About VARUBI® (rolapitant)
Antagonist of the neurokinin 1 (NK-1) receptor, which is activated following administration of emetogenic chemotherapy1,2
Long half-life (≈7 days), allowing for a
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
- VARUBI is contraindicated in patients taking CYP2D6 substrates with a narrow therapeutic index, such as thioridazine and pimozide. VARUBI can significantly increase the plasma concentrations of thioridazine and pimozide, which may result in QT prolongation and Torsades de Pointes.
Warnings and Precautions
Interaction with CYP2D6 substrates
- VARUBI is a moderate inhibitor of CYP2D6 and significantly increases the plasma concentrations of CYP2D6 substrates for at least 28 days, with inhibitory effects expected to persist for an unknown duration.
- Monitor for adverse reactions when VARUBI is coadministered with CYP2D6 substrates without a narrow therapeutic index (avoid coadministration with CYP2D6 substrates with a narrow therapeutic index, thioridazine and pimozide; see Contraindication). Consider interactions with CYP2D6 substrates before starting treatment with VARUBI.