Akynzeo

Generic name: netupitant and palonosetron

Drug class: Miscellaneous antiemetics

Dosage form: Capsules, Injection

Root of administration: Oral, Intravenous

Dose:

• Oral Capsules: 300 mg netupitant and 0.5 mg palonosetron, taken once orally approximately 1 hour before chemotherapy on Day 1, in combination with dexamethasone.
• Intravenous Injection: 235 mg fosnetupitant and 0.25 mg palonosetron, administered as a single intravenous infusion approximately 30 minutes before chemotherapy on Day 1, in combination with dexamethasone.

Mechanism of action: Netupitant is a substance P/neurokinin-1 (NK-1) receptor antagonist, and palonosetron is a serotonin-3 (5-HT₃) receptor antagonist. Together, they inhibit the receptors that drive acute and delayed chemotherapy-induced nausea and vomiting (CINV). Palonosetron prevents nausea and vomiting during the acute phase, while netupitant prevents nausea and vomiting during both the acute and delayed phases after cancer chemotherapy.

Drug usage cases:

• Prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy, including cisplatin-based chemotherapy.
• Prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy, including anthracyclines and cyclophosphamide-based chemotherapy.

Drug contraindications:

• Hypersensitivity to netupitant, palonosetron, or any component of the formulation.
• Concomitant use with pimozide, thioridazine, or other drugs that prolong the QT interval.
• Concomitant use with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing MAOIs.

Side effects:

• Headache
• Fatigue
• Constipation
• Elevated liver enzymes (ALT, AST)
• Elevated creatinine levels
• Hypersensitivity reactions, including anaphylaxis
• Serotonin syndrome, especially when used with other serotonergic drugs

Warnings:

• Hypersensitivity reactions, including anaphylaxis, have been reported. Seek immediate medical attention if symptoms such as hives, facial swelling, difficulty breathing, or chest pain occur.
• Serotonin syndrome is a potentially life-threatening condition that can occur, particularly when used with other serotonergic drugs. Symptoms may include agitation, hallucinations, rapid heartbeat, high blood pressure, fever, nausea, vomiting, diarrhea, tremors, muscle rigidity, and seizures. Discontinue AKYNZEO and seek emergency medical care if these symptoms develop.
• Use caution in patients with a history of QT interval prolongation or other cardiac conditions.
• Monitor liver and kidney function during treatment, as AKYNZEO may affect these organs.

Use during pregnancy or breastfeeding:

AKYNZEO may harm an unborn baby. It is not known if AKYNZEO passes into breast milk, and it should not be used during breastfeeding. Women who are pregnant or planning to become pregnant should discuss the risks and benefits of AKYNZEO with their healthcare provider. Women who are breastfeeding should not use AKYNZEO and should consult their healthcare provider for alternative treatments.