Patients experiencing delayed CINV may suffer in silence1,2

More than half of patients undergoing emetogenic chemotherapy experience delayed chemotherapy-induced nausea and vomiting (CINV), despite 97% receiving a 5-hydroxytryptamine-3 (serotonin) receptor antagonist (5-HT3 RA) and 78% receiving a corticosteroid.1

 

Oncologists and nurses commonly underestimate the incidence of delayed CINV1

tablet - perception chart mobile - perception chart
 
 
Factors that increase CINV risk5,6
  • mobile - factors - age
  • mobile - factors - female
  • mobile - factors - anxiety
  • mobile - factors - prior
  • mobile - factors - alcohol
Factors that increase CINV risk5,6
factors - age factors - female factors - anxiety factors - prior factors - alcohol
 
a A standard drink is 1.5 ounces (oz) of 80-proof spirits (hard liquor), 12 oz of beer, or 5 oz of wine.
tablet - CINV pathway mobile - CINV pathway
5-HT3, 5-hydroxytryptamine-3 (serotonin); GI, gastrointestinal; NK-1, neurokinin 1.
 
Blocking both 5-HT3 and NK-1 receptors, rather than inhibiting 5-HT3 receptors alone, has demonstrated superior protection from CINV5,9
 

Use of combination therapeutics provides greater efficacy and prevention of delayed CINV symptoms5

CINV combination therapy
  • Emetogenic chemotherapy triggers receptors in both the peripheral and central nervous systems5,8,10
  • Following chemotherapy administration, the delayed phase of CINV (25-120 h) is driven by the release of the neurotransmitter substance P8,10
  • Substance P is highly concentrated in the emetic centers of the brain and binds to the NK-1 receptor, stimulating induction of vomiting pathways10,11
 
 

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. Grunberg SM, Deuson RR, Mavros P, et al. Incidence of chemotherapy-induced nausea and emesis after modern antiemetics. Cancer. 2004;100(10):2261-2268. 2. Salsman JM, Grunberg SM, Beaumont JL, et al. Communicating about chemotherapy-induced nausea and vomiting: a comparison of patient and provider perspectives. J Natl Compr Canc Netw. 2012;10(2):149-157. 3. Majem M, Moreno ME, Calvo N, et al. Perception of healthcare providers versus patient reported incidence of chemotherapy-induced nausea and vomiting after the addition of NK-1 receptor antagonists. Support Care Cancer. 2010;19(12):1983-1990. 4. Sun CC, Bodurka DC, Weaver CB, et al. Rankings and symptom assessments of side effects from chemotherapy: insights from experienced patients with ovarian cancer. Support Care Cancer. 2005;13(4):219-227. 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. 6. Shih V, Wan HS, Chan A. Clinical predictors of chemotherapy-induced nausea and vomiting in breast cancer patients receiving adjuvant doxorubicin and cyclophosphamide. Ann Pharmacother. 2009;43(3):444-452. 7. Aziz F. Neurokinin-1 receptor antagonists for chemotherapy-induced nausea and vomiting. Ann Palliat Med. 2012;1(2):130-136. 8. Hesketh PJ, Van Belle S, Aapro M, et al. Differential involvement of neurotransmitters through the time course of cisplatin-induced emesis as revealed by therapy with specific receptor antagonists. Eur J Cancer. 2003;39(8):1074-1080. 9. Rojas C, Raje M, Tsukamoto T, Slusher BS. Molecular mechanisms of 5-HT3 and NK1 receptor antagonists in prevention of emesis. Eur J Pharmacol. 2014;722:26-37. 10. Janelsins MC, Tejani MA, Kamen C, Peoples AR, Mustian KM, Morrow GR. Current pharmacotherapy for chemotherapy-induced nausea and vomiting in cancer patients. Expert Opin Pharmacother. 2013;14(6):757-766. 11. Saito R, Takano Y, Kamiya HO. Roles of substance P and NK1 receptor in the brainstem in the development of emesis. J Pharmacol Sci. 2003;91(2):87-94.

 
 
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