Neurokinin-1 receptor antagonists: review of their role for the prevention of chemotherapy-induced nausea and vomiting in adults

References

• Ballatori E, Roila F, Ruggeri B, et al. The impact of chemotherapy-induced nausea and vomiting on health-related quality of life. Support Care Cancer. 2007;15(2):179–185.
   PubMed Web of Science ®Google Scholar
• Bloechl-Daum B, Deuson RR, Mavros P, et al. Delayed nausea and vomiting continue to reduce patients’ quality of life after highly and moderately emetogenic chemotherapy despite antiemetic treatment. J Clin Oncol. 2006;24(27):4472–4478.
   PubMed Web of Science ®Google Scholar
• Basch E, Deal AM, Kris MG, et al. Symptom monitoring with patient-reported outcomes during routine cancer treatment: A randomized controlled trial. J Clin Oncol. 2016;34(6):557–565.
   PubMed Web of Science ®Google Scholar
• Basch E, Deal AM, Dueck AC, et al. Overall survival results of a trial assessing patient-reported outcomes for symptom monitoring during routine cancer treatment. JAMA. 2017;318(2):197–198.
   Google Scholar
• Dibble SL, Isreal J, Nussey B, et al. Delayed chemotherapy-induced nausea in women treated for breast cancer. Oncol Nurs Forum. 2003;30(2):E40–7.
   PubMedGoogle Scholar
• Cohen L, de Moor CA, Eisenberg P, et al. Chemotherapy-induced nausea and vomiting: incidence and impact on patient quality of life at community oncology settings. Support Care Cancer. 2007;15(5):497–503.
   PubMed Web of Science ®Google Scholar
• Tortorice PV, O’Connell MB. Management of chemotherapy-induced nausea and vomiting. Pharmacotherapy. 1990;10(2):129–145.
   PubMed Web of Science ®Google Scholar
• 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.
   PubMed Web of Science ®Google Scholar
• Janelsins MC, Tejani MA, Kamen C, et al. Current pharmacotherapy for chemotherapy-induced nausea and vomiting in cancer patients. Expert Opin Pharmacother. 2013;14(6):757–766.
   PubMed Web of Science ®Google Scholar
• Roila F, Molassiotis A, Herrstedt J, et al. MASCC and ESMO guideline update for the prevention of chemotherapy- and radiotherapy-induced nausea and vomiting and of nausea and vomiting in advanced cancer patients. Ann Oncol. 2016;27(suppl 5):v119–33.
   PubMed Web of Science ®Google Scholar
• Hesketh PJ, Kris MG, Basch E, et al. Antiemetics: American society of clinical oncology clinical practice guideline update. J Clin Oncol. 2017;35(28):3240–3261.
   PubMed Web of Science ®Google Scholar
• National Comprehensive Cancer Network. NCCN clinical practice guidelines (NCCN Guidelines®). Antiemesis. 2019. Version 1.2019
   Google Scholar
• Aapro MS, Alberts DS. High-dose dexamethasone for prevention of cis-platin-induced vomiting. Cancer Chemother Pharmacol. 1981;7(1):11–14.
   PubMed Web of Science ®Google Scholar
• Gralla RJ, Itri LM, Pisko SE, et al. Antiemetic efficacy of high-dose metoclopramide: randomized trials with placebo and prochlorperazine in patients with chemotherapy-induced nausea and vomiting. N Engl J Med. 1981;305(16):905–909.
   PubMed Web of Science ®Google Scholar
• Joss RA, Bacchi M, Buser K, et al. Ondansetron plus dexamethasone is superior to ondansetron alone in the prevention of emesis in chemotherapy-naive and previously treated patients. Swiss group for clinical cancer research (SAKK). Ann Oncol. 1994;5(3):253–258.
   PubMed Web of Science ®Google Scholar
• Navari RM, Aapro M. Antiemetic prophylaxis for chemotherapy-induced nausea and vomiting. N Engl J Med. 2016;374(14):1356–1367.
   PubMed Web of Science ®Google Scholar
• Hainsworth J, Harvey W, Pendergrass K, et al. A single-blind comparison of intravenous ondansetron, a selective serotonin antagonist, with intravenous metoclopramide in the prevention of nausea and vomiting associated with high-dose cisplatin chemotherapy. J Clin Oncol. 1991;9(5):721–728.
   PubMed Web of Science ®Google Scholar
• Jordan K, Jahn F, Aapro M. Recent developments in the prevention of chemotherapy-induced nausea and vomiting (CINV): a comprehensive review. Ann Oncol. 2015;26(6):1081–1090.
   PubMed Web of Science ®Google Scholar
• Jordan K, Gralla R, Rizzi G, et al. Efficacy benefit of an NK1 receptor antagonist (NK1RA) in patients receiving carboplatin: supportive evidence with NEPA (a fixed combination of the NK1 RA, netupitant, and palonosetron) and aprepitant regimens. Support Care Cancer. 2016;24(11):4617–4625.
   PubMed Web of Science ®Google Scholar
• Hesketh PJ, Schnadig ID, Schwartzberg LS, et al. Efficacy of the neurokinin-1 receptor antagonist rolapitant in preventing nausea and vomiting in patients receiving carboplatin-based chemotherapy. Cancer. 2016;122(15):2418–2425.
   PubMed Web of Science ®Google Scholar
• Zhang Y, Yang Y, Zhang Z, et al. Neurokinin-1 receptor antagonist-based triple regimens in preventing chemotherapy-induced nausea and vomiting: a network meta-analysis. J Natl Cancer Inst. 2016;109(2):djw217.
   Google Scholar
• Zhang Y, Hou X, Zhang R, et al. Optimal prophylaxis of chemotherapy-induced nausea and vomiting for moderately emetogenic chemotherapy: a meta-analysis. Future Oncol. 2018;14(19):1933–1941.
   PubMed Web of Science ®Google Scholar
• Di Maio M, Baratelli C, Bironzo P, et al. Efficacy of neurokinin-1 receptor antagonists in the prevention of chemotherapy-induced nausea and vomiting in patients receiving carboplatin-based chemotherapy: A systematic review and meta-analysis. Crit Rev Oncol Hematol. 2018;124:21–28.
   PubMed Web of Science ®Google Scholar
• Peroutka SJ, Snyder SH. Antiemetics: neurotransmitter receptor binding predicts therapeutic actions. Lancet. 1982;1(8273):658–659.
   PubMed Web of Science ®Google Scholar
• Borison HL, McCarthy LE. Neuropharmacology of chemotherapy-induced emesis. Drugs. 1983;25(suppl 1):8–17.
   PubMed Web of Science ®Google Scholar
• Clark-Snow RA, VIdall C, Börjeson S, et al. Fixed combination antiemetic: a literature review on prevention of chemotherapy-induced nausea and vomiting using netupitant/palonosetron. Clin J Oncol Nurs. 2018;22(2):E52–E63.
   Google Scholar
• Hesketh PJ. Chemotherapy-induced nausea and vomiting. N Engl J Med. 2008;358(23):2482–2494.
   PubMed Web of Science ®Google Scholar
• Wickham R. Evolving treatment paradigms for chemotherapy-induced nausea and vomiting. Cancer Control. 2012;19(2 suppl):3–9.
   PubMed Web of Science ®Google Scholar
• Aapro M, Molassiotis A, Dicato M, et al. The effect of guideline-consistent antiemetic therapy on chemotherapy-induced nausea and vomiting (CINV): the Pan European Emesis Registry (PEER). Ann Oncol. 2012;23(8):1986–1992.
   PubMed Web of Science ®Google Scholar
• Dranitsaris G, Molassiotis A, Clemons M, et al. The development of a prediction tool to identify cancer patients at high risk for chemotherapy-induced nausea and vomiting. Ann Oncol. 2017;28(6):1260–1267.
   PubMed Web of Science ®Google Scholar
• Aapro M, Ruffo P, Panteri R, et al. Oncologist perspectives on chemotherapy-induced nausea and vomiting (CINV) management and outcomes: A quantitative market research-based survey. Cancer Rep. 2018;1:e1127.
   Google Scholar
• Grunberg SM, Deuson RR, Mavros P, et al. Incidence of chemotherapy-induced nausea and emesis after modern antiemetics. Cancer. 2004;100(10):2261–2268.
   PubMed Web of Science ®Google Scholar
• Basch E. The missing voice of patients in drug-safety reporting. N Engl J Med. 2010;362(10):865–869.
   PubMed Web of Science ®Google Scholar
• 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.
   PubMed Web of Science ®Google Scholar
• Dielenseger P, Börjeson S, Vidall C, et al. Evaluation of antiemetic practices for prevention of chemotherapy-induced nausea and vomiting (CINV): results of a European oncology nurse survey. Support Care Cancer. 2019. DOI:10.1007/s00520-019-04697-1
   PubMed Web of Science ®Google Scholar
• Clark-Snow R, Affronti ML, Rittenberg CN. Chemotherapy-induced nausea and vomiting (CINV) and adherence to antiemetic guidelines: results of a survey of oncology nurses. Support Care Cancer. 2018;26(2):557–564.
   PubMed Web of Science ®Google Scholar
• Caberlotto L, Hurd YL, Murdock P, et al. Neurokinin 1 receptor and relative abundance of the short and long isoforms in the human brain. Eur J Neurosci. 2003;17(9):1736–1746.
   PubMed Web of Science ®Google Scholar
• Tattersall FD, Rycroft W, Francis B, et al. Tachykinin NK1 receptor antagonists act centrally to inhibit emesis induced by the chemotherapeutic agent cisplatin in ferrets. Neuropharmacology. 1996;35(8):1121–1129.
   PubMed Web of Science ®Google Scholar
• Emend® (aprepitant) [prescribing information]. Whitehouse Station, NJ, USA: Merck Sharp & Dohme Corp; 2019.
   Google Scholar
• Cinvanti® (aprepitant) injectable emulsion [prescribing information]. San Diego, CA, USA: Heron Therapeutics, Inc; 2019.
   Google Scholar
• Emend® (fosaprepitant) for injection, for intravenous use [prescribing information]. Whitehouse Station, NJ, USA: Merck Sharp & Dohme Corp; 2018.
   Google Scholar
• Varubi® (rolapitant) tablets and Varubi® (rolapitant) injectable emulsion [prescribing information]. Waltham, MA, USA: TESARO Inc; 2018.
   Google Scholar
• US Food and drug Administration. Safety alerts for human medical products. Varubi (rolapitant) injectable emulsion: health care provider letter - anaphylaxis and other serious hypersensitivity reactions. Silver Spring (MD); 2018 Jan 16 [cited 2019 Mar]. Available from: https://www.fda.gov/safety/medwatch/safetyinformation/safetyalertsforhumanmedicalproducts/ucm592592.htm
   Google Scholar
• Akynzeo® (netupitant and palonosetron) capsules; Akynzeo® (fosnetupitant and palonosetron) for injection [prescribing information]. Dublin, Ireland: Helsinn Birex Pharmaceuticals Ltd; 2018.
   Google Scholar
• Kurteva G, Chilingirova N, Rizzi G, et al. Pharmacokinetics (PK) and safety of intravenous fixed combination fosnetupitant/palonosetron (IV NEPA) for prevention of chemotherapy-induced nausea and vomiting in highly emetogenic chemotherapy (HEC). Presented at: Hematology/Oncology Pharmacy Association 14th Annual Conference; 2018 Mar 21–24; Denver, CO.
   Google Scholar
• Stathis M, Pietra C, Rojas C, et al. Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects. Eur J Pharmacol. 2012;689(1–3):25–30.
   PubMed Web of Science ®Google Scholar
• Rojas C, Raje M, Tsukamoto T, et al. Molecular mechanisms of 5-HT(3) and NK(1) receptor antagonists in prevention of emesis. Eur J Pharmacol. 2014;722:26–37.
   PubMed Web of Science ®Google Scholar
• Thomas AG, Stathis M, Rojas C, et al. Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014;232(8):2637–2644.
   PubMed Web of Science ®Google Scholar
• Huskey SE, Dean BJ, Bakhtiar R, et al. Brain penetration of aprepitant, a substance P receptor antagonist, in ferrets. Drug Metab Dispos. 2003;31(6):785–791.
   PubMed Web of Science ®Google Scholar
• Duffy RA, Morgan C, Naylor R, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012;102(1):95–100.
   PubMed Web of Science ®Google Scholar
• Rizzi A, Campi B, Camarda V, et al. In vitro and in vivo pharmacological characterization of the novel NK1 receptor selective antagonist Netupitant. Peptides. 2012;37(1):86–97.
   PubMed Web of Science ®Google Scholar
• Bergström M, Hargreaves RJ, Burns HD, et al. Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant. Biol Psychiatry. 2004;55(10):1007–1012.
   PubMed Web of Science ®Google Scholar
• Wang X, Zhang ZY, Powers D, et al. Rolapitant absolute bioavailability and PET imaging studies in healthy adult volunteers. Clin Pharmacol Ther. 2017;102(2):332–339.
   PubMed Web of Science ®Google Scholar
• Spinelli T, Calcagnile S, Giuliano C, et al. Netupitant PET imaging and ADME studies in humans. J Clin Pharmacol. 2014;54(1):97–108.
   PubMed Web of Science ®Google Scholar
• Yasuno F, Sanabria SM, Burns D, et al. PET imaging of neurokinin-1 receptors with [(18)F]SPA-RQ in human subjects: assessment of reference tissue models and their test-retest reproducibility. Synapse. 2007;61(4):242–251.
   PubMed Web of Science ®Google Scholar
• Rapoport BL. Differential pharmacology and clinical utility of rolapitant in chemotherapy-induced nausea and vomiting. Cancer Manag Res. 2017;9:41–50.
   PubMed Web of Science ®Google Scholar
• Ottoboni T, Keller MR, Cravets M, et al. Bioequivalence of HTX-019 (aprepitant IV) and fosaprepitant in healthy subjects: a Phase I, open-label, randomized, two-way crossover evaluation. Drug Des Devel Ther. 2018;12:429–435.
   PubMed Web of Science ®Google Scholar
• Stiff PJ, Fox-Geiman MP, Kiley K, et al. Prevention of nausea and vomiting associated with stem cell transplant: results of a prospective, randomized trial of aprepitant used with highly emetogenic chemotherapy preparative regimens. Biol Blood Marrow Transplant. 2013;19(1):49–55.e1.
   PubMed Web of Science ®Google Scholar
• Schwartzberg L, Parisi S, Bernareggi A Model-predicted netupitant pharmacokinetic (PK) profiles on repeated-dose schedules: accumulation and safety considerations for chemotherapy-induced nausea and vomiting (CINV) prophylaxis in multiday emetogenic chemotherapy. Presented at: 2016 American Society of Health-System Pharmacists Midyear Clinical Meeting & Exhibition; 2016 Dec 4–8; Las Vegas, NV.
   Google Scholar
• Electronic Medicines Compendium. IVEMEND 150 mg powder for infusion [summary of product characteristics]. 2018 [cited 2019 Mar]. Available from: https://www.medicines.org.uk/emc/product/5947/smpc
   Google Scholar
• Sanchez RI, Wang RW, Newton DJ, et al. Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant. Drug Metab Dispos. 2004;32(11):1287–1292.
   PubMed Web of Science ®Google Scholar
• Shadle CR, Lee Y, Majumdar AK, et al. Evaluation of potential inductive effects of aprepitant on cytochrome P450 3A4 and 2C9 activity. J Clin Pharmacol. 2004;44(3):215–223.
   PubMed Web of Science ®Google Scholar
• Aapro MS, Walko CM. Aprepitant: drug-drug interactions in perspective. Ann Oncol. 2010;21(12):2316–2323.
   PubMed Web of Science ®Google Scholar
• Howell JE, Szabatura AH, Hatfield Seung A, et al. Characterization of the occurrence of ifosfamide-induced neurotoxicity with concomitant aprepitant. J Oncol Pharm Pract. 2008;14(3):157–162.
   PubMedGoogle Scholar
• Séjourné A, Noal S, Boone M, et al. Two cases of fatal encephalopathy related to ifosfamide: an adverse role of aprepitant? Case Rep Oncol. 2014;7(3):669–672.
   PubMedGoogle Scholar
• Marbury TC, Ngo PL, Shadle CR, et al. Pharmacokinetics of oral dexamethasone and midazolam when administered with single-dose intravenous 150 mg fosaprepitant in healthy adult subjects. J Clin Pharmacol. 2011;51(12):1712–1720.
   PubMed Web of Science ®Google Scholar
• Depré M, Van Hecken A, Oeyen M, et al. Effect of aprepitant on the pharmacokinetics and pharmacodynamics of warfarin. Eur J Clin Pharmacol. 2005;61(5–6):341–346.
   PubMed Web of Science ®Google Scholar
• Feuring M, Lee Y, Orlowski LH, et al. Lack of effect of aprepitant on digoxin pharmacokinetics in healthy subjects. J Clin Pharmacol. 2003;43(8):912–917.
   PubMed Web of Science ®Google Scholar
• Egerer G, Eisenlohr K, Gronkowski M, et al. The NK1 receptor antagonist aprepitant does not alter the pharmacokinetics of high-dose melphalan chemotherapy in patients with multiple myeloma. Br J Clin Pharmacol. 2010;70(6):903–907.
   PubMed Web of Science ®Google Scholar
• Gridelli C, Aapro M. Factors influencing the choice of 5-HT3-receptor antagonist antiemetics: focus on elderly cancer patients. Support Care Cancer. 2004;12(7):487–496.
   PubMed Web of Science ®Google Scholar
• Lanzarotti C, Rossi G. Effect of netupitant, a highly selective NK1 receptor antagonist, on the pharmacokinetics of midazolam, erythromycin, and dexamethasone. Support Care Cancer. 2013;21(10):2783–2791.
   PubMed Web of Science ®Google Scholar
• Aapro M, Rugo H, Rossi G, et al. A randomized phase III study evaluating the efficacy and safety of NEPA, a fixed-dose combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting following moderately emetogenic chemotherapy. Ann Oncol. 2014;25(7):1328–1333.
   PubMed Web of Science ®Google Scholar
• Hesketh PJ, Rossi G, Rizzi G, et al. Efficacy and safety of NEPA, an oral combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting following highly emetogenic chemotherapy: a randomized dose-ranging pivotal study. Ann Oncol. 2014;25(7):1340–1346.
   PubMed Web of Science ®Google Scholar
• Gralla RJ, Bosnjak SM, Hontsa A, et al. A phase III study evaluating the safety and efficacy of NEPA, a fixed-dose combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting over repeated cycles of chemotherapy. Ann Oncol. 2014;25(7):1333–1339.
   PubMed Web of Science ®Google Scholar
• Schwartzberg L, Roeland E, Andric Z, et al. Phase III safety study of intravenous NEPA: a novel fixed antiemetic combination of fosnetupitant and palonosetron in patients receiving highly emetogenic chemotherapy. Ann Oncol. 2018;29(7):1535–1540.
   PubMed Web of Science ®Google Scholar
• Aapro M, Jordan K, Palmas M, et al. No signals of increased toxicity after concomitant administration of NEPA with etoposide or docetaxel: pooled safety data analysis from 4 pivotal studies. Poster presented at: 2016 Multinational Association of Supportive Care in Cancer/International Society of Oral Oncology Annual Meeting on Supportive Care in Cancer; 2016 Jun 23–25; Adelaide, Australia.
   Google Scholar
• Calcagnile S, Lanzarotti C, Rossi G, et al. Effect of netupitant, a highly selective NK1 receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Support Care Cancer. 2013;21(10):2879–2887.
   PubMed Web of Science ®Google Scholar
• Aapro M, Zhang L, Yennu S, et al. Preventing chemotherapy-induced nausea and vomiting with netupitant/palonosetron, the first fixed combination antiemetic: current and future perspective. Future Oncol. 2019;15(10):1067–1084.
   PubMed Web of Science ®Google Scholar
• Campos D, Pereira JR, Reinhardt RR, et al. Prevention of cisplatin-induced emesis by the oral neurokinin-1 antagonist, MK-869, in combination with granisetron and dexamethasone or with dexamethasone alone. J Clin Oncol. 2001;19(6):1759–1767.
   PubMed Web of Science ®Google Scholar
• Hesketh PJ, Grunberg SM, Gralla RJ, et al. The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: a multinational, randomized, double-blind, placebo-controlled trial in patients receiving high-dose cisplatin—the aprepitant protocol 052 study group. J Clin Oncol. 2003;21(22):4112–4119.
   PubMed Web of Science ®Google Scholar
• Poli-Bigelli S, Rodrigues-Pereira J, Carides AD, et al. Addition of the neurokinin 1 receptor antagonist aprepitant to standard antiemetic therapy improves control of chemotherapy-induced nausea and vomiting. Results from a randomized, double-blind, placebo-controlled trial in Latin America. Cancer. 2003;97(12):3090–3098.
   PubMed Web of Science ®Google Scholar
• Schmoll HJ, Aapro MS, Poli-Bigelli S, et al. Comparison of an aprepitant regimen with a multiple-day ondansetron regimen, both with dexamethasone, for antiemetic efficacy in high-dose cisplatin treatment. Ann Oncol. 2006;17(6):1000–1006.
   PubMed Web of Science ®Google Scholar
• Warr DG, Hesketh PJ, Gralla RJ, et al. Efficacy and tolerability of aprepitant for the prevention of chemotherapy-induced nausea and vomiting in patients with breast cancer after moderately emetogenic chemotherapy. J Clin Oncol. 2005;23(12):2822–2830.
   PubMed Web of Science ®Google Scholar
• Herrstedt J, Muss HB, Warr DG, et al. Efficacy and tolerability of aprepitant for the prevention of chemotherapy-induced nausea and emesis over multiple cycles of moderately emetogenic chemotherapy. Cancer. 2005;104(7):1548–1555.
   PubMed Web of Science ®Google Scholar
• Rapoport BL, Jordan K, Boice JA, et al. Aprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with a broad range of moderately emetogenic chemotherapies and tumor types: a randomized, double-blind study. Support Care Cancer. 2010;18(4):423–431.
   PubMed Web of Science ®Google Scholar
• Grunberg S, Chua D, Maru A, et al. Single-dose fosaprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with cisplatin therapy: randomized, double-blind study protocol–EASE. J Clin Oncol. 2011;29(11):1495–1501.
   PubMed Web of Science ®Google Scholar
• Lasseter KC, Gambale J, Jin B, et al. Tolerability of fosaprepitant and bioequivalency to aprepitant in healthy subjects. J Clin Pharmacol. 2007;47(7):834–840.
   PubMed Web of Science ®Google Scholar
• Saito H, Yoshizawa H, Yoshimori K, et al. Efficacy and safety of single-dose fosaprepitant in the prevention of chemotherapy-induced nausea and vomiting in patients receiving high-dose cisplatin: a multicentre, randomised, double-blind, placebo-controlled phase 3 trial. Ann Oncol. 2013;24(4):1067–1073.
   PubMed Web of Science ®Google Scholar
• Weinstein C, Jordan K, Green SA, et al. Single-dose fosaprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with moderately emetogenic chemotherapy: results of a randomized, double-blind phase III trial. Ann Oncol. 2016;27(1):172–178.
   PubMed Web of Science ®Google Scholar
• Ottoboni T, Lauw M, Keller MR, et al. Safety of HTX-019 (intravenous aprepitant) and fosaprepitant in healthy subjects. Future Oncol. 2018;14(27):2849–2859.
   PubMed Web of Science ®Google Scholar
• Schwartzberg LS, Navari RM. Safety of polysorbate 80 in the oncology setting. Adv Ther. 2018;35(6):754–767.
   PubMed Web of Science ®Google Scholar
• Ottoboni T, Lauw M, Keller MR, et al. HTX-019 via 2-min injection or 30-min infusion in healthy subjects. Future Oncol. 2019;15(8):865–874.
   PubMed Web of Science ®Google Scholar
• US Food and Drug Administration. FDA approves new drug treatment for nausea and vomiting from chemotherapy. Silver Spring (MD); 2015 Sep [cited 2019 Mar]. Available from: https://wayback.archive-it.org/7993/20180126023448/https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm460838.htm
   Google Scholar
• European Medicines Agency. Varuby (rolapitant). 2017 [cited 2019 Mar]. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/Summary_of_opinion_-_Initial_authorisation/human/004196/WC500222193.pdf
   Google Scholar
• 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. Lancet Oncol. 2015;16(9):1071–1078.
   PubMed Web of Science ®Google Scholar
• 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 randomised, active-controlled, double-blind, phase 3 trials. Lancet Oncol. 2015;16(9):1079–1089.
   PubMed Web of Science ®Google Scholar
• US Food and Drug Administration. FDA approves Akynzeo for nausea and vomiting associated with cancer chemotherapy. Silver Spring (MD); 2014 Oct [cited 2019 Mar]. Available from: https://wayback.archive-it.org/7993/20161022101304/http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm418375.htm
   Google Scholar
• European Medicines Agency. Akynzeo (netupitant/palonosetron). 2015 [cited 2019 Mar]. Available from: http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/003728/human_med_001862.jsp&mid=WC0b01ac058001d124
   Google Scholar
• Schwartzberg L, Karthaus M, Rossi G, et al. Fixed combination of oral NEPA (netupitant-palonosetron) for the prevention of acute and delayed chemotherapy-induced nausea and vomiting in patients receiving multiple cycles of chemotherapy: efficacy data from 2 randomized, double-blind phase III studies. Cancer Med. 2019 [cited Mar]. DOI:10.1002/cam4.2091.
   PubMed Web of Science ®Google Scholar
• Zhang L, Lu S, Feng J, et al. A randomized phase III study evaluating the efficacy of single-dose NEPA, a fixed antiemetic combination of netupitant and palonosetron, versus an aprepitant regimen for the prevention of chemotherapy-induced nausea and vomiting (CINV) in patients receiving highly emetogenic chemotherapy (HEC). Ann Oncol. 2018;29(2):452–458.
   PubMed Web of Science ®Google Scholar
• Roeland E, Binder G, Ma J, et al. Evaluation of daily breakthrough chemotherapy-induced nausea and vomiting (CINV) rates in a phase III study of NEPA versus an aprepitant (APR)/granisetron (GRAN) regimen. J Clin Oncol. 2017;35(31 suppl):abstract 120.
   Web of Science ®Google Scholar
• ALOXI® (palonosetron) [prescribing information]. Dublin, Ireland: Helsinn Birex Pharmaceuticals Ltd; 2018.
   Google Scholar
• Karthaus M, Szabò P, Voisin D, et al. Phase III study of palonosetron (PALO) given as 30-min IV infusion (IV inf) versus 30-sec IV bolus (IV bol) for prevention of chemotherapy-induced nausea and vomiting (CINV) associated with highly emetogenic chemotherapy (HEC). J Clin Oncol. 2017;35(31 suppl):abstract 227.
   Web of Science ®Google Scholar
• Roeland E, Hesketh PJ, Zhang L, et al. Efficacy of an intravenous formulation of NEPA, a fixed combination of fosnetupitant and palonosetron, compared with oral NEPA studies in the prevention of chemotherapy-induced nausea and vomiting (CINV): an analysis of 1026 patient experiences. J Clin Oncol. 2018;36(15 suppl):abstract e22177.
   Web of Science ®Google Scholar
• Dos Santos LV, Souza FH, Brunetto AT, et al. Neurokinin-1 receptor antagonists for chemotherapy-induced nausea and vomiting: a systematic review. J Natl Cancer Inst. 2012;104(17):1280–1292.
   PubMedGoogle Scholar
• Yuan DM, Li Q, Zhang Q, et al. Efficacy and safety of neurokinin-1 receptor antagonists for prevention of chemotherapy-induced nausea and vomiting: systematic review and meta-analysis of randomized controlled trials. Asian Pac J Cancer Prev. 2016;17(4):1661–1675.
   PubMedGoogle Scholar
• Spinelli T, Moresino C, Baumann S, et al. Effects of combined netupitant and palonosetron (NEPA), a cancer supportive care antiemetic, on the ECG of healthy subjects: an ICH E14 thorough QT trial. Springerplus. 2014;3:389.
   PubMed Web of Science ®Google Scholar
• Ruhlmann CH, Christensen TB, Dohn LH, et al. Efficacy and safety of fosaprepitant for the prevention of nausea and emesis during 5 weeks of chemoradiotherapy for cervical cancer (the GAND-emesis study): a multinational, randomised, placebo-controlled, double-blind, phase 3 trial. Lancet Oncol. 2016;17(4):509–518.
   PubMed Web of Science ®Google Scholar
• Leal AD, Kadakia KC, Looker S, et al. Fosaprepitant-induced phlebitis: a focus on patients receiving doxorubicin/cyclophosphamide therapy. Support Care Cancer. 2014;22(5):1313–1317.
   PubMed Web of Science ®Google Scholar
• Hegerova LT, Leal AD, Grendahl DC, et al. An analysis of fosaprepitant-induced venous toxicity in patients receiving highly emetogenic chemotherapy. Support Care Cancer. 2015;23(1):55–59.
   PubMed Web of Science ®Google Scholar
• Sato Y, Kondo M, Inagaki A, et al. Highly frequent and enhanced injection site reaction induced by peripheral venous injection of fosaprepitant in anthracycline-treated patients. J Cancer. 2014;5(5):390–397.
   PubMed Web of Science ®Google Scholar
• Boccia R, Geller RB, Clendeninn N, et al. Hypersensitivity and infusion-site adverse events with intravenous fosaprepitant after anthracycline-containing chemotherapy: a retrospective study. Future Oncol. 2019;15(3):297–303.
   PubMed Web of Science ®Google Scholar
• Navari RM. HTX-019: polysorbate 80- and synthetic surfactant-free neurokinin 1 receptor antagonist for chemotherapy-induced nausea and vomiting prophylaxis. Future Oncol. 2019;15(3):241–255.
   PubMed Web of Science ®Google Scholar
• Wang X, Zhang ZY, Powers D, et al. Bioequivalence of intravenous and oral rolapitant: results from a randomized, open-label pivotal study. J Clin Pharmacol. 2017;57(12):1600–1606.
   PubMed Web of Science ®Google Scholar
• Wang X, Zhang ZY, Wang J, et al. Pharmacokinetics, safety, and tolerability of rolapitant administered intravenously following single ascending and multiple ascending doses in healthy subjects. Clin Pharmacol Drug Dev. 2019;8(2):160–171.
   PubMed Web of Science ®Google Scholar
• de Wit R, Herrstedt J, Rapoport B, et al. The oral NK1 antagonist, aprepitant, given with standard antiemetics provides protection against nausea and vomiting over multiple cycles of cisplatin-based chemotherapy: a combined analysis of two randomized, placebo-controlled phase III clinical trials. Eur J Cancer. 2004;40(3):403–410.
   PubMed Web of Science ®Google Scholar
• Rapoport B, Schwartzberg L, Chasen M, et al. Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy. Eur J Cancer. 2016;57:23–30.
   PubMed Web of Science ®Google Scholar
• Dechaphunkul A, Lu S, Olivari S, et al. Efficacy of single dose NEPA, a fixed combination of netupitant and palonosetron, versus a 3-day regimen of aprepitant/granisetron (APR/GRAN) for prevention of nausea in patients receiving high dose cisplatin. Presented at: ESMO Asia 2018 Congress; 2018 Nov 23 –25; Singapore.
   Google Scholar
• Aapro M, Spinelli T, Palmas M, et al. Association between neurokinin-1 (NK1) receptor occupancy (RO) of netupitant (NETU) and efficacy of NEPA, the fixed antiemetic combination of NETU and palonosetron (PALO). Poster presented at: 2015 Multinational Association of Supportive Care in Cancer/International Society of Oral Oncology Annual Meeting on Supportive Care in Cancer; 2015 Jun 25–27; Copenhagen, Denmark.
   Google Scholar
• Baron-Hay S, Aapro M, Bernareggi A, et al. Timing flexibility of oral NEPA, netupitant-palonosetron combination, administration for the prevention of chemotherapy-induced nausea and vomiting (CINV). Support Care Cancer. 2019;27(4):1309–1317.
   PubMed Web of Science ®Google Scholar