About VARUBI® (rolapitant)

Factors that increase CINV risk5,6
  • mobile - Antagonist of the neurokinin 1 (NK-1) receptor
  • mobile - Peak plasma concentration (Cmax) was observed approximately 4 hours following administration of VARUBI
  • mobile - Long half-life
  • mobile - Selectivity and high affinity
Antagonist of the neurokinin 1 (NK-1) receptor
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 VARUBI
Peak plasma concentration (Cmax) was observed approximately 4 hours following administration of VARUBI1
Long half-life
Long half-life (≈7 days), allowing for a single dose1
Selectivity and high affinity
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

 
 
mobile - MOA poster

Warnings and precautions

Interaction with CYP2D6 substrates with a narrow therapeutic index

 
 

Indication and Important Safety Information for VARUBI® (rolapitant)

Indication

  • VARUBI, in combination with other antiemetic agents, is indicated in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy

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

Adverse reactions

  • In patients receiving cisplatin-based highly emetogenic chemotherapy in cycle 1, the most common adverse reactions reported at an incidence of ≥5% and a frequency greater than control were neutropenia (9% VARUBI vs 8% control) and hiccups (5% vs 4%)
  • In patients receiving moderately emetogenic chemotherapy and combinations of anthracycline and cyclophosphamide in cycle 1, the most common adverse reactions reported at an incidence of ≥5% and a frequency greater than control were decreased appetite (9% VARUBI vs 7% control), neutropenia (7% vs 6%), and dizziness (6% vs 4%)

Drug interactions

  • VARUBI is an inhibitor of breast cancer resistance protein (BCRP) and P-glycoprotein (P-gp). Increased plasma concentrations of BCRP and P-gp substrates with a narrow therapeutic index may result in potential adverse reactions. Monitor for adverse reactions related to the concomitant drug if use with VARUBI cannot be avoided
  • Avoid use of VARUBI in patients who require chronic administration of strong CYP3A4 inducers (eg, rifampin) as significantly reduced plasma concentrations of VARUBI can decrease the efficacy of VARUBI
 

Please see full Prescribing Information.

 
 

References: 1. VARUBI [package insert]. Waltham, MA: TESARO, Inc.; 2015. 2. Aziz F. Neurokinin-1 receptor antagonists for chemotherapy-induced nausea and vomiting. Ann Palliat Med. 2012;1(2):130-136. 3. Data on file. TESARO, Inc.

 
 
varubi logo - color varubi logo - white
Indication and Important Safety Information for VARUBI® (rolapitant)   button arrow