Netupitant, Palonosetron

Products

The fixed combination of netupitant and palonosetron has been approved in capsule form (Akynzeo). The drug was released in many countries in 2015.

Structure and properties

Netupitant (C30H32F6N4O, Mr = 578.6 g/mol) is a fluorinated piperazine and pyrimidine derivative. Palonosetron (C19H24N2O, Mr = 296.4 g/mol) is present in drugs as palonosetron hydrochloride, a white crystalline powder that is soluble in water.

Effects

Netupitant and palonosetron both have antiemetic properties. Netupitant is a selective antagonist at substance P/neurokinin-1 receptors. It has a long half-life of more than 90 hours. Palonosetron is a serotonin 5-HT3 receptor antagonist.

Indications

For the prevention of nausea and vomiting associated with chemotherapy in patients with cancer.

Dosage

According to the SmPC. Capsules may be taken independently of meals.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Netupitant is a substrate and mild inhibitor of CYP3A4 and corresponding drug-drug interactions are possible. In combination with serotonergic agents, serotonin syndrome may possibly occur.

Adverse effects

The most common possible adverse effects include headache, weakness, dyspepsia, fatigue, constipation, and skin flushing.