treated with palonosetron, with or without known hypersensitivity to other 5-HT3 receptor antagonists

Serotonin syndrome has been reported with 5-HT3 receptor antagonists (eg, palonosetron); most reports have been associated with concomitant use of serotonergic drugs (eg, selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors, mirtazapine, fentanyl, lithium, tramadol, and IV methylene blue); discontinue netupitant/palonosetron if symptoms occur

Limited available data with its use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes

No data on the presence of netupitant (or fosnetupitant) or palonosetron in human milk, the effects on the breastfed infant, or the effects on milk production

Adults

1 capsule (netupitant 300 mg; palonosetron 0.5 mg) PO as a single dose; 1 vial (235 mg fosnetupitant/0.25 mg palonosetron) IV infusion.

Geriatric

1 capsule (netupitant 300 mg; palonosetron 0.5 mg) PO as a single dose; 1 vial (235 mg fosnetupitant/0.25 mg palonosetron) IV infusion.

Adolescents

Safety and efficacy have not been established.

Children

Safety and efficacy have not been established.

Infants

Not indicated.

Neonates

Not indicated.

Netupitant/palonosetron

capsule

  • 300mg/0.5mg

injection

  • lyophilized powder for reconstitution: (235mg/0.25mg)/vial
  • ready-to-dilute IV solution: (235mg/0.25mg)/20mL vial
  • Note: Parenteral products contain fosnetupitant, a prodrug of netupitant

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