Rolapitant in the Treatment of Nausea and Vomiting Associated With Chemotherapy

摘要

Rolapitant is a long-acting neurokinin1 receptor antagonist (NK1 RA) which is metabolized by CYP3A4 but does not inhibit or induce it, thereby reducing potential drug interactions. Four initial randomized studies compared rolapitant with placebo when added to a 5-hydroxytryptamine3 receptor antagonist (5HT3 RA) and dexamethasone for chemotherapy-induced emesis. Three were with highly emetic chemotherapy (HEC) and one with moderately emetic chemotherapy (MEC) and anthracycline/cyclophosphamide (AC). The rolapitant groups receiving HEC yielded statistically significantly improved responses in all phases of emesis (except the acute and overall phases in study 2) when compared with active controls. Overall (0-120?h), the response was better in the rolapitant arm for AC (P?=?.0332) and non-AC MEC (including carboplatin) (P?=?.0003). The efficacy of rolapitant is sustained over multiple cycles. Rolapitant 180?mg orally is well tolerated with similar side effects between the rolapitant and active control arms. It is effective in younger and older adults. Further studies will define its place among other NK1 RAs.