Akynzeo

Akynzeo is a fixed-dose antiemetic combination that contains netupitant, a neurokinin-1 (NK1) receptor antagonist, and palonosetron, a serotonin-3 (5-HT3) receptor antagonist. By blocking NK1 receptors and 5-HT3 receptors, Akynzeo reduces the risk of chemotherapy-induced nausea and vomiting (CINV). The long-acting NK1 blockade helps cover both the acute and delayed phases of CINV.

Indications and administration

Akynzeo is approved for the prevention of acute and delayed CINV in adults receiving moderately or highly emetogenic chemotherapy. It is given as a single oral capsule about one hour before chemotherapy. Each capsule contains netupitant 300 mg and palonosetron 0.5 mg. In clinical practice, Akynzeo is often used with corticosteroids such as dexamethasone, following guidelines for antiemetic regimens.

Pharmacology and interactions

Netupitant is a moderate inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme, and palonosetron is a 5-HT3 receptor antagonist. Because of CYP3A4 inhibition, co-administered drugs metabolized by this enzyme may have altered exposures, and corticosteroid doses may require adjustment when used with Akynzeo. The combination has a relatively favorable QT risk profile due to the palonosetron component, but clinicians monitor for interactions with other QT-prolonging agents and drugs affecting gastric motility or hepatic function.

Safety and adverse effects

Common adverse events reported with Akynzeo include fatigue, headache, constipation, and diarrhea. As with NK1 antagonists, rare hypersensitivity or hepatic effects may occur, and liver function should be monitored in patients with hepatic impairment. The product requires consideration of drug interactions and individual patient factors.

Manufacturer and approvals

Akynzeo is marketed by Helsinn Healthcare. It has been approved in various regions for adult patients undergoing chemotherapy, with dosing and combination guidelines reflecting local regulatory labeling.