The safety of rolapitant for the treatment of nausea and vomiting associated with chemotherapy.

Introduction: Chemotherapy-induced nausea and vomiting is a significant clinical issue that affects patients' quality of life as well as treatment decisions. Significant improvements in the control of chemotherapy-induced nausea and vomiting have occurred in the past 15 years with the introduction of new antiemetic agents 5-HT3, receptor antagonists, neurokinin-1 receptor antagonists, and olanzapine. Oral (aprepitant, 2003; netupitant, 2014; rolapitant, 2015) neurokinin-1 receptor antagonists have been developed along with intravenous formulations (fosaprepitant, NEPA, rolapitant, HTX-019) for the prevention of chemotherapy-induced nausea and vomiting.Areas covered: This review presents a description of the safety and efficacy of rolapitant along with a comparison to the other oral and intravenous formulations of the neurokinin-1 receptor antagonists.

Expert Opinion: Oral rolapitant has been demonstrated in clinical trials to be safe and effective in controlling chemotherapy-induced nausea and vomiting in patients receiving moderately and highly emetogenic chemotherapy. Rolapitant has a longer half-life (180 h) than other commercially available NK-1 receptor antagonists and does not induce or inhibit CYP34A, unlike the other NK-1 receptor antagonists. Future studies may determine if these may be important clinical issues.