Demonstrated tolerability profile for VARUBI® (rolapitant)

Patients from three phase 3 trials (highly emetogenic chemotherapy [HEC] studies 1 and 2 and moderately emetogenic chemotherapy [MEC] study) and one phase 2 HEC trial were included in the safety population1-3

 
Adverse reactions with VARUBI were reported by approximately 7% of patients versus approximately 6% of patients receiving control in cycle 1.4
 
 

The most common adverse reactions (≥3%) observed in clinical trials with VARUBI during cycle 1 with cytotoxic chemotherapy4

Cisplatin-based HEC Carboplatin-based HEC
 
a The VARUBI regimen consisted of VARUBI, dexamethasone, and a 5-HT3 receptor antagonist.4
b The active control regimen consisted of placebo, dexamethasone, and a 5-HT3 receptor antagonist.4
c Since the start of the study, AC has been reclassified as HEC.5 Types of MEC included in this study were carboplatin, cyclophosphamide (<1,500 mg/m2), and irinotecan.2
Common reactions (≥3%) shown in the tables include those in which the rate for VARUBI exceeded the rate for control.
5-HT3, 5-hydroxytryptamine-3 (serotonin); AC, anthracycline and cyclophosphamide; HEC, highly emetogenic chemotherapy; MEC, moderately emetogenic chemotherapy.
 

Safety in multiple-cycle extensions

Adverse reactions in the multiple-cycle extensions of HEC and MEC studies for up to 6 cycles of chemotherapy were generally similar to those observed in cycle 1.4

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.4

 
You may report side effects to the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. You may also report side effects to TESARO, Inc., at 1-844-4-TESARO (1-844-483-7276).
 
 

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. Rapoport BL, Chasen MR, Gridelli C, et al. Safety and efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting after administration of cisplatin-based highly emetogenic chemotherapy in patients with cancer: two randomized, active-controlled, double-blind, phase 3 trials [published online August 11, 2015]. Lancet Oncol. doi:10.1016/S1470-2045(15)00035-2. 2. Schwartzberg LS, Modiano MR, Rapoport BL, et al. Safety and efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting after administration of moderately emetogenic chemotherapy or anthracycline and cyclophosphamide regimens in patients with cancer: a randomised, active-controlled, double-blind, phase 3 trial [published online August 11, 2015]. Lancet Oncol. doi:10.1016/S1470-2045(15)00034-0. 3. Rapoport B, Chua D, Poma A, Arora S, Wang Y, Fein LE. Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC) [published online May 5, 2015]. Support Care Cancer. doi:10.1007/s00520-015-2738-1. 4. VARUBI [package insert]. Waltham, MA: TESARO, Inc.; 2015. 5. Referenced with permission from the NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®) for Antiemesis v.2.2015. © National Comprehensive Cancer Network, Inc., 2015. All rights reserved. Accessed October 13, 2015. To view the most recent and complete version of the guideline, go online to NCCN.org. NATIONAL COMPREHENSIVE CANCER NETWORK®, NCCN®, NCCN GUIDELINES®, and all other NCCN Content are trademarks owned by the National Comprehensive Cancer Network, Inc.

 
 
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