For US health-care professionals only. Prescribing Information

About VARUBI® (rolapitant)

Antagonist of the neurokinin 1 (NK-1) receptor, which is activated following administration of emetogenic chemotherapy1,2

Peak plasma concentration (Cmax) was observed approximately 4 hours following administration of VARUBI1

Long half-life (≈7 days), allowing for a single dose1

Selectivity and high affinity (Ki = 0.66 nM) for NK-1 receptors1,3

The relationship between pharmacokinetic parameters and clinical efficacy of VARUBI has not been established.1

Contraindication

  • VARUBI is contraindicated in patients receiving thioridazine, a CYP2D6 substrate. A significant increase in plasma concentrations of thioridazine may result in QT prolongation and Torsades de Pointes

Warnings and precautions

Interaction with CYP2D6 substrates with a narrow therapeutic index

  • The inhibitory effect of VARUBI on CYP2D6 lasts for at least 7 days and may last longer after administration of a single dose of VARUBI
  • Avoid use of VARUBI in patients who are receiving pimozide, a CYP2D6 substrate. An increase in plasma concentrations of pimozide may result in QT prolongation
  • Monitor for adverse reactions if concomitant use of VARUBI and other CYP2D6 substrates with a narrow therapeutic index cannot be avoided