Rolapitant

Products

Rolapitant was approved in the form of film-coated tablets in the United States in 2015, in the EU in 2017, and in many countries in 2018 (Varuby).

Structure and properties

Rolapitant (C25H26F6N2O2, Mr = 500.5 g/mol) is present in the drug as rolapitane hydrochloride, a white powder that is more soluble in water at low pH values.

Effects

Rolapitant has antiemetic properties. The effects are due to selective and competitive antagonism at neurokinin-1 receptors. Rolapitant has a long half-life of approximately one week.

Indications

For prevention of nausea and vomiting associated with chemotherapy (combination treatment).

Dosage

According to the package insert. Tablets are taken one to two hours before chemotherapy.

Contraindications

  • Hypersensitivity
  • Combination with thioridazine, a substrate of CYP2D6.

For complete precautions, see the drug label.

Interactions

Rolapitant is a substrate of CYP3A4 and an inhibitor of CYP2D6, P-glycoprotein, and BCRP. Corresponding drug-drug interactions are possible.

Adverse effects

The most common possible adverse effects include neutropenia, hiccups, poor appetite, and dizziness.