Netupitant-Palonosetron

Netupitant-Palonosetron is a combination medication used for treating nausea and vomiting induced by chemotherapy.

• Netupitant-Palonosetron is available under various brand names: Akynzeo, fosnetupitant

Common side effects of Netupitant-Palonosetron include:

• headache,
• weakness,
• indigestion,
• fatigue,
• constipation, and
• skin redness

Serious side effects of Netupitant-Palonosetron include:

• hives,
• chest pain
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• agitation, 
• hallucinations, 
• fever, 
• sweating, 
• shivering, 
• fast heart rate, 
• muscle stiffness, 
• twitching,
• loss of coordination, 
• nausea, 
• vomiting, or 
• diarrhea.

Rare side effects of Netupitant-Palonosetron include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Capsule

• 300 mg/0.5 mg

Injection

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

Chemotherapy-Induced Nausea & Vomiting

Adult dosage

Highly emetogenic chemotherapy

• 1 capsule (300 mg/0.5 mg) oral approximately 1 hour before starting chemotherapy OR
• 1 reconstituted vial (235mg/0.25mg) IV over 30 min starting 30 min before chemotherapy PLUS
• Dexamethasone 12 mg PO 30 minutes prior to chemotherapy on day 1 and 8 mg orally every day on days 2-4

Chemotherapy not considered highly emetogenic

• Includes anthracyclines and cyclophosphamide-based chemotherapy
• 1 capsule (300 mg/0.5 mg) orally ~1 hr before starting chemotherapy PLUS
• Dexamethasone 12 mg orally 30 minutes prior to chemotherapy on day 1
• Administration of dexamethasone on days 2-4 is not necessary

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Netupitant-Palonosetron has severe interactions with the following drugs:
  • apomorphine
  • flibanserin
  • lonafarnib
• Netupitant-Palonosetron has serious interactions with at least 84 other drugs.
• Netupitant-Palonosetron has moderate interactions with at least 67 other drugs.
• Netupitant-Palonosetron has no noted minor interactions with the following drugs:
  • estradiol vaginal
  • irinotecan
  • irinotecan liposomal

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Netupitant-Palonosetron?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Netupitant-Palonosetron?”

Cautions

• 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
• Drug interactions overview
  • Netupitant is a CYP3A4 substrate and a moderate inhibitor of CYP3A4
  • Palonosetron is mainly metabolized by CYP2D6 and to a lesser extent by CYP3A4 and CYP1A2
  • Strong CYP3A4 inducers (e.g., rifampin) can decrease netupitant-Palonosetron efficacy by substantially reducing plasma concentrations of the netupitant component; avoid use
  • Concomitant use with a strong CYP3A4 inhibitor (e.g., ketoconazole) can increase the systemic exposure to the netupitant component; no dosage adjustment is necessary for single dose administration

Pregnancy & Lactation

• Limited available data with its use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes
• Lactation
  • 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
  • Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for netupitant-Palonosetron and any potential adverse effect on the breastfed child from netupitant-Palonosetron or from the underlying maternal condition